Day: August 19, 2020

154127-42-1, (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound B (50.0 g, 140.7 mmol) was added to 450 mL of acetonitrile, trimethyl orthoacetate (27.0 g, 225.1 mmol) and triethylamine (1.4 g, 14.0 mmol) were added with stirring, and the mixture was heated to 78C. , stirring for 5h,HPLC monitoring showed complete reaction and the HPLC monitoring results are shown in Table 1 (see FIG. 1).Cool to 40C, distill off under reduced pressure, and concentrate to a minimum volume.Compound C crude product was obtained.The crude compound C was dissolved in 180 mL of tetrahydrofuran, cooled to -10 DEG C, triethylamine (31.3 g, 309.5 mmol) was slowly added dropwise at a drip rate of 1 d/s, and the addition was completed at a drip rate of 3 d/s. 4- A solution of tosyl chloride (53.5 g, 280.6 mmol) in 70 mL of tetrahydrofuran. After the addition, the temperature was controlled at -4C, and the reaction was complete after about 3 hours.At a controlled temperature of 10 C. or less, a 70% aqueous solution of ethylamine (361.0 g, 5.6 M) was slowly added dropwise at a rate of 5 d/s. After the addition, the temperature was kept stirring at 12C and the reaction was complete after about 15 hours.The mixture was concentrated under reduced pressure to 70-80 mL, and the temperature was lowered to 0C. The temperature was controlled below 30C, and concentrated hydrochloric acid (12 mol/L) was added dropwise to adjust the pH to 1 to 2, and then about 14 mL of concentrated hydrochloric acid (12 mol/L) was added. The mixture was stirred at room temperature for 1 hour. The reaction was extracted twice with methyl tert-butyl ether (2*250 mL). The organic phases were combined and extracted once with dilute hydrochloric acid (1 mol/L, 100 mL). Combine the aqueous phases, slowly add sodium bicarbonate solids, adjust the pH to 5-6, add 150 mL of water, and adjust the pH to 7-8 with 7% sodium bicarbonate solution. After adjustment, stir at room temperature for 15 h and slowly crystallize. After filtration, the filter cake was rinsed with 30 mL of water and the cake was dried to obtain 35.4 g of product with a purity of 98.3%.Add 250 mL of dichloromethane, 25 mL of methanol to the filter mother liquor, stir, extract, separate, and concentrate the organic phase to dryness4.6 g of yellow viscous material was added and 10 mL of ethyl acetate was added. Heat to 70 ~ 75 C dissolved, slowly dropped to 0 ~ 10 C, stirring 1 ~ 2h, precipitation of a white solid, continue stirring 3 ~ 4h, filtration, with 3mL water filter cake, filter cake drying,Obtained product 2.4g, purity 97.3%.Combined, the purity was 98.1%, the total yield was 65.3%, the ignition residue was 0.08%, and the chiral purity was 99.7%.

154127-42-1 (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide 15225314, athiazines compound, is more and more widely used in various.

Reference£º
Patent; Shandong Weizhi Pharmaceutical Co., Ltd.; Shanghai Weizhi Pharmaceutical Technology Co., Ltd.; Wang Jianhua; He Yigang; Wei Yanjun; Xing Yanping; Zhao Tianchang; (27 pag.)CN107759618; (2018); A;,
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.

In a 250 ml three-necked flask, 0.01 mol of raw material A1, 0.012 mol of raw material B1, 150 ml of toluene were added under a nitrogen atmosphere, and the mixture was stirred and mixed.Then, 0.03 mol of sodium t-butoxide, 5 ¡Á 10 -5 mol of Pd 2 (dba) 3, 5 ¡Á 10 -5 mol of tri-tert-butylphosphine was added, and the mixture was heated to 105 C, and refluxed for 24 hours.The sampling point plate shows that no raw material A1 remains, the reaction is complete; it is naturally cooled to room temperature, filtered, and the filtrate is steamed to a non-fraction (-0.09 MPa, 85 C) under reduced pressure, and passed through a neutral silica gel column to obtain an intermediate B1.HPLC purity 99.2%, yield 75.2%;

The synthetic route of 3939-23-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Jiangsu March Optoelectric Technology Co., Ltd.; Tang Dandan; Zhang Zhaochao; Li Chong; Zhang Xiaoqing; (44 pag.)CN108218853; (2018); A;,
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.92-30-8,2-(Trifluoromethyl)-10H-phenothiazine,as a common compound, the synthetic route is as follows.

Step a 4-(3′-indolyl)-1-[1″-(2′”-trifluoromethyl-10′”-phenothiazinyl)-2″-methyl-3″-propionyl]-piperidine hydrochloride 27 g of 2-trifluoromethyl-phenothiazine and 12 g of alpha-methylacryloyl chloride in 100 ml of toluene were 1 for 2 hours and the mixture was evaporated to dryness. The residue was chromatographed over silica gel and elution with a 1– 1 benzene-cyclohexane mixture gave 18 g of 2-trifluoromethyl-10-(alpha-methyl acryloyl)-phenothiazine in the form of white crystals melting at 103¡ãC.

The synthetic route of 92-30-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Roussel-UCLAF; US3988453; (1976); A;,
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.92-30-8,2-(Trifluoromethyl)-10H-phenothiazine,as a common compound, the synthetic route is as follows.

Compound 27; 10-[2-(N-Boc-4-piperidyl)ethyl]-2-trifluoromethylphenothiazine; To a stirred solution of 2-trifluoromethylphenothizine 1 (0.9 Ig, 3.42 mmol), sodium hydride (0.2g, 4.0 mmol) in DME (20 mL) at 90¡ãC was added N-Boc- 4-(2-bromoethyl)piperidine 26 (1.Og, 3.42 mmol) dropwise under an atmosphere of argon. The reaction mixture was stirred for 12h at reflux temperature. The reaction mixture was filtered, and filtrate was concentrated under vacuum. The residue was partitioned between ethyl acetate (25 mL) and brine (1OmL). The organic layer was dried over anhydrous sodium sulphate, filtered, and evaporated. The resulting residue was purified by column chromatography (8:2 n-hexane : ethyl acetate) on silica gel to give phenothiazine derivative 27 (0.3 g, 18percent) as a foam. MS(ESI): m/z 479(M+H).

The synthetic route of 92-30-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IMMUNE CONTROL, INC.; WO2008/27521; (2008); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

3080-99-7, 3,4-Dihydro-2H-benzo[b][1,4]thiazine is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(3d) Potassium carbonate (5.2 g, 37.7 mmol) and methyl 4-(bromomethyl)benzoate (2.8 g, 12.6 mmol) were added to a solution of (3c) (1.9 g, 12.6 mmol) in 20 mL of anhydrous DMF. The reaction mixture was heated to 80 C. overnight. After cooling to rt, the solid was filtered off and rinsed with DMF. The filtrate was concentrated in vacuo and the residue was purified on silica gel column to provide methyl 4-(2,3-dihydro-4H-1,4-benzothiazin-4-ylmethyl)benzoate (3.02 g, 80%).

As the paragraph descriping shows that 3080-99-7 is playing an increasingly important role.

Reference£º
Patent; Duan, Jingwu; Jiang, Bin; Chen, Lihua; Lu, Zhonghui; Barbosa, Joseph; Pitts, William J.; US2003/229084; (2003); 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.

Intermediate 524-Fluoro- 2-(l,l-dioxo-llambda6-[l,2]thiazinan-2-yl)benzonitrile: To a solution of l,l-dioxo[l,2]thiazinane (8.84 g, 65.4 mmol) in DMF (20 mL) and THF (10 mL) was added portion-wise sodium hydride (1.65 g, 65.5 mmol, 95%). After stirring for 30 min, 2,4-difluorobenzonitrile (10.0 g, 72 mmol) was added and the mixture was stirred at 90 C for 2.5 h. The mixture was cooled and concentrated and the residue was purified by flash chromatography eluting with 0%-l 0% EtOAc/hexane to give the title compound as white needles (1.37 g, 8% yield). 1H-NMR (500 MHz, CDCl3) delta: 7.70 (IH, dd, J= 8.8, 5.8 Hz), 7.30 (IH, dd, J= 8.8, 2.4 Hz), 7.15-7.12 (IH, m), 3.72 (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 C11H12N2FO2S: 255.06; found: 255.19.

37441-50-2 1,2-Thiazinane 1,1-dioxide 303508, athiazines compound, is more and more widely used in various.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2007/58646; (2007); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

92-30-8, 2-(Trifluoromethyl)-10H-phenothiazine is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a mixture of sodium hydride suspension (60percent, 0.26 g, 6.67 mmol) and phenothiazine derivative in abs. THF (50 cm3) was added the appropriate 3-aryltetrazolo[1,5-a]pyridin-4-ium tetrafluoroborate (1) in portions over 20 min, and the mixture was stirred at room temperature for 2 days. After evaporation of the reaction mixture, the residue was dissolved in a 1:1 mixture of EtOAc:water (50 cm3) and the solid product was filtered off. The aqueous mother liquor was extracted with EtOAc (thrice) and the organic phase was dried over anhydrous Na2SO4, filtered and evaporated. The combined organic solvent was evaporated, the residue was washed with diethyl ether then it was recrystallized from ethyl acetate – unless otherwise stated – to give the product.

As the paragraph descriping shows that 92-30-8 is playing an increasingly important role.

Reference£º
Article; Taka?cs, Daniella; Nagy, Ildiko?; Bombicz, Petra; Egyed, Orsolya; Jemnitz, Katalin; Riedl, Zsuzsanna; Molna?r, Jo?zsef; Amaral, Leonard; Hajo?s, Gyo?rgy; Bioorganic and Medicinal Chemistry; vol. 20; 14; (2012); p. 4258 – 4270;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

92-30-8, 2-(Trifluoromethyl)-10H-phenothiazine is a thiazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a stirred solution of phenothiazine or 2-(trifluoromethyl)-10H-phenothiazine (3 mmol) in dichloromethane (20 mL), K2CO3 (5 mmol) and propargyl bromide (5 mmol) were added carefully and the reaction mixture was refluxed for 7 h. After the reaction, the system was concentrated under vacuum, the residue was dissolved in EtOAc (40 mL) and washed by pure water and brine, and dried over anhydrous Na2SO4 and concentrated under vacuum to afford crude products 8a-8b, which were used in the next reaction without further purification.

The synthetic route of 92-30-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Zhang, Jun-Xia; Guo, Jiao-Mei; Zhang, Ting-Ting; Lin, Hong-Jun; Qi, Nai-Song; Li, Zhen-Guo; Zhou, Ji-Chun; Zhang, Zhen-Zhong; Molecules; vol. 23; 6; (2018);,
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.92-30-8,2-(Trifluoromethyl)-10H-phenothiazine,as a common compound, the synthetic route is as follows.

To a mixture of 2-(trifluoromethyl)-l0i7-phenothiazine (5.0 g, 18.726 mmol) and NaH (0.674 g, 28.09 mmol) in DMF (50 mL) was added 2-(bromomethyl)oxirane (3.8 g, 28.09 mmol) at 0 C. The mixture was allowed to slowly warm to rt and was stirred at room temperature overnight. Then the mixture was added to water (100 mL) and extracted with EtOAc (100 mL x 3). The combined organic layers were washed with brine (30 mL), dried over sodium sulfate, and concentrated to dryness. The residue was purified by column chromatography on silica gel (PE/EtOAc = 8/1) to afford compound 2-1 (4.5 g, 75% yield) as a white solid. ‘H NMR (400 MHz, Patent; CAMP4 THERAPEUTICS CORPORATION; BUMCROT, David, A.; SEHGAL, Alfica; HERTZOG, Donald L.; (172 pag.)WO2019/195789; (2019); 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.38642-74-9,2-Cyano-phenothiazine,as a common compound, the synthetic route is as follows.

2-cyanophenothiazine (0.74 g, 3.30 mmol) was dissolved in 10 mL of anhydrous DMF. The mixture was cooled to 0 C and 60 % NaH (0.40 g, 9.90 mmol) was added. The dark mixture was stirred at 0 C for an additional 15 mm and Di-tert-butyl dicarbonate (0.90 g, 3.96 mmol) was added. The mixture was stirred at room temperature for 3 h and was diluted with 50 mL of brine. The aqueous layer was extracted with three 25 mL portions of ethyl acetate. The combined organic extract was dried over anhydrous MgSO4 and concentrated under diminished pressure. The crude was purified on a silica gel column (10 cm x 2 cm). Elution with ethyl acetate-hexane (1:9) gave 1 as a pale yellow solid: yield 1.07 g (100%); silica gel TLC R10.26 (ethyl acetate-hexane 1:9); ?HNIVIR (CDC13) 51.49 (s, 9H), 7.16-7.20 (m, 1H), 7.28-7.33 (m, 2H), 7.40 (s, 2H), 7.49 (d, 1H, J= 8.4 Hz) and 7.80 (s, 1H); ?3CI?IvIR 28.1, 83.1, 110.2, 118.2, 126.6, 127.2, 127.3, 127.5, 128.1,129.1, 130.3, 130.6, 137.7, 139.0, 139.1 and 151.8; mass spectrum (APCI), m/z 325.1017 (M+H) (C18H17N202S requires m/z 325.1011).

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

Reference£º
Patent; ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY; HECHT, Sidney; KHDOUR, Omar; CHOWDHURY, Sandipan, Roy; BANDYOPADHAY, Indrajit; (85 pag.)WO2016/133995; (2016); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem