Heterocyclic Building Blocks-Thiomorpholine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.114525-81-4,(R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid,as a common compound, the synthetic route is as follows.,114525-81-4

Step a. Referring to Scheme 5-2, a mixture of compound 17 (667 mg, 2.4 mmol), (i^-N-Boc-thiomorpholine-S-carboxylic acid (594 mg, 2.4 mmol) and Et3N (486 mg, 4.8 mmol) in EtOAc (20 mL) was stirred at rt for 2h. Subsequently, the reaction mixture was concentrated and the residue was dried in vacuo to give crude compound 19, which was used for the next step without further purification. LC-MS (ESI): m/z 466.0 (M+Na)+.

The synthetic route of 114525-81-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRESIDIO PHARMACEUTICALS, INC.; LI, Leping; ZHONG, Min; WO2010/65668; (2010); A1;,
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128453-98-5, 4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid is a Thiomorpholine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,128453-98-5

To the reaction flask was added 1-tert-butoxycarbonylthiomorpholine-2-carboxylic acid (2.47 g, 10 mmol)And dichloromethane (20 mL),After stirring and dissolving,Ice bath cooling,Triethylamine (1.55 mL, 11 mmol) was added in turn,Isobutyl chloroformate (1.503 g, 11 mmol),After the reaction under ice bath for 1 hour,2,6-dimethylaniline 3a (1.51 g, 12.5 mmol) was added,The reaction was stirred at room temperature for 6 hours.(30 mL) and dichloromethane (20 mL) were added thereto, and the aqueous layer was extracted with dichloromethane (20 mL x 3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. Chromatography Separation and Purification (petroleum ether / ethyl acetate (v / v) = 5: 1-1: 1)To give a pale yellow solidTert-butyl 3 – ((2,6-dimethylphenyl) carbamoyl) thiomorpholine-4-carboxylate (40a) (1.57 g, yield 44.7%).

The synthetic route of 128453-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sichuan Hai Sike Pharmaceutical Co., Ltd.; Wang Wei; Chen Lei; Wang Wenjing; Wei Yonggang; Liu Zhenhong; Qin Linlin; (74 pag.)CN106928127; (2017); A;,
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Thiomorpholine | C4H9NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.39093-93-1,Thiomorpholine 1,1-dioxide,as a common compound, the synthetic route is as follows.,39093-93-1

Example 24 {6-[3-(3-Chloro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-(1,1-dioxo-1lambda6-thiomorpholin-4-yl)-methanone To a solution of 6-[3-(3-chloro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-nicotinic acid (69 mg, 0.2 mmol) in DMF (300 muL) were added 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (71 mg, 0.22 mmol), N,N-diisopropyl ethyl amine (171 muL, 1.0 mmol) and thiomorpholine-S,S-dioxide (0.22 mmol). The resulting reaction mixture was stirred for 1 h at room temperature. Concentration and purification by chromatography (SiO2, heptane:ethyl acetate=100:0 to 1:1) afforded the title compound (80 mg, 87percent) which was obtained as a white solid. MS: m/e=462.1 [M+H]+.

The synthetic route of 39093-93-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hoffmann-La Roche Inc.; Dott, Pascal; Hanlon, Steven Paul; Hildbrand, Stefan; Iding, Hans; Thomas, Andrew; Waldmeier, Pius; US2013/102778; (2013); A1;,
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Thiomorpholine | C4H9NS – PubChem

39093-93-1, Thiomorpholine 1,1-dioxide is a Thiomorpholine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,39093-93-1

Preparation 75 4-(3-Methoxy-4-nitrobenzyl)thiomorpholine-1,1-dioxide Thiomorpholine 1,1-dioxide (0.242 g, 1.788 mmol) and triethylamine (0.19 mL, 1.341 mmol) were added to a solution of 4-(bromomethyl)-2-methoxy-1-nitrobenzene (Preparation 74, 0.22 g, 0.894 mmol) in THF (2.2 mL). The reaction mixture was stirred overnight at room temperature before being concentrated under reduced pressure and purified via Biotage silica gel column chromatography eluting with (DCM/EtOAc 99/1 to 90/10) to afford the title product as a white solid (242 mg, 90percent). 1H NMR (500 MHz, CDCl3): delta 3.00-3.04 (m, 4H), 3.09-3.12 (m, 4H), 3.71 (s, 2H), 3.98 (s, 3H), 7.01 (m, 1H), 7.09 (m, 1H), 7.84 (d, J=8.2 Hz, 1H). LC (Method C)-MS (ESI, m/z) tR 2.03 min, 301 [(M+H+), 100percent].

The synthetic route of 39093-93-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; Bavetsias, Vassilios; Atrash, Butrus; Naud, Sebastien Gaston Andre; Sheldrake, Peter William; Blagg, Julian; US2013/345181; (2013); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59801-62-6,Thiomorpholine 1,1-dioxide hydrochloride,as a common compound, the synthetic route is as follows.,59801-62-6

After 158 mg of cis-(+)-2-(4-Bromomethylbenzyl)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1 -one obtained in the step 1 in Example 2-1 was dissolved in 20 mL of N,N-Dimethylformamide, 1.10 g of 1,1,-Dioxidothiomorpholine hydrochloride and 1.77 g of Potassium carbonate were added thereto and then the reaction liquid was stirred at room temperature for 9 hours. Water was added to the reaction liquid, and the reaction liquid was subjected to extraction procedure with ethyl acetate. The organic layer was washed with water and saturated saline and dried with anhydrous Magnesium sulfate, and the solvent was evaporated in vacuo. The crude product was purified through silica gel column chromatography to obtain 827 mg of the objective compound as a white amorphous substance. 1H-NMR(CDCl3) delta: 1.9-2.3(3H,m), 2.83(1H,t), 2.9-3.1(9H,m), 3.35(1H,ddd), 3.61(2H,s), 3.92(3H,s), 3.93(3H,s), 5.02(2H,dd), 5.73(2H,m), 6.86(1H,d), 7.2-7.3(3H,m), 7.36(2H,d), 7.46(1H,d) Specific rotation [alpha]D25 = 418.59 (c = 1.0, chloroform)

As the paragraph descriping shows that 59801-62-6 is playing an increasingly important role.

Reference£º
Patent; Nippon Shinyaku Co., Ltd.; EP1873147; (2008); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Thiomorpholine 1,1-dioxide, cas is 39093-93-1, it is a common heterocyclic compound, the Thiomorpholine compound, its synthesis route is as follows.

A mixture of 4-bromobenzyl bromide (1.0 g, 4.0 mmol), triethylamine (0.84 mL,6.0 mmol) and thiomorpholine 1,1-dioxide (1.09 g, 8.0 mmol) in THF (10 mL) was stirred at ambient temperature for 16 h. The solvent was evaporated and the resultant residue diluted with saturated aqueous sodium bicarbonate solution and extracted with ethyl acetate (2 x 50 mL). The combined organic layer was dried over sodium sulfate, filtered and evaporated to afford the title compound (0.90 g, 74percent). 1H NMR (CDCl3, 300MHz): 7.50-7.44 (m, 2H), 7.22-7.16 (m, 2H), 3.60 (s, 2H), 3.09-3.02 (m, 4H), 3.00-2.94 (m, 4H)., 39093-93-1

As the rapid development of chemical substances, we look forward to future research findings about 39093-93-1

Reference£º
Patent; GENENTECH, INC.; WO2009/151598; (2009); A1;,
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Thiomorpholine | C4H9NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20196-21-8,Thiomorpholin-3-one,as a common compound, the synthetic route is as follows.,20196-21-8

Preparation 4 4-(3,4-Dichlorophenyl)-thiomorpholin-3-one Under a nitrogen atmosphere in a flame-dried flask, sodium hydride (72 mg, 1.79 mmol, 60% oil dispersion) was washed with hexanes and then treated with 6 mL of anhydrous DMF, and cooled to 0 C. Thiomorpholin-3-one (200 mg, 1.71 mmol) was added in one portion with stirring. After gas evolution had stopped (ca. 30 min), 4-iodo-1,2-dichlorobenzene (700 mg, 2.56 mmol) was added, followed after 5 minutes by copper (I) bromide (490 mg, 3.42 mmol). After heating at 75 C. overnight, the mixture was partitioned between ethyl acetate and 1N lithium chloride, filtered through diatomaceous earth and combined with additional ethyl acetate washes of the diatomaceous earth filter cake. The organic layers were washed with additional 1N lithium chloride, brine (saturated sodium chloride) and dried over calcium sulfate (CaSO4). Concentration in vacuo gave 363 mg of light brown oil which was flash chromatographed (30-50% ethyl acetate in hexanes) to give a white solid, 108 mg. 1H-NMR (CDCl3, 400 MHz) d 7.44 (1H, d), 7.37 (1H, s), 7.12 (1H, dd), 3.93 (2H, t), 3.43 (2H, s), 3.01 (2H, t).

The synthetic route of 20196-21-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gibbs, Megan Ann; Howard, Harry Ralph; Sprouse, Jeffrey Scott; Schachter, Joel Barry; Chappell, Phillip Branch; US2002/49214; (2002); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Thiomorpholine 1,1-dioxide, cas is 39093-93-1, it is a common heterocyclic compound, the Thiomorpholine compound, its synthesis route is as follows.

N-(5-bromopentyl)phthalimide (1.2g, 4mmol) and thiomorpholine 1,1-dioxide (1.08g, 80mmol) and DIPEA (2ml, 11mmol) was added 10mL i-PrOH, the temperature was raised to 105 deg. C stirred for 16 hours. LCMS traced the reaction. After completion of the reaction it was concentrated, 50ml of water was added, sonicated, and filtered to give a white solid N-(5-(1,1-dioxothiomorpholin-4-yl)pentyl)phthalimide (1.0g, 97percent yield)., 39093-93-1

As the rapid development of chemical substances, we look forward to future research findings about 39093-93-1

Reference£º
Patent; Shenzen Chipscreen Biosciences Ltd.; Lu, Xianping; Liu, Jindi; Yang, Qianjiao; Li, Zhiping; Pan, Desi; Shan, Song; Zhu, Jiangfei; Wang, Xianghui; Liu, Xiangheng; Ning, Zhiqiang; (30 pag.)CN105481778; (2016); A;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Thiomorpholine 1,1-dioxide, cas is 39093-93-1, it is a common heterocyclic compound, the Thiomorpholine compound, its synthesis route is as follows.

Thiomorpholine 1,1-dioxide (2.00 g, 14.8 mmol) was dissolved in THF (20 mL) at 0 ¡ãC. Di-tert-butyl dicarbonate (3.55 g, 16.3 mmol) was added, followed by triethylamine (4.12 mL, 29.6 mmol). The resulting mixture was stirred at room temperature overnight. It was diluted with EtOAc and washed with brine. The organic layer was dried over MgS04 and concentrated. The crude residue obtained was subjected to purification on the ISCO using an 80 g column and eluting with 0-70percent EtOAc/hexanes (5percent KMnCn aq. was used in staining the TLC plates). The appropriate fractions were combined and concentrated to obtain (3.46 g, 99percent) of the title compound. NMR (400MHz, CDCh) delta 4.00 – 3.89 (m, 4H), 3.06 – 2.97 (m, 4H), 1.51 (s, 10H), 39093-93-1

As the rapid development of chemical substances, we look forward to future research findings about 39093-93-1

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; NORRIS, Derek J.; VACCARO, Wayne; DEBENEDETTO, Mikkel V.; DEGNAN, Andrew P.; DELUCCA, George V.; DESKUS, Jeffrey A.; HAN, Wen-Ching; KUMI, Godwin Kwame; SCHMITZ, William D.; STARRETT, John E., JR.; HILL, Matthew D.; HUANG, Hong; (563 pag.)WO2016/183118; (2016); A1;,
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Thiomorpholine | C4H9NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76176-87-9,Thiomorpholine-1-oxide hydrochloride,as a common compound, the synthetic route is as follows.,76176-87-9

To a suspension of Intermediate 41 (68.4 mg, 0.146 mmol, 1.0 eq) in anhydrous CH2CI2 (3 mL) was added 1-oxide thiomorpholine hydrochloride (45.6 mg, 0.293 mmol, 2.0 eq) and sodium acetate (24.0 mg, 0.293 mmol, 2.0 eq) and the resulting suspension was stirred at 42 C for 6 h. After cooling to rt, NaBH(OAc)3(62.1 mg, 0.293 mmol, 2.0 eq) was added and the reaction mixture was stirred at rt for 16 h. Additional portions of sodium acetate (12.0 mg, 0.147 mmol, 1.0 eq), 1-oxide thiomorpholine hydrochloride (22.8 mg, 0.147 mmol, 1.0 eq) and NaBH(OAc)3 (31.1 mg, 0.147 mmol, 1.0 eq) were added and the reaction was stirred at 40C for 18 h. Upon cooling to rt, the reaction was quenched with 1 Maqueous NaOH (5 mL) then poured into H20 (15 mL) and extracted with CH2CI2(3 x 15 mL). The combined organic extracts were concentrated in vacuo andpurified by silica gel chromatography using EtOAc/MeOH (1 :0-13:1). The productwas re-dissolved in CH2CI2/MeOH (4:1, 10 mL) and swirled with MP-TMT resin(157 mg, 0.173 mmol) at rt overnight. The solution was filtered and the resinwashed with CH2CI2/MeOH (4:1, 100 mL). The filtrate was concentrated in vacuoand purified a second time by silica gel column chromatography with CH2CI2/MeOH (1:0-12:1) to yield Example S as a white solid (37.6 mg, 45%).1H NMR (300MHz, DMSO-d5) oH. 12.47 (5, 1H), 8.54-8.67 (m, 2H), 8.28 (dd, J=7.4, 0.8 Hz, 1H), 7.98 (5, 1H), 7.64 (d, J=8.1 Hz, 1H), 7.40-7.52 (m, 1H), 4.08-4.19 (m, 4H), 3.81-3.92 (m, 6H), 2.86-3.02 (m, 4H), 2.68-2.80 (m, 4H).19F NMR (282MHz, DMSO-d5) 0F. -58.8 (5, 3F).MS (ESj 571.0 (100%, [M+H]j.

As the paragraph descriping shows that 76176-87-9 is playing an increasingly important role.

Reference£º
Patent; KARUS THERAPEUTICS LTD; SHUTTLEWORTH, Stephen Joseph; SILVA, Franck Alexandre; CECIL, Alexander Richard Liam; ALEXANDER, Rikki Peter; GATLAND, Alice Elizabeth; FINNEMORE, Daniel John; (123 pag.)WO2017/29521; (2017); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem