Tag: 272437-84-0

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.272437-84-0,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid,as a common compound, the synthetic route is as follows.

Preparation of 4-[(3-oxo-3,4-dihydro-2H-benzo[l ,41thiazine-6-carbonyl)-aminol-piperidine- 1-carboxylic acid tert-butyl ester:3-Oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (556 mg, 2.45 mmol, 1.0 eq) is added at room temperature to a stirred solution of 4-amino-piperidine- 1-carboxylic acid tert- butyl ester (500 mg, 2.45 mmol, 1.0 eq) in N,N-dimethylformamide (20 mL), followed by 1- hydroxybenzotriazole (421 mg, 2.69 mmol, 1.1 eq), N-(3-dimethylaminopropyl)-N’- ethylcarbodiimide hydrochloride (550 mg, 2.81 mmol, 1.15 eq) and N,N- diisopropylethylamine (962 L, 5.50 mmol, 2.25 eq). After 15 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3 x 30 – – mL) and water (30 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to give a crude product that is purified by column chromatography (silica gel, eluent: cyclohexane:ethyl acetate :methanol, 1 :3:0 to 0/9/1, v/v/v) to afford 4-[(3-oxo-3,4- dihydro-2H-benzo [ 1 ,4]thiazine-6-carbonyl)-amino ] -piperidine- 1 -carboxylic acid tert-butyl ester as a light yellow solid (621 mg, 62% yield).1H-NMR (400 MHz, DMSO- 6) delta ppm: 10.66 (s, 1H), 8.27 (d, J = 7.8 Hz, 1H), 7.42 (m, 3H), 3.96 (m, 3H), 3.51 (s, 2H), 2.90 (m, 2H), 1.76 (m, 2H), 1.40 (m, 11H).MS m/z (+ESI): 392.3 [M+H]+, 414.3 [M+Na]+.

As the paragraph descriping shows that 272437-84-0 is playing an increasingly important role.

Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck Hubert; XIE, Tong; XU, Lin; WO2012/171860; (2012); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.272437-84-0,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid,as a common compound, the synthetic route is as follows.

Preparation of ?ralpha^5-4-r(3-oxo-3,4-dihvdro-2H-benzori,41thiazine-6-carbonyl)-aminol- cvclohexanecarboxylic acid methyl ester: 3-Oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (116 mg, 0.50 mmol, 1.0 eq) is added at room temperature to a stirred solution of tralphar¡ã-4-amino-cyclohexanecarboxylic acid methyl ester (80 mg, 0.50 mmol, 1.0 eq) in 7V,N-dimethylformamide (4 mL), followed by 1-hydroxybenzotriazole (74 mg, 0.55 mmol, 1.1 eq), 7V-(3-dimethylaminopropyl)-N’- ethylcarbodiimide hydrochloride (107 mg, 0.56 mmol, 1.15 eq) and N1N- diisopropylethylamine (192 muL, 1.12 mmol, 2.25 eq). After 15 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3 x 10 mL) and water (10 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to afford tralphar¡ã-4-[(3-oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carbonyl)- amino] -cyclohexanecarboxylic acid methyl ester as an off-white solid (127 mg, 66% yield).MS m/z (+ESI): 349.2 [M+Eta]”

As the paragraph descriping shows that 272437-84-0 is playing an increasingly important role.

Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck Hubert; ROUSSEL, Patrick; WO2010/84152; (2010); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.272437-84-0,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid,as a common compound, the synthetic route is as follows.

Acid (4a) in tetrahydrofuran (SOmL) and triethylamine (4.7mL) was cooled to 0C and isobutylchloroformate (4.02mL) was added dropwise and the solution was stirred at 0C for 2 hours, when it was filtered into a stirred solution of sodium borohydride (3. 14g) in ice/water (50mL). The mixture was stirred at 0C for 1 hour and allowed to warm to room temperature. It was acidified with 2M hydrochloric acid, evaporated to half volume, and the resulting product was collected, washed with water and dried in vacuo, to give a white solid (4. 5g). MS (-ve ion electrospray) m/z 194 (M-H)-

272437-84-0 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid 760993, athiazines compound, is more and more widely used in various.

Reference£º
Patent; SMITHKLINE BEECHAM P.L.C.; WO2003/87098; (2003); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

272437-84-0, 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The acid (a) in tetrahydrofuran (50 ml) and triethylamine (4.7 ml) was cooled to [0C] and [ISOBUTYLCHLOROFORMATE] (4.02 ml) was added dropwise and the solution was stirred at [0C] for 2 hours, when it was filtered into a stirred solution of sodium borohydride (3.14 g) in ice/water (50 ml). The mixture was stirred at [0C] for 1 hour and allowed to warm to room temperature. It was acidified with 2M hydrochloric acid, evaporated to half volume, and the resulting product was collected, washed with water and dried in vacuo, to give a white solid (4.5 g). MS (-ve ion electrospray) [M/Z] 194 (M-H)-

The synthetic route of 272437-84-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/2992; (2004); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

272437-84-0, 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (31 mg, 0.14 mmol, 1.0 eq) is added at room temperature to a stirred solution of l-(6-methoxy-3,4-dihydro-2H-l-oxa-9-aza- phenanthrene-3-yl)-piperidin-4-ylamine (50 mg, 0.14 mmol, 1.0 eq) in N,N- dimethylformamide (3 mL), followed by 1-hydroxybenzotriazole (21 mg, 0.15 mmol, 1.1 eq), N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (31 mg, 0.16 mmol, 1.15 eq) and NN-diisopropylethylamine (53 mu, 0.31 mmol, 2.25 eq). After 15 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3 x 10 mL) and water (10 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to give a crude product that is purified by preparative HPLC to afford 3-oxo-3,4- dihydro-2H-benzo[ 1 ,4]thiazine-6-carboxylic acid [ 1 -(6-methoxy-3 ,4-dihydro-2H- 1 -oxa-9- aza-phenanthrene-3-yl)-piperidin-4-yl] -amide as an off-white lyophilizated powder (24 mg, 33% yield). 1H-NMR (400 MHz, DMSO-dtf) delta ppm: 10.66 (br, 1H), 8.33 (s, 1H), 8.24 (d, J = 7.6 Hz, 1H), 7.81 (d, J = 9.0 Hz, 1H), 7.42 (m, 2H), 7.38 (m, 1H), 7.20 (m, 2H), 4.47 (d, J = 11.0 Hz, 1H), 4.02 (m, 1H), 3.93 (s, 3H), 3.78 (m, 1H), 3.50 (s, 2H), 3.20 (m, 1H), 3.08 (m, 2H), 3.00 (m, 2H), 2.42 (m, 2H), 1.81 (m, 2H), 1.58 (m, 2H).MS m/z (+ESI): 505.2 [M+H]+.

272437-84-0 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid 760993, athiazines compound, is more and more widely used in various.

Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck, Hubert; TANG, XiaoHu; XIE, Tong; XU, Lin; WO2011/73378; (2011); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

272437-84-0, 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of 3-oxo-3,4-dihydro-2H-benzo[l,41thiazine-6-carboxylic acid [tra/? -4-(8- methoxy-l,2-dihydro-3-oxa-5,9-diaza-cyclopenta[alnaphthalen-2-ylmethyl)-cyclohexyll- amide:3-Oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (31 mg, 0.14 mmol, 1.0 eq) is added at room temperature to a stirred solution of tra?s-4-(8-methoxy-l,2-dihydro-3-oxa-5,9- diaza-cyclopenta[a]naphthalen-2-ylmethyl)-cyclohexylamine (47 mg, 0.14 mmol, 1.0 eq) in N,N-dimethylformamide (4 mL), followed by 1-hydroxybenzotriazole (24 mg, 0.16 mmol, 1.1 eq), N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (32 mg, 0.16 mmol, 1.15 eq) and NN-diisopropylethylamine (56 mu, 0.32 mmol, 2.25 eq). After 15 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3 x 10 mL) and water (10 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to give a crude product that is purified by preparative HPLC to afford 3-oxo-3,4- dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid [tra?s-4-(8-methoxy-l,2-dihydro-3-oxa- – -5,9-diaza-cyclopenta[a]naphthalen-2-ylmethyl)-cyclohexyl]-amide as a white lyophilized powder (16 mg, 21% yield).1H-NMR (400 MHz, DMSO- 6) delta ppm: 10.67 (s, 1H), 8.49 (s, 1H), 8.23 (d, J = 7.9 Hz, 1H), 8.19 (d, J = 9.0 Hz, 1H), 7.44 (m, 3H), 7.06 (d, J = 9.1 Hz, 1H), 5.21 (m, 1H), 4.01 (s, 3H), 3.74 (m, 2H), 3.51 (s, 2H), 3.14 (dd, J = 7.9, 16.8 Hz, 1H), 1.80-2.00 (m, 5H), 1.66 (m, 1H), 1.57 (m, 1H), 1.39 (m, 2H), 1.13 (m, 2H).MS m/z (+ESI): 505.5 [M+H]+.

The synthetic route of 272437-84-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck Hubert; XIE, Tong; XU, Lin; WO2012/171860; (2012); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

272437-84-0, 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of (3-oxo-3,4-dihvdro-2H-benzori,41thiazine-6-carboxylic acid {trans-4-2-(6- methoxy-ri,51naphthyridin-3-yloxy)-ethyll-cvclohexyU)-amide: 3-Oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (59 mg, 0.25 mmol, 1.0 eq) is added at room temperature to a stirred solution of tralphar¡ã-4-[2-(6-methoxy- [l,5]naphthyridin-3-yloxy)-ethyl]-cyclohexylamine (80 mg, 0.25 mmol, 1.0 eq) inN,N- dimethylformamide (5 mL), followed by 1-hydroxybenzotriazole (37 mg, 0.28 mmol, 1.1 eq), N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (56 mg, 0.29 mmol, 1.15 eq) and 7V,N-diisopropylethylamine (97 muL, 0.57 mmol, 2.25 eq). After 15 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3 x 10 mL) and water (10 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to give a crude product that is purified by preparative EtaPLC to afford (3-oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid {trans-4-[2-(6- methoxy-[l,5]naphthyridin-3-yloxy)-ethyl]-cyclohexyl})-amide as a white lyophilizated powder (36 mg, 27% yield). 1H-NMR (400 MHz, DMSO-t/6) delta ppm: 10.64 (s, IH), 8.53 (d, J = 2.8 Hz, IH), 8.19 (dd, J = 0.7, 9.0 Hz, 2H), 7.62 (dd, J = 0.5, 2.5 Hz, IH), 7.37-7.46 (m, 3H), 7.07 (d, J = 9.0 Hz, IH), 4.24 (t, J = 6.6 Hz, 2H), 4.00 (s, 3H), 3.70-3.80 (m, IH), 3.50 (s, 2H), 1.80-1.90 (m, 4H), 1.70-1.80 (m, 2H), 1.45-1.55 (m, IH), 1.30-1.40 (m, 2H), 1.05-1.18 (m, 2H). MS m/z (+ESI): 493.4 [M+H]+.

As the paragraph descriping shows that 272437-84-0 is playing an increasingly important role.

Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck Hubert; ROUSSEL, Patrick; WO2010/84152; (2010); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.272437-84-0,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid,as a common compound, the synthetic route is as follows.

Preparation of 3-oxo-3,4-dihvdro-2H-benzori,41thiazine-6-carboxylic acid (l-[2-(6- methoxy-quinolin-3-ylsulfanyl)-ethyll-piperidin-4-vU -amide: 3-oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (21 mg, 0.09 mmol, 1.0 eq) is added at room temperature to a stirred solution of l-[2-(6-methoxy-quinolin-3-ylsulfanyl)- ethyl]-piperidin-4-ylamine (30 mg, 0.09 mmol, 1.0 eq) in N,N-dimethylformamide (3 mL), followed by 1-hydroxybenzotriazole (13 mg, 0.10 mmol, 1.1 eq), N-Q- dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (20 mg, 0.10 mmol, 1.15 eq) and N,N-diisopropylethylamine (35 muL, 0.20 mmol, 2.25 eq). After 15 hours stirring at room temperature, solvent is evaporated and the residue is extracted with dichloromethane (3 x 5 mL) and water (5 mL). The combined organic layers are dried over sodium sulfate, filtered and concentrated to give a residue that is purified by preparative EtaPLC to afford 3-oxo-3,4- dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid {l-[2-(6-methoxy-quinolin-3- ylsulfanyl)-ethyl]-piperidin-4-yl} -amide as a white solid (30 mg, 59% yield).1H-NMR (400 MHz, DMSO-t/6) delta ppm: 11.65 (s, IH), 8.65 (d, J = 2.5 Hz, IH), 8.20-8.25 (m, 2H), 7.88 (d, J = 8.8 Hz, IH), 7.30-7.45 (m, 5H), 3.93 (s, 3H), 3.75 (m, IH), 3.50 (s, 2H), 3.29 (t, J = 7.0 Hz, 2H), 2.95 (m, 2H), 2.66 (t, J = 7.0 Hz, 2H), 2.11 (m, 2H), 1.78 (m, 2H), 1.58 (m, 2H). MS m/z (+ESI): 509.3 [M+H]+.

272437-84-0 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid 760993, athiazines compound, is more and more widely used in various.

Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck Hubert; ROUSSEL, Patrick; WO2010/84152; (2010); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem