Heterocyclic Building Blocks-Thiomorpholine

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.

To a solution of compound 1 (21.0 mg, 0.0467 mmol, 1.0 eq) in DMF (1 ml_) was added A/,A/-diisopropylethylamine (32.6 pL, 0.187 mmol, 4.0 eq), HATU (26.7 mg, 0.0701 mmol, 1.5 eq) and thiomorpholine-1 -oxide hydrochloride (2) (14.6 mg, 0.0935 mmol, 2.0 eq). The reaction was stirred at room temperature for 17.5 h then diluted with EtOAc (10 ml_), washed with 1 M HCI (2 x 10 ml_) and brine (10 ml_), dried over MgS04, filtered and concentrated in vacuo. Purification by silica gel chromatography using hexane/EtOAc/MeOH (1 :0:0 – 0:1 :0 – 0:9: 1 ) yielded compound FD as a white solid (17.6 mg, 68%). (1239) LCMS (ES): Found 550.9 [M+Hf. (1240) 1H NMR (300MHz, DMSO-cf6), d: 8.88 (d, J=1.3 Hz, 1 H), 8.45 (dd, J=2.6, 1.5 Hz, 1 H), 8.36 (d, J=2.6 Hz, 1 H), 7.85 (d, J=9.4 Hz, 1 H), 7.81 (d, J=9.4 Hz, 1 H), 7.75 (d, J=3.8 Hz, 1 H), 7.32 (d, J=3.8 Hz, 1 H), 5.72-5.80 (m, 2H), 4.34-4.48 (m, 1 H), 3.89-4.06 (m, 2H), 3.66-3.84 (m, 1 H), 2.75-3.1 1 (m, 4H). (1241) 19F NMR (282MHz, DMSO-cf6), d: -64.79 (s, 3F).

76176-87-9 Thiomorpholine-1-oxide hydrochloride 20441479, aThiomorpholine compound, is more and more widely used in various.

Reference£º
Patent; KARUS THERAPEUTICS LIMITED; SHUTTLEWORTH, Stephen Joseph; GATLAND, Alice Elizabeth; FINNEMORE, Daniel John; ALEXANDER, Rikki Peter; SILVA, Franck; CECIL, Alexander; (233 pag.)WO2019/166824; (2019); 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.20196-21-8,Thiomorpholin-3-one,as a common compound, the synthetic route is as follows.

Step B Thiomorpholin-3-thione A mixture of 1.17 g (10 mmol) of thiomorpholin-3-one and 11 mmoles of Lawesson’s reagent in 25 mL of toluene was heated to reflux 2 hrs. The reaction mixture was cooled and the solvent was removed to give a residue. This was taken up in methylene chloride and applied on silica gel column and eluted with ethyl acetate containing methylene chloride (10%). The desired thiomorpholin-3-thione in 65% yield as a solid. 1 H NMR (CDCl3): 2.90(m,2H); 3.62(m,2H); 3.76(s,2H); 8.65(b,1H)

As the paragraph descriping shows that 20196-21-8 is playing an increasingly important role.

Reference£º
Patent; Merck & Co., Inc.; US5629322; (1997); A;,
Thiomorpholine – Wikipedia
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

[3740] A solution of methyl 3-fluoiO-4-((( l-methyl- l H-indazol-4-yl)amino)methyl)benzoate (0.384 g, 1.225 mmol), N,N-diisopropylethylamine ( 1.280 mL, 7.351 mmol) and triphosgene (0.182 g, 0.61 mmol) in dichloromethane (5 mL) was stirred at the room temperature for 30 min, and mixed with thiomorpholine 1 , 1 -dioxide (0.166 g, 1.225 mmol). The reaction mixture was stirred at the same temperature for additional 1 8 hr. Then, water was added to the reaction mixture, followed by extraction with dichloromethane. The bi-phasic mixture was passed through a plastic frit to remove the solid residues and aqueous layer, and the organic layer collected was concentrated in vacuo. The residue was chromatographed (Si02, 12 g cartridge; methanol / dichloromethane = 0 percent to 5 percent ) to give methyl 3-fluoro-4-((N-( l-methyl- l H-indazol-4-yl)- l , l-dioxidothiomorpholine-4-carboxamido )methyl)benzoate as pale yellow oil (0.531 g, 91.3 percent).

39093-93-1 Thiomorpholine 1,1-dioxide 6484228, aThiomorpholine compound, is more and more widely used in various.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; KIM, Yuntae; LEE, Chang Sik; SONG, Hyeseung; GWAK, Dal-Yong; LEE, Jaeyoung; OH, Jung Taek; LEE, Chang Gon; KIM, II Hyang; (1041 pag.)WO2017/23133; (2017); A2;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

20196-21-8, Thiomorpholin-3-one is a Thiomorpholine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 5 4-(4-Trifluoromethylphenyl)-thiomorpholin-3-one. A mixture of thiomorpholin-3-one (500 mg, 4.27 mmol), 4-trifluoromethyl-1-iodobenzene (1.25 mL, 8.5 mmol) and copper metal (814 mg, 12.8 mmol) was heated in a sealed glass tube at 185-200 C. for 18 hours. The residue was then purified by flash chromatography to give 260 mg of the title product as a white solid. M.p. 85-87 C. Mass spectrum 262 (M-1). 1H-NMR (CDCl3, 400 MHz) d 7.62 (2H, d), 7.37 (2H, d), 3.97 (2H, t), 3.43 (2H, s), 3.01 (2H, t).

As the paragraph descriping shows that 20196-21-8 is playing an increasingly important role.

Reference£º
Patent; Gibbs, Megan Ann; Howard, Harry Ralph; Sprouse, Jeffrey Scott; Schachter, Joel Barry; Chappell, Phillip Branch; US2002/49214; (2002); 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

A solution of MuomicronetaiotaomicronphiIotaiotaomicronGammaetaepsilon 1,1-dioxide (1.0 g, 7.40 mmol) in DCM (30 mL) was added dropwise over 20 min to a cooled (0 ¡ãC) and argon flushed mixture of 2-bromoacetyl bromide (970 L, 11.10 mmol) and K3PO4 (3.93 g, 18.5 mmol) in DCM (20 mL) and the mixture was stirred at RT overnight. The reaction mixture was diluted with DCM (50 mL) and quenched with aq. 0.5 M HC1 (10 mL). Water (50 mL) and brine (50 mL) were added and the layers were separated. The aqueous layer was extracted with DCM (50 mL) and the combined organic layers were washed with aq. 10percent KHCO3 (100 mL) and brine (50 mL), dried over Na2S04(s) and concentrated to dryness. The residue was triturated with Et20 (50 mL) for 30 min. The solid material was filtered off, washed with some Et20 and dried under reduced pressure to afford 2-bromo-l-(l,l- dioxidothiomo holino)ethanone (1.20 g, 4.69 mmol, 63percent). LCMS: calculated for [M+H]+= 256.1/258.1, found 256.0/258.0.

39093-93-1 Thiomorpholine 1,1-dioxide 6484228, aThiomorpholine compound, is more and more widely used in various.

Reference£º
Patent; GRUeNENTHAL GMBH; RATCLIFFE, Paul; KONETZKI, Ingo; SITNIKOV, Nikolay; KOCH, Thomas; JOSTOCK, Ruth; (121 pag.)WO2019/12037; (2019); 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.39093-93-1,Thiomorpholine 1,1-dioxide,as a common compound, the synthetic route is as follows.

A mixture of (S) – 4 – (1 – (4-fluoro-phenyl) – 2-methoxy-ethylamine) – 5-methyl-pyrrolo [2,1-f] [1, 2, 4] triazine-6-carboxylic acid (100 mg, 0 . 29mmol) and thiomorpholine -1,1-dioxide (58 mg, 0 . 44mmol) dissolved in N, N-dimethyl formamide (5 ml) in, then add 1-hydroxy benzotriazole (51 mg, 0 . 38mmol), 1-ethyl-3 – (3-dimethylamino-propyl) carbodiimide hydrochloride (74 mg, 0 . 38mmol) and triethylamine (88 mg, 0 . 87mmol), stirring the mixture at room temperature until the TLC reaction monitoring raw material the reaction is complete, to be added in to the reaction solution (100 ml), ethyl acetate (50 ml ¡Á 3) extraction, then by saturated sodium chloride solution (100 ml ¡Á 2) washing, the organic phase is dried with anhydrous sodium sulfate, concentrated under reduced pressure, the resulting residue is purified with silica gel column chromatography, to obtain (S) – (1,1-dioxy thiophosphoro morphline) – {4 – [1 – (4-fluorophenyl) – 2-methoxy-ethylamine] – 5-methyl-pyrrolo [2,1-f] [1, 2, 4] triazin-6-yl}}-methyl ketone (105 mg, white solid), yield: 78.4percent.

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

Reference£º
Patent; SHANGHAI CDYMAX PHARMACEUTICALS CO LTD; An, XiaoXia; Bie, PingYan; Yang, wuli; Liu, Jun; (49 pag.)CN103848833; (2016); B;,
Thiomorpholine – Wikipedia
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.

Trifluoro-methanesulfonic acid 3-cyano-6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazol-8-yl ester (Compound B1, 30 mg, 0.069 mmol) was dissolved in 1,4-dioxane (1 mL), added with thiomorpholine 1,1-dioxide (19 mg, 2 eq.), Pd2 (dba)3 (6.3 mg, 0.1 eq.), BINAP (8.6 mg, 0.2 eq.) and K3PO4 (29 mg, 2 eq.), and stirred at 100¡ã C. overnight. The reaction solution was added to water, and then extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over sodium sulfate. The drying agent was removed by filtration and the residues obtained after concentration under reduced pressure were purified by silica gel column chromatography (ethyl acetate/hexane) to obtain the target compound (white powder, 2.1 mg, 7percent). 1H-NMR (270 MHz, DMSO-d6) delta: 8. 29 (1H, d, J=8.6 Hz), 8. 07 (1H, d, J=8. 9 Hz), 8.00 (1H, s), 7. 55 (1H, dd, J=8. 5, 1. 7 Hz), 7. 34 (1H, d, J=2. 0 Hz), 7. 15 (1H, dd, J=9.1, 2.7 Hz), 4. 01 (4H, s), 3. 16 (4H, s), 1. 77 (6H, s).LCMS: m/z 420 [M+H]+

39093-93-1 Thiomorpholine 1,1-dioxide 6484228, aThiomorpholine compound, is more and more widely used in various.

Reference£º
Patent; Chugai Seiyaku Kabushiki Kaisha; US2012/83488; (2012); A1;,
Thiomorpholine – Wikipedia
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

To a mixture of 1-bromo-4- (bromomethyl) benzene (500 mg, 2.00 mmol) and thiomorpholine 1, 1-dioxide (513 mg, 2.99 mmol) was added THF (10 mL) and triethylamine (0.84 mL) in turn. After the mixture was stirred at rt for 15 h, the raw materail was consumed monitored by TLC. The reaction mixture was diluted with EtOAc (200 mL) and washed with saturated aqueous NaCl (50 mL) three times. The combined organic layers were concentrated in vacuo. The residue was purified by silica gel column chromatography eluted with PE/EtOAc (v/v) 3/1 to give a white solid product (310 mg, 50.9) .[0893]MS (ESI, pos. ion) m/z: 304.1 [M+1]+ and[0894]1H NMR (400 MHz, CDCl3) : delta (ppm) 7.46 (d, J 8.4 Hz, 2H) , 7.19 (d, J 8.4 Hz, 2H) , 3.59 (s, 2H) , 3.07-3.05 (m, 4H) , 2.98-2.95 (m, 4H)

39093-93-1 Thiomorpholine 1,1-dioxide 6484228, aThiomorpholine compound, is more and more widely used in various.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; LIU, Bing; ZHANG, Yingjun; CHENG, Changchung; HUANG, Jiuzhong; BAI, Shun; REN, Xingye; LI, Zhi; ZHOU, Youbai; (368 pag.)WO2016/615; (2016); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

59801-62-6, Thiomorpholine 1,1-dioxide hydrochloride is a Thiomorpholine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7-(3-chloro-phenylamino )-3-methyl-lH-pyrrolo[2,3-c ]pyridine-4-carboxylic acid (150mg) in dimethylformamide (4ml) was added 4-ethylmorpholine (253mul), thiomorpholine 1,1- dioxide hydrochloride (90. mg), 1-hydroxybenzotriazole hydrate (105mg) and 1-(3- dimethylaminopropyl) -3-ethylcarbodiimide hydrochloride (115mg) and the solution stirred at room temperature overnight. The dimethylformamide was evaporated and the residue dissolved in ethyl acetate (40ml) and washed with 5% sodium hydrogen carbonate solution (25ml) and water (25ml). The organic layer was dried (MgS04) and evaporated to give an orange oil. The residue was triturated with diethyl ether to give a white solid which was then filtered off, sucked dry then dried at 40C under vacuum to afford the title compound (75mg). NMR (d6-DMSO) 8 2.11 (3H, s), 2.49-2.57 (8H, m), 6.94 (1H, d), 7.31 (1H, t), 7.38 (1H, s), 7.73 (1H, d), 7.82 (1H, s), 8.32 (1H, s), 9.45 (1H, s), 11.65 (1H, brs). LC/MS [MH+] 419 consistent with molecular formula C19H1935ClN4O3S

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2005/121140; (2005); A1;,
Thiomorpholine – Wikipedia
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

(Step 3)1-BOC-3-bromo-5-bromomethyl-7-nitro-2-phenyl-indole (1.0 g, 2 mmol) obtained in Step 2 was dissolved in DCM (10 mL), and thereto Et3N (560 uL, 4 mmol) and 1,1-dioxo-thio-morpholine (300 mg, 3 mmol) were added. The mixture was stirred for 12 hours at room temperature. At the end of the reaction, added saturated aqueous NH4Cl solution, extracted with DCM. After drying the extract, the solvent was removed under reduced pressure and the residue was purified by column chromatography to give 1-BOC-3-bromo-5-(1,1-dioxo-thiomorpholine-4-yl)methyl-7-nitro-2-phenyl-1H-indole (825 mg, 78percent).

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

Reference£º
Patent; Kim, Soon Ha; Kim, Hyoung Jin; Chung, Chul Woong; Park, Heui Sul; Kwak, Hyo Shin; Kim, Sung Ho; Park, Jin Gu; US2010/291533; (2010); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem