Day: November 4, 2021

In 2019 BIOORG CHEM published article about ACID-BINDING PROTEIN; LINEAR-REGRESSION; CELL-GROWTH; QSAR; EXPRESSION; PLS; DISCOVERY; PROSTATE; DESIGN; POTENT in [Floresta, Giuseppe; Spampinato, Ambra; Zagni, Chiara; Rescifina, Antonio] Univ Catania, Dept Drug Sci, Vle A Doria 6, I-95125 Catania, Italy; [Floresta, Giuseppe] Univ Catania, Dept Chem Sci, Vle A Doria, I-95125 Catania, Italy; [Floresta, Giuseppe; Cilibrizzi, Agostino] Kings Coll London, Inst Pharmaceut Sci, Stamford St, London SE1 9NH, England; [Cilibrizzi, Agostino; Abbate, Vincenzo] Kings Coll London, Sch Populat Hlth & Environm Sci, Kings Forens, Franklin Wilkins Bldg,150 Stamford St, London SE1 9NH, England in 2019, Cited 68. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Name: 2-Aminobenzamide

Following on the recent publication of pharmacologically relevant effects, small molecule inhibitors of adipocyte fatty-acid binding protein 4 (FABP4) have attracted high interest. FABP4 is mainly expressed in macrophages and adipose tissue, where it regulates fatty acid storage and lipolysis, being also an important mediator of inflammation. In this regard, FABP4 recently demonstrated an interesting molecular target for the treatment of type 2 diabetes, other metabolic diseases and some type of cancers. In the past years, hundreds of effective FABP4 inhibitors have been synthesized. In this paper, a quantitative structure-activity relationship (QSAR) model has been produced, in order to predict the bioactivity of FABP4 inhibitors. The methodology has been combined with a scaffold-hopping approach, allowing to identify three new molecules that act as effective inhibitors of this protein. These molecules, synthesized and tested for their FABP4 inhibitor activity, showed IC(50 )values between 3.70 and 5.59 mu M, with a high level of agreement with the predicted values.

Name: 2-Aminobenzamide. Bye, fridends, I hope you can learn more about C7H8N2O, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

In 2019 BIOORG CHEM published article about INHIBITOR INHIBITORY-ACTIVITY; MUSHROOM TYROSINASE; ANTIVIRAL EVALUATION; ANTICANCER; ANTIBACTERIAL; ELUCIDATION; INSIGHTS in [Chortani, Sarra; Horchani, Mabrouk; Ben Jannet, Hichem; Romdhane, Anis] Univ Monasrir, Fac Sci Monastir, Lab Heterocycl Chem Nat Prod & React LR11ES39, Team Med Chem & Nat Prod, Ave Environm, Monastir 5019, Tunisia; [Nimbarte, Vijaykumar D.] Univ Havre, UFR Sci & Tech, Lab Chem, URCOM,EA 3221,INC3M CNRS,F3038, BP 1123,25 Rue Philipe Lebon, F-76063 Le Havre, France in 2019, Cited 44. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Product Details of 88-68-6

2-substitued-benzopyrimidinones 2 were synthesized in high to excellent yields in a single step via condensation of 2-aminobenzamide 1 with some aryl-aldehydes in the presence of iodine. Cyclocondensation reaction of hydrazides 3 which were obtained in two steps from benzopyrimidinones 2, with some electrophilic species such as 2,4-pentandione, 2,5-hexandione, 1-phenylbutan-1,3-dione and cyclic anyhdrides provided the new compounds 4a-c, 5a-c, 6a-c, 7a-c, 8a-c and 9a-c. The synthesized compounds were characterized by spectroscopic means. They were also evaluated for their anti-tyrosinase potential. The structure-activity relationship (SAR) was discussed on the basis of the molecular docking analysis.

Product Details of 88-68-6. Welcome to talk about 88-68-6, If you have any questions, you can contact Chortani, S; Nimbarte, VD; Horchani, M; Ben Jannet, H; Romdhane, A or send Email.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2) published in 2019. Safety of 2-Aminobenzamide, Reprint Addresses Moslin, R (corresponding author), Bristol Myers Squibb Res & Dev, Immunosci Discovery Chem, POB 4000, Princeton, NJ 08543 USA.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide

As a member of the Janus OAK) family of nonreceptor tyrosine kinases, TYK2 plays an important role in mediating the signaling of pro-inflammatory cytokines including IL-12, IL-23, and type 1 interferons. The nicotinamide 4, identified by a SPA-based high-throughput screen targeting the TYK2 pseudokinase domain, potently inhibits IL-23 and IFN alpha signaling in cellular assays. The described work details the optimization of this poorly selective hit (4) to potent and selective molecules such as 47 and 48. The discoveries described herein were critical to the eventual identification of the clinical TYK2 JH2 inhibitor (see following report in this issue). Compound 48 provided robust inhibition in a mouse IL-12-induced IFN gamma pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model. These results demonstrate the ability of TYK2 JH2 domain binders to provide a highly selective alternative to conventional TYK2 orthosteric inhibitors.

Welcome to talk about 88-68-6, If you have any questions, you can contact Moslin, R; Zhang, YL; Wrobleski, ST; Lin, SQ; Mertzman, M; Spergel, S; Tokarski, JS; Strnad, J; Gillooly, K; McIntyre, KW; Zupa-Fernandez, A; Cheng, LH; Sun, HD; Chaudhry, C; Huang, C; D’Arienzo, C; Heimrich, E; Yang, XX; Muckelbauer, JK; Chang, C; Tredup, J; Mulligan, D; Xie, DL; Aranibar, N; Chiney, M; Burke, JR; Lombardo, L; Carter, PH; Weinstein, DS or send Email.. Safety of 2-Aminobenzamide

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Hetero-Diels-Alder Reactions of In Situ-Generated Azoalkenes with Thioketones; Experimental and Theoretical Studies WOS:000650677000001 published article about THIOCARBONYL S-METHANIDES; EFFICIENT SYNTHESIS; 1,3-DIPOLAR CYCLOADDITIONS; FERROCENYL THIOKETONES; ALPHA-NITROSOALKENES; HETARYL; ARYL; CHEMISTRY; 1,2-DIAZA-1,3-DIENES; THIOCHALCONES in [Mloston, Grzegorz; Urbaniak, Katarzyna; Sobiecka, Malwina] Univ Lodz, Fac Chem, Dept Organ & Appl Chem, 12 Tamka St, PL-91403 Lodz, Poland; [Heimgartner, Heinz] Univ Zurich, Dept Chem, Winterthurerstr 190, CH-8057 Zurich, Switzerland; [Wuerthwein, Ernst-Ulrich] Westfalische Wilhelms Univ Munster, Organ Chem Inst, Corrensstr 40, D-48149 Munster, Germany; [Wuerthwein, Ernst-Ulrich] Westfalische Wilhelms Univ Munster, Ctr Multiscale Theory & Computat CMTC, Corrensstr 40, D-48149 Munster, Germany; [Zimmer, Reinhold; Lentz, Dieter; Reissig, Hans-Ulrich] Free Univ Berlin, Inst Chem & Biochem, Takustr 3, D-14195 Berlin, Germany in 2021.0, Cited 67.0. The Name is Benzophenone. Through research, I have a further understanding and discovery of 119-61-9. SDS of cas: 119-61-9

The hetero-Diels-Alder reactions of in situ-generated azoalkenes with thioketones were shown to offer a straightforward method for an efficient and regioselective synthesis of scarcely known N-substituted 1,3,4-thiadiazine derivatives. The scope of the method was fairly broad, allowing the use of a series of aryl-, ferrocenyl-, and alkyl-substituted thioketones. However, in the case of N-tosyl-substituted cycloadducts derived from 1-thioxo-2,2,4,4-tetramethylcyclobutan-3-one and the structurally analogous 1,3-dithione, a more complicated pathway was observed. By elimination of toluene sulfinic acid, the initially formed cycloadducts afforded 2H-1,3,4-thiadiazines as final products. Advanced DFT calculations revealed that the observed high regioselectivity was due to kinetic reaction control and that the (4 + 2)-cycloadditions of sterically less unhindered thiones occurred via highly unsymmetric transition states with shorter C..S-distances (2.27-2.58 angstrom) and longer N..C-distances (3.02-3.57 angstrom). In the extreme case of the sterically very hindered 2,2,4,4-tetramethylcyclobutan-1,3-dione-derived thioketones, a zwitterionic intermediate with a fully formed C-S bond was detected, which underwent ring closure to the 1,3,4-thiadiazine derivative in a second step. For the hypothetical formation of the regioisomeric 1,2,3-thiadiazine derivatives, the DFT calculations proposed more symmetric transition states with considerably higher energies.

SDS of cas: 119-61-9. Welcome to talk about 119-61-9, If you have any questions, you can contact Mloston, G; Urbaniak, K; Sobiecka, M; Heimgartner, H; Wurthwein, EU; Zimmer, R; Lentz, D; Reissig, HU or send Email.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Glucose and insulin responses to an intravenous glucose tolerance test administered to feed-restricted dairy cows receiving folic acid and vitamin B-12 supplements WOS:000471756100036 published article about INTRAMUSCULAR INJECTIONS; LACTATIONAL PERFORMANCE; DIETARY-SUPPLEMENTS; METABOLISM; RESISTANCE; METHIONINE; ENERGY; MILK; FOLATE in [Girard, C. L.; Vanacker, N.; Beaudet, V; Duplessis, M.; Lacasse, P.] Agr & Agroalimentaire Canada, Ctr Rech & Dev Sherbrooke, Sherbrooke, PQ J1M 0C8, Canada; [Vanacker, N.] Univ Sherbrooke, Dept Biol, Fac Sci, Sherbrooke, PQ J1K 2R1, Canada in 2019.0, Cited 37.0. Application In Synthesis of 1-Phenylurea. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8

The present experiment was conducted to determine whether, during periods of negative energy balance, the increase in glucose availability, despite similar DMI and greater milk production, induced by a combined supplement of folic acid and vitamin B-12 was related to effects of insulin on metabolism. Sixteen multiparous Holstein cows averaging 45 days in milk (standard deviation: 3) were assigned to 8 blocks of 2 animals each according to their milk production (45 kg/d; standard deviation: 6) during the week preceding the beginning of the experiment. Within each block, they received weekly intramuscular injections of either saline (CON) or folic acid and vitamin B-12 (VIT) during 5 consecutive weeks. During the last week, the cows were fed 75% of their ad libitum intake during 4 d. Blood samples were taken the morning before starting the feed restriction and on the third day of feed restriction. On the fourth day of feed restriction, the daily meal was not served and an intravenous glucose tolerance test was performed. During the 4 wk preceding the feed restriction, milk production and DMI were not affected by treatments. During the feed restriction, the vitamin supplement tended to decrease milk fat concentration and increase milk concentration of lactose. Plasma concentrations of homocysteine, Ile, Leu, Val, and branched-chain AA increased in VIT cows during the restriction but not in CON cows. During the glucose tolerance test, insulin peak height was lower and insulin incremental positive area under the curve tended to be lower for VIT than for CON [83 (95% confidence interval, CI: 64-108) vs. 123 (95% CI: 84-180) mu g.180 min/L, respectively]. Free fatty acid nadir was reached earlier for VIT than for CON [34 (95% CI: 26-43) vs. 46 (95% CI: 31-57) min, respectively]. Glucose area under the curve, clearance rate and peak height, insulin time to reach the peak and clearance rate, and free fatty acid nadir did not differ between VIT and CON. The reduction in insulin release during a glucose tolerance test without changes in glucose clearance rate or area under the curve suggests that the vitamin supplement improved insulin sensitivity in feed-restricted lactating dairy cows.

Application In Synthesis of 1-Phenylurea. Welcome to talk about 64-10-8, If you have any questions, you can contact Girard, CL; Vanacker, N; Beaudet, V; Duplessis, M; Lacasse, P or send Email.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Study on the performance and mechanism of degradation of toluene with non-thermal plasmas synergized supported TiO2/gamma-Al2O3 catalyst WOS:000670392300001 published article about BARRIER DISCHARGE REACTOR; BY-PRODUCTS; PHOTOCATALYTIC ACTIVITIES; ATMOSPHERIC-PRESSURE; VISIBLE-LIGHT; GAS-PHASE; REMOVAL; DECOMPOSITION; CONVERSION; OXIDATION in [Li, Mengyu; Li, Dandan; Zhang, Ziqi; Ji, Chunjie; Zhou, Shuo; Guo, Wenwen; Zhao, Chaocheng; Liu, Fang; Han, Fenglei] China Univ Petr East China, Sch Chem Engn, Qingdao 266580, Shandong, Peoples R China; [Zhao, Chaocheng; Liu, Fang; Han, Fenglei] Minist Sci & Technol, Key Lab Petr & Petrochem Pollut Control & Treatme, Beijing, Peoples R China in 2021.0, Cited 54.0. COA of Formula: C13H10O. The Name is Benzophenone. Through research, I have a further understanding and discovery of 119-61-9

The degradation of toluene in dielectric barrier discharge (DBD) reactor packed with supported photocatalysts TiO2/gamma-Al2O3, Ce-TiO2/gamma-Al2O3, Ag-TiO2/gamma-Al2O3, La-TiO2/gamma-Al2O3, and Co-TiO2/gamma-Al2O3 was investigated.The supported catalysts were prepared by sol-gel and impregnation methods and were characterized in detail using N-2 adsorption,XRD,TEM,XPS and UV-Vis analysis technology. Compared to the non-thermal plasma (NTP) alone system, the degradation rate of toluene and CO2 selectivity improved significantly with the combination of plasma and photocatalysts, meanwhile, the CO selectivity and the by-products NO2 and O-3 reduced. When the photocatalyst Ag-TiO2/gamma-Al2O3 was packed into the discharge region,this plasma-photocatalytic system could completely remove toluene with above 81% CO2 selectivity and greatly reduced concentration of poisonous byproducts (O-3 and NO2) at 5 kJ.L-1, while exhibiting superior stability. The energy efficiency of the hybrid system was increased by about 1.4-3 times, compared with the separated NTP. The main energy loss was the formation of by-products and the loss of light and heat. Finally, the intermediate products of the toluene degradation process of different catalyst systems were analyzed by GC-MS, and the mechanism of toluene degradation by the NTP-photocatalytic system was concluded. The process of NTP synergistic photocatalytic degradation of toluene mainly included three aspects: NTP degradation of toluene, photocatalytic oxidation degradation of toluene, and the synergistic effect between the two. The results can provide a theoretical basis for the study on the performance of VOCs degradation by NTP, and have certain guiding significance for the application and mechanism research of VOCs degradation by NTP.

COA of Formula: C13H10O. About Benzophenone, If you have any questions, you can contact Li, MY; Li, DD; Zhang, ZQ; Ji, CJ; Zhou, S; Guo, WW; Zhao, CC; Liu, F; Han, FL or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Category: thiomorpholine. Authors Gregson, CHU; Noble, A; Aggarwal, VK in WILEY-V C H VERLAG GMBH published article about in [Gregson, Charlotte H. U.; Noble, Adam; Aggarwal, Varinder K.] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England in 2021.0, Cited 44.0. The Name is Benzophenone. Through research, I have a further understanding and discovery of 119-61-9

The azetidine moiety is a privileged motif in medicinal chemistry and new methods that access them efficiently are highly sought after. Towards this goal, we have found that azabicyclo[1.1.0]butyl carbinols, readily obtained from the highly strained azabicyclo[1.1.0]butane (ABB), can undergo divergent strain-release reactions upon N-activation. Treatment with trifluoroacetic anhydride or triflic anhydride triggered a semipinacol rearrangement to give keto 1,3,3-substituted azetidines. More than 20 examples were explored, enabling us to evaluate selectivity and the migratory aptitude of different groups. Alternatively, treatment of the same alcohols with benzyl chloroformate in the presence of NaI led to iodohydrin intermediates which gave spiroepoxy azetidines upon treatment with base. The electronic nature of the activating agent dictates which pathway operates.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

I found the field of Chemistry very interesting. Saw the article CuI/I-2-Catalyzed Concise Synthesis of Substituted 6-Aminoisoquinolinoquinazoline Carboxylates from Anthranilamide published in 2020. Name: 2-Aminobenzamide, Reprint Addresses Alla, M (corresponding author), Indian Inst Chem Technol, CSIR, Div Fluoro & Agro Chem, Hyderabad 500007, Andhra Pradesh, India.; Alla, M (corresponding author), Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide

A one pot sequential addition protocol for synthesis of polycyclic quinazolines with beta-amino acid motifs has been achieved starting from anthranilamide. Initialin situformation of 2-(2-bromophenyl)quinazolin-4(3H)-one followed by addition of alkyl cyanoacetates catalyzed by copper (I) salts gives the target compound in good to excellent yields. The expedient and facile cascade protocol involves nucleophilic alpha-arylation, intramolecular cycloamidation of nitriles followed by 1,3-hydrogen shift allowing direct access to 6-amino-8-oxo-8H-isoquinolino[1,2-b]quinazoline-5-carboxylates.

Name: 2-Aminobenzamide. Welcome to talk about 88-68-6, If you have any questions, you can contact Reddy, PG; Indukuri, DR; Alla, M or send Email.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Ansari, SA; Deshmukh, SU; Patil, RB; Damale, MG; Patil, RH; Alkahtani, HM; Almehizia, AA; Al-Tuwajiri, HM; Aleanizy, FS; Alqahtani, FY; Pathan, SK; Sangshetti, JN in [Ansari, Siddique A.; Alkahtani, Hamad M.; Almehizia, Abdulrahman A.; Al-Tuwajiri, Hanaa M.] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, POB 2454, Riyadh 11451, Saudi Arabia; [Deshmukh, Satish U.] Deogiri Coll, Dept Chem, Aurangabad 431005, Maharashtra, India; [Patil, Rajesh B.] Smt Kashibai Navale Coll Pharm, Sinhgad Tech Educ Societys, Pune 411048, Maharashtra, India; [Damale, Manoj G.] Srinath Coll Pharm, Dept Pharmaceut Med Chem, Aurangabad 431136, Maharashtra, India; [Patil, Rajendra H.] Savitribai Phule Pune Univ, Dept Biotechnol, Pune 411007, Maharashtra, India; [Aleanizy, Fadilah S.; Alqahtani, Fulwah Y.] King Saud Univ, Dept Pharmaceutcs, Coll Pharm, POB 2454, Riyadh 11451, Saudi Arabia; [Pathan, Shahebaaz K.; Sangshetti, Jaiprakash N.] YB Chavan Coll Pharm, Dr Rafiq Zakaria Campus, Aurangabad 431001, Maharashtra, India published Identification of Promising Biofilm Inhibitory and Cytotoxic Quinazolin-4-one Derivatives: Synthesis, Evaluation, Molecular Docking and ADMET Studies in 2019, Cited 35. COA of Formula: C7H8N2O. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

A library of 2,3-dihydroquinazolin-4(1H)-one derivatives (5 a-k) were synthesized in good yield by using 1-Ethyl-3-Methylimidazolium hydrogen sulphate (10 mol %) as a catalyst and were evaluated for their anti-biofilm, antimicrobial and cytotoxicity potential. Among the synthesized compounds, 2-(4-(1H-1,2,4-triazol-1-yl)phenyl)-2,3-dihydroquinazolin-4(1H)-one (5d) and 2,3-dihydro-2-(2,4,6-trimethoxyphenyl) quinazolin-4(1H)-one (5j) displayed better anti-biofilm activity than fluconazole (IC50 = 40 mu M) with IC50 values less than 30 mu M. Compound 5d also appeared to be fungicidal against C. Albicans having MIC=33.5 mu g/ml comparable with standard fluconazole (50 mu g/ml). All the synthesized compounds were also evaluated for cytotoxic activity by using MTT assay against HeLa, A-549 and MDA-MB-231 cell lines. The compound 5d was found to be more potent against MDA-MB-231 and A549 cell lines (IC50 = 11 +/- 2 mu M and 34 +/- 8 mu M respectively) than 5-fluorouracil (IC50 = 19 +/- 3 mu M and 51 +/- 5 mu M respectively). The compounds substituted with 6-methyl-4-oxo-4H-chromen-3-yl (5a), biphenyl (5c) and 2-hydroxy-5-bromophenyl (5e) were also found to be more potent against MDA-MB-231 cell lines (IC50 = 13 +/- 3 – 14 +/- 4 mu M) than 5-fluorouracil. Molecular docking simulations were also carried out using secreted aspartyl protease (SAP5), pepA enzyme of C. albicans for biofilm inhibition and EGFR tyrosine kinase for cyto-toxicity studies. The study reveals that the compounds 5d and 5e can serve as an important lead moiety for biofilm inhibition and cyto-toxicity against MDA-MB-231 and A549 cancer cell-lines indicating their potential in the treatment of tougher fungal infections and breast and lung cancer.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Long, J; Selikhov, AN; Mamontova, E; Lyssenko, KA; Guari, Y; Larionova, J; Trifonov, AA in [Long, Jerome; Mamontova, Ekaterina; Guari, Yannick; Larionova, Joulia] Univ Montpellier, CNRS, Inst Charles Gerhardt, ENSCM,Equipe Ingenierie Mol & Nanoobjets, F-34095 Montpellier 5, France; [Selikhov, Alexander N.; Trifonov, Alexander A.] Russian Acad Sci, Inst Organometall Chem, 49 Tropinina Str,GSP-445, Nizhnii Novgorod 630950, Russia; [Selikhov, Alexander N.; Lyssenko, Konstantin A.; Trifonov, Alexander A.] Russian Acad Sci, Inst Organoelement Cpds, 28 Vavilova Str, Moscow, Russia; [Lyssenko, Konstantin A.] Moscow MV Lomonosov State Univ, Chem Dept, Moscow 119991, Russia published Synthesis, structure, magnetic and luminescence properties of two dysprosium single-molecule magnets based on phenoxide dye ligands in 2020, Cited 34. Formula: C14H10O. The Name is Anthrone. Through research, I have a further understanding and discovery of 90-44-8.

We report here two dysprosium complexes based on phenoxide-based emissive ligands 1-(2,4-dimetylphenylazo)-2-naphtholate (L1) and anthracenolate (L2). While 1 is a dinuclear homoleptic complex [Dy-2(L1)(6)].2C(7)H(8) exhibiting zero-field slow relaxation of magnetization, 2 is a mononuclear complex [Dy(L2)(3)(py)(3)] (py = pyridine) showing field-induced relaxation.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem