Day: September 3, 2020

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

Production Example 4 Compound J7-4 9-(4-Isopropyl-piperazin-1-yl)-6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile [0519] trifluoro-methane sulfonic 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.), Pd2dba3 (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. all night and all day. The reaction solution was poured into 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 Compound B2-10 (8-(1,1-dioxothiomorpholino)-6,6-dimethyl-11-oxo-6,11 dih dro-5H-benzo b carbazole-3-carbonitrile) (white powder, 2.1 mg, 7percent)), the title compound was synthesized from the Compound J6 and 1-isopropyl-piperazine. [0521] 1H-NMR (270 MHz, DMSO-d6) delta: 12.80 (1H, s), 8.33 (1H, d, J=7.6 Hz), 8.02 (1H, s), 7.66 (3H, m), 7.33 (1H, d, J=8.2 Hz), 3.21 (4H, br), 2.66 (5H, m), 1.72 (6H, s), 1.02 (6H, d, J=6.3 Hz). [0522] LCMS: m/z 413 [M+H]+ [0523] HPLC retention time: 1.38 minutes (analysis condition S), 39093-93-1

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

Reference£º
Patent; Furumoto, Kentaro; Shiraki, Koji; Hirayama, Tomoaki; US2013/143877; (2013); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Name is Thiomorpholine-1-oxide hydrochloride, as a common heterocyclic compound, it belongs to Thiomorpholine compound, and cas is 76176-87-9, its synthesis route is as follows.,76176-87-9

Inermediate AU: (c/s)-5-lodo-7-[3-(1 -oxo-thiomorpholin-4-ylmethyl)-cyclobutyl]-7H- pyrrolo[2,3-d]pyrimidin-4-ylamineTo the stirred solution of (c/s)-[3-(4-amino-5-iodo-pyrrolo [2,3-d]pyrimidin-7-yl)-cyclobutyl] methanol (Intermediate J: 348 mg, 1.0 mmol) and acetonitrile (70 mL) was added IBX (Atlantic SciTech 86900: 561 mg, 2.0 mmol, 2 eq). The reaction mixture was stirred for 1 hour at 80 C. The reaction mixture was filtered at 40 C and the filtrate was concentrated. To the residue was added subsequently DCM (50 mL), ethyl-diisopropyl-amine (3.43 mL, 20 mmol, 20 eq), 1 -oxide thiomorpholin hydrochloride (312 mg, 2.0 mmol, 2 eq) and sodium triacetox- yborohydride (637 mg, 3.0 mmol, 3 eq) with stirring at room temperature. The reaction mixture was stirred for 1 hour at ro temperature and then partitioned between NaHC03 1 M and EtOAc. The combined organic layers were washed with water and brine, dried (Na2S04), filtered and concentrated. The residue was purified by silica gel column chromatography (DCM/MeOH/NH3aq, 200:20: 1 ) to afford the title compound as pale yellow crystals: HPLC/MS (Method Z) tR 0.92 minutes, M+H 446.2. TLC; Rf = 0.26 (DCM/MeOH/NH3aq, 200:20:1).

With the complex challenges of chemical substances, we look forward to future research findings about Thiomorpholine-1-oxide hydrochloride

Reference£º
Patent; NOVARTIS AG; IRM LLC, a Delaware Limited Liability Company; CHEN, Bei; FAIRHURST, Robin, Alec; FLOERSHEIMER, Andreas; FURET, Pascal; JIANG, Songchun; LU, Wenshuo; MARSILJE, Thomas, H.; VAUPEL, Andrea; WO2011/64211; (2011); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Name is Thiomorpholin-3-one, as a common heterocyclic compound, it belongs to Thiomorpholine compound, and cas is 20196-21-8, its synthesis route is as follows.,20196-21-8

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).

With the complex challenges of chemical substances, we look forward to future research findings about Thiomorpholin-3-one

Reference£º
Patent; Pfizer INC; US6423708; (2002); B1;,
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.,39093-93-1

A) 1,1-Dioxo-thiomorpholine-4-carbonyl Chloride To a solution of thiomorpholine 1,1-dioxide (0.181 g, 0.00105 mol) in dry THF (5 mL) was added DIPEA (0.3 mL, 0.00191 mol) at 0¡ã C. To the resulting mixture was added triphosgene (0.11 g, 0.00037 mol) and the mixture was stirred for 2 h at ambient temperature.

39093-93-1 is used more and more widely, we look forward to future research findings about Thiomorpholine 1,1-dioxide

Reference£º
Patent; Kilburn, John Paul; Andersen, Henrik Sune; Kampen, Gita Camilla Tejlgaard; Ebdrup, Soren; US2009/118259; (2009); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

A common heterocyclic compound, the Thiomorpholine compound, name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid,cas is 114525-81-4, mainly used in chemical industry, its synthesis route is as follows.

To a 25mL round bottom flask, Intermediate 7 (540 mg, 1.45 mmol), Intermediate 9 (359 mg, 1.45 mmol), EDCI (418 mg, 2.18 mmol), HOBt (294 mg, 2.18 mmol), DIEA (374 mg, 2.9 mmol) and tetrahydrofuran (9 mL) were added, and stirred at room temperature overnight. Thereafter, the reaction product was subjected to vacuum distillation for removal of solvent, dissolved with water, and extracted 3 times with ethyl acetate. The extracts were combined, washed 3 times with saturated brine, concentrated, and separated through a silica gel column (eluent: petroleum ether/ethyl acetate), to give 688 mg of a white foamy solid product, yield 78.8%. [0081] 1H-NMR (400 MHz, CDCl3) delta ppm: 7.42 (1H, d, J = 1.12 Hz), 7.27 (2H, m), 5.75 (1H, s), 5.19 (1H, s), 4.58 (2H, s), 3.95-3.44(10H, brm), 3.12 (1H, m), 2.82 (2H, m), 2.43 (2H, m), 1.92 (9H, s); EI-MS (m/z): 601.1 [M+H]+., 114525-81-4

As the rapid development of chemical substances, we look forward to future research findings about 114525-81-4

Reference£º
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; Peking University; LI, Song; WANG, Ying; XIAO, Junhai; MA, Dalong; GONG, Hongwei; QI, Hui; WANG, Lili; LING, Xiaomei; ZHENG, Zhibing; ZHANG, Yang; ZHONG, Wu; LI, Meina; XIE, Yunde; XU, Enquan; LI, Xingzhou; MA, Jing; ZHAO, Guoming; ZHOU, Xinbo; WANG, Xiaokui; LIU, Hongying; EP2805947; (2014); 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.,39093-93-1

1,3-dibromobenzene (1.6g, 6.81mmol),thiomorpholine dioxide (300mg, 2.22mmol) BINAP (300mg, 0.48mmol), cesium carbonate (2.5g, 23.67mmol) and palladiumacetate (150mg) were dissolved in 10mL dry toluene in a 50mL single-neck flask. The reaction solution washeated to 90¡ãC under argon atmosphere and stirred for 18 hours. After completion of the reaction, the reaction solutionwas filtered, the filtrate was evaporated to dryness under reduced pressure, and the residue was purified by columnchromatography to give 90mg product, which was directly used in the next step.

39093-93-1 is used more and more widely, we look forward to future research findings about Thiomorpholine 1,1-dioxide

Reference£º
Patent; Shanghai Pharmaceuticals Holding Co., Ltd.; XIA, Guangxin; LI, Di; ZUO, Hongjian; WU, Guangsheng; DUAN, Lingjun; ZHANG, Jing; MAO, Yu; LIU, Yanjun; (152 pag.)EP3424928; (2019); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

N-Boc-2-thiomorpholinecarboxylic Acid, cas is 134676-67-8, it is a common heterocyclic compound, the Thiomorpholine compound, its synthesis route is as follows.,134676-67-8

To a solution of 4-(tert-butoxycarbonyl)thiomorpholine-2-carboxylic acid (0.8 g, 3.24 mmol) in anhydrous THF (20 mL) was added slowly at 0 C. BH3 solution (1 M in THF, 13.2 mL). The reaction mixture was stirred at RT overnight then quenched with saturated NaHCO3 (50 mL). The aqueous layer was extracted with EtOAc (2¡Á50 mL). The combined organic layers were washed with brine and dried (MgSO4), filtered and concentrated in vacuo to afford tert-butyl 2-(hydroxymethyl)thiomorpholine-4-carboxylate (0.75 g, crude) as colorless oil, which was used without further purification.

134676-67-8 is used more and more widely, we look forward to future research findings about N-Boc-2-thiomorpholinecarboxylic Acid

Reference£º
Patent; GENENTECH, INC.; Rudolph, Joachim; Gazzard, Lewis J.; Crawford, James J.; Ndubaku, Chudi; Drobnick, Joy; Lee, Wendy; US2015/31674; (2015); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

As a common heterocyclic compound, it belongs to Thiomorpholine compound, name is Thiomorpholine 1,1-dioxide, and cas is 39093-93-1, its synthesis route is as follows.,39093-93-1

A mixture isopropyl 4-((lr,4r)-4-(5-chloropyrazin-2-yloxy)cyclohexyloxy)piperidine-l- carboxylate (50 mg, 0.126 mmol), diacetoxypalladium (2.8 mg, 0.013 mmol), thiomorpholine- 1 ,1-dioxide (17 mg, 0.126 mmol), sodium 2-methylpropan-2-olate (29 mg, 0.302 mmol), and l ,l’-3/4w(di-t-butylphosphino)ferrocene (12 mg, 0.025 mmol) in 1 ,4-dioxane (0.8 mL) was heated at 100 ¡ãC for 1 h under microwave irradiation. LCMS showed product had formed and no starting material remained. Water was added to the reaction mixture and it was extracted with DCM (3 x 15 mL). The organic layer was rinsed with brine, dried with Na2S04 and concentrated to give a brown oil. The brown oil was purified using Biotage.(TM). flash chromatography and a 25 g SNAP.(TM). column, 20-100percent EtOAc-hexanes, 15 column volumes. Fractions containing product were combined and concentrated to give the title compound (25 mg, 0.050 mmol, 40.1 percent yield) as a light brown solid. ‘H NMR (CDCI3 , 400 MHz) delta 1.23 (d, J = 4 Hz, 6H), 1.46-1.55 (m, 6H), 1.77-1.82 (m, 2H), 1.96-2.01 (m, 2H), 2.09-2.14 (m, 2H), 3.06 (t, J = 4Hz , 4H), 3.09-3.16 (m, 2H), 3.48-3.52 (m, 1H), 3.54-3.59 (m, 1H), 3.78-3.84 (m, 2H), 4.06 (t, J = 4Hz , 4H), 4.85-4.94 (m, 2H), 7.73 (s, 1H), 7.82 (s, 1H), LCMS m/z: 497.6 [M+H]+.

With the complex challenges of chemical substances, we look forward to future research findings about 39093-93-1,belong Thiomorpholine compound

Reference£º
Patent; ARENA PHARMACEUTICALS, INC.; JONES, Robert M.; HAN, Sangdon; BUZARD, Daniel J.; LEHMANN, Juerg; NARAYANAN, Sanju; YUE, Dawei; WO2011/127051; (2011); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO161,mainly used in chemical industry, its synthesis route is as follows.,134676-67-8

8.1.6) fe/f-Butyl 2-(hvdroxymethyl)thiomorpholine-4-carboxylate. Thiomorpholine-2,4-dicarboxylic acid 4-te/f-butyl ester (0.20 g, 0.809 mmol) was suspended in THF (15 mL) and cooled to 4C. Then, lithium aluminum hydride (92 mg, 2.43 mmol) was added in small portions. The reaction mixture was allowed to warm up to room temperature overnight. Next day, The reaction was quenched by addition of saturated Na2SO4 solution (2 mL) and EtOAc (22 mL). The reaction mixture was stirred overnight and filtered over dicalite. The filtrate was evaporated till dryness and the crude product was purified by column chromatography (SiO2, heptane/EtOAc; 100% heptane to 40% EtOAc as mobile phase) to give the title compound in 48% yield (91 mg, 0.39 mmol).

With the complex challenges of chemical substances, we look forward to future research findings about N-Boc-2-thiomorpholinecarboxylic Acid,belong Thiomorpholine compound

Reference£º
Patent; N.V. ORGANON; PHARMACOPEIA, LLC; WO2009/124965; (2009); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

(R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, cas is 114525-81-4, it is a common heterocyclic compound, the Thiomorpholine compound, its synthesis route is as follows.,114525-81-4

Referring to Scheme 5-2, a mixture of compound 17 (667 mg, 2.4 mmol), (R)-N-Boc-thiomorpholine-3-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)+.

With the rapid development of chemical substances, we look forward to future research findings about (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid

Reference£º
Patent; PRESIDIO PHARMACEUTICALS, INC.; LI, Leping; ZHONG, Min; WO2011/150243; (2011); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem