Month: August 2020

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3939-23-9,3-Bromo-10H-phenothiazine,as a common compound, the synthetic route is as follows.

2, under nitrogen protection will be prepared in step 1 p-phenylenediamine and phenothiazine derivatives according to 1:1 molar ratio was added to toluene, while adding potassium tert-butyl alcohol and palladium acetate as a catalyst,The reaction was heated to 80 C for 3 hours and then cooled to room temperature. The reaction was filtered,The filtrate was washed with dichloromethane and then the solvent was evaporated to dryness. The crude product was repeatedly washed with methanol and acetone,The product is obtained after purification by column chromatography.

3939-23-9 3-Bromo-10H-phenothiazine 283308, athiazines compound, is more and more widely used in various.

Reference£º
Patent; Changchun Hai Purunsi Technology Co., Ltd.; Guo Jianhua; (12 pag.)CN106831645; (2017); A;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

37441-50-2, 1,2-Thiazinane 1,1-dioxide is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of 2,4-difluorobenzonitrile (10.0 g, 72 mmol) and 1,1-dioxo-1?6-[1,2]thiazin-2-ane (8.84 g, 65.4 mmol) in 1:1 tetrahydrofuran/dimethylformamide (40 mL) was added potassium carbonate (9.0 g, 65.4 mmol). The mixture was stirred at 90 C. for 18 h then filtered and concentrated. The residue was purified by flash chromatography (SiO2) eluting with 10%-50% ethyl acetate/hexanes followed by recrystallization from hot ethyl acetate/hexane to give the title compound as white needles (0.537 g, 3% yield). 1H NMR (500 MHz, CD3OD) ? ppm: 7.70 (1H, dd, J=8.8, 5.8 Hz), 7.30 (1H, dd, J=8.8, 2.4 Hz), 7.15-7.12 (1H, m), 3.27 (2H, t, J=5.3 Hz), 3.33 (2H, t, J=6.1 Hz), 2.40-2.35 (2H, m), 2.05-2.01 (2H, m). LCMS (M+H) calcd for C11H16N2OF: 255.06; found: 255.19.

As the paragraph descriping shows that 37441-50-2 is playing an increasingly important role.

Reference£º
Patent; Naidu, B. Narasimhulu; Banville, Jacques; Beaulieu, Francis; Connolly, Timothy P.; Krystal, Mark R.; Matiskella, John D.; Ouellet, Carl; Plamondon, Serge; Remillard, Roger; Sorenson, Margaret E.; Ueda, Yasutsugu; Walker, Michael A.; US2005/267105; (2005); 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.3080-99-7,3,4-Dihydro-2H-benzo[b][1,4]thiazine,as a common compound, the synthetic route is as follows.

To a round bottom flask charged with compound 16-1 (151 mg, 1.0 mmol) and methyl 4-(bromomethyl)benzoate (228 mg, 1.0 mmol) in DMF (5 mL) was added K2CO3 (276 mg, 2.0 mmol). The resulting mixture was allowed to stir for 2 h at 80 C. The mixture was cooled to room temperature and after addition of water (15 mL) extracted with EtOAc (3 x 15 mL). The combined organic extracts were washed with brine (20 mL), dried over sodium sulfate, and concentrated under vacuum. The crude product was purified by flash chromatography (0 – 50% EtOAc/hexanes) to afford as colorless oil (110 mg, 37%).1H NMR (CDCI3) delta 8.00, 7.33 (AlphaAlpha’ChiChi’ multiplet, AX + J AX = 8.4 Hz, 4H), 7.08 (dd, / = 7.7 Hz, 1.5 Hz, 1H), 6.90 (incompletely resolved ddd approaching dt, average of two larger / = 7.8 Hz, additional / = 1.1 Hz, 1H), 6.63 (incompletely resolved ddd approaching dt, average of two larger / = 7.5 Hz, additional / = 0.8 Hz, 1H), 6.54 (dd, 7 = 8.3 Hz, 0.7 Hz, 1H), 4.57 (s, 2H), 3.90 (s, 3H), 3.69, 3.08 (AlphaAlpha’ChiChi’ multiplet, AX + J AX = 10.4 Hz, 4H). 13C NMR (CDCI3) delta 166.9, 143.8, 143.4, 130.1 (2C), 129.1, 128.0, 126.6 (2C), 126.1, 118.0, 117.8, 113.2, 56.3, 52.1, 50.6, 25.9. ESI LRMS: [M+H]+, mlz 300.2.

The synthetic route of 3080-99-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS; KOZIKOWSKI, Alan; SHEN, Sida; BERGMAN, Joel; (100 pag.)WO2017/142883; (2017); 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.37441-50-2,1,2-Thiazinane 1,1-dioxide,as a common compound, the synthetic route is as follows.

6- (1, 1-Dioxo- [1, 2]-thiazinan-2-yl)-3-hydroxy-4-methoxy- pyridine-2-carboxylic acid 4-fluoro-benzylamide compound 62 To a solution of 3-benzyloxy-6-bromo-4-methoxy-pyridine-2- carboxylic acid 4-fluoro-benzylamide (44.5 mg, 0.1 mmol) in toluene (4 ml) were added 1, 4-butanesultam (16.2 mg, 0.12 mmol), cesium carbonate (65 mg, 0.2 mmol), CuI (1.9 mg, 0.01 mmol), 1, 10-phenanthroline (3.6 mg, 0.02 mmol). Under nitrogen, the mixture was stirred at 100’C overnight. After removal of the solvent under reduced pressure, the residue was dissolved into water (10 mL) and extracted with dichloromethane (3 x 10 mL), and the combined organic layers were dried over anhydrous sodium sulfate. Evaporation of the solvent under reduced pressure provided a residue, which was purified on silica gel column eluting with hexane and ethyl acetate (5: 5) to afford a white solid (45 mg). This product (40 mg) was deprotected using hydrogenolysis in methanol to provide the title compound (30 mg).. 1H NMR (400 MHz, CDC13) : 6 [ppm] 12.22 (s, 1H), 7.90 (br s, 1H), 7.30 (m, 2H), 7.07 (m, 3H), 4.58 (d, 2H), 3.92 (m, 5H), 3.13 (m, 2H), 2.30 (m, 2H), 1.89 (m, 2H). LC/MS : m/z 410.2 (M + H+).

As the paragraph descriping shows that 37441-50-2 is playing an increasingly important role.

Reference£º
Patent; VIROCHEM PHARMA INC.; WO2005/42524; (2005); 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.37441-50-2,1,2-Thiazinane 1,1-dioxide,as a common compound, the synthetic route is as follows.

Part E 7-Bromo-2-ethoxymethyl-1-(3-isopropoxypropyl)-1FI imidazo[4,5-c]quinolin-4- amine (0.75 g), 1,4-butanesultam (0.29 g), copper (I) (68 mg), (No.)-trans-1,2- diaminocyclohexane (42 muL), potassium phosphate (0.79 g) and dioxane (4 mL) were added to a scintillation vial. The vial was flushed with nitrogen, sealed with a Teflon- lined cap, placed in an oil bath, and heated at 110 C for 30 hours. The reaction was cooled to ambient temperature, diluted with chloroform and filtered through a bed of CELITE filter agent. The solvent was evaporated and the residue was purified by column chromatography on a Biotage HorizonNo. High-Performance Flash Chromatography instrument using a silica gel cartridge. The polar component of the eluent was chloroform:methanol:ammonium hydroxide 80:18:2 (CMA). The purification was carried out eluting with chloroform: CMA in a gradient from 99: 1 to 90: 10. Additional purification by recrystallization from acetonitrile provided 0.47 g of 7-(1,1-dioxo- [1,2]thiazinan-2-yl)-2-ethoxymethyl-1-(3-isopropoxypropyl)-1H imidazo[4,5-c]quinolin- 4-amine as pale yellow crystals, mp 172-174 C.

As the paragraph descriping shows that 37441-50-2 is playing an increasingly important role.

Reference£º
Patent; 3M INNOVATIVE PROPERTIES COMPANY; WO2005/123080; (2005); A2;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

37441-50-2, 1,2-Thiazinane 1,1-dioxide is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

8-HYDROXY- [1, 6] naphthyridine-7-carboxylic acid methyl ester 1A. 4 (WO 0230930 A2, p. 171) is reacted with one molar equivalent of N-bromosuccinimide in dichloromethane, to yield 5-BROMO-8-HYDROXY- [1, 6] NAPHTLIYRIDINE-7-CARBOXYLIC acid methyl ester, 1A. 5. The phenol is then reacted with p-toluenesulfonyl chloride and triethylamine in CHLOROFONN, FOR example as described in WO 02 30931 A2 p. 72, to give 5-bromo-8- (toluene-4-sulfonyloxy)- [1, 6] naphthyridine-7-carboxylic acid methyl ester 1A. 6. The product is then reacted with [1, 2] thiazinane 1, 1-dioxide 1A. 7 and cuprous oxide in pyridine at reflux, for example as described in WO 0230931 A2, p. 73, to produce 5- (1, 1-DIOXO- 1,2] thiazinan-2-yl)-8- (toluene-4-sulfonyloxy)- [1, 6] naphthyridine-7-carboxylic acid methyl ester 1A. 8. Deprotection, for example by reaction with methanol sodium methoxide in DIMETHYLFORMAMIDE, as described in WO 0230931 A2 p. 74, then affords the phenol 1A. 9.

The synthetic route of 37441-50-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GILEAD SCIENCES, INC.; WO2005/28478; (2005); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

1771-18-2, 2-Methoxyphenothiazine is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step a 4-(3′-indolyl)-1-[1″-(2′”-methoxy-10′”-phenothiazinyl) -2″-methyl-3″-propionyl]-piperidine hydrochloride A mixture of 23 g of 2methoxy-phenothiazine, 21 g of methacryloyl chloride and 120 ml of toluene was refluxed for 3 hours and was then cooled and washed with 250 ml of N sodium hydroxide. The organic phase was decanted and the aqueous phase was washed twice with 50 ml of toluene. The combined organic phases were washed with water, dried over magnesium sulfate, treated with carbon black and evaporated to dryness to obtain 29.6 g of 2-methoxy-10-(alpha-methyl acryloyl)-phenothiazine melting at 91-92 C.

As the paragraph descriping shows that 1771-18-2 is playing an increasingly important role.

Reference£º
Patent; Roussel-UCLAF; US3988453; (1976); A;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

38642-74-9, 2-Cyano-phenothiazine is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In an air atmosphere, 2-phenylindole 1a (0.60 mmol), phenothiazine 2a (0.30 mmol),10mol% cuprous bromide and DMF (2mL) were added to the Schlenk reaction tube in sequence.In a constant temperature heating magnetic stirrer, the reaction was stirred at room temperature for 24 hours.After the reaction was completed, it was quenched with distilled water, extracted with ethyl acetate (3 ¡Á 20 mL), and the organic layers were combined.After drying over anhydrous sodium sulfate and spinning the organic phase, The crude product by column chromatography to give the pure product 3a (103.1 mg, 88%).

As the paragraph descriping shows that 38642-74-9 is playing an increasingly important role.

Reference£º
Patent; Henan Normal University; Zhao Peizheng; Wang Ke; Liu Jianming; Wang Zhixian; Shao Huibin; Yue Yuanyuan; (9 pag.)CN110407830; (2019); A;,
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