Month: September 2020

A common heterocyclic compound, 272437-84-0,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route. 272437-84-0

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]”, 272437-84-0

This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid,272437-84-0,its application will become more common.

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

A common heterocyclic compound, 92-30-8,2-(Trifluoromethyl)-10H-phenothiazine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route. 92-30-8

Compound 21; 10-(4-chlorobutyl)-2-trifluoromethylphenothiazine; To a stirred solution of 2-trifluoromethylphenothiazine 1 (4.Og, 15 mmol), sodium hydride (1.2g, 24 mmol) in dry toluene (40 mL), 1-bromo 4- chlorobutane (3.0 g, 17.6 mmol) was added. The reaction mixture was stirred for 18 hours at 110 C under an atmosphere of argon. The solution was cooled to room temperature and poured into an ice-water mixture. The crude product was extracted with ethyl acetate (3chi50mL) and the organic phase was dried over sodium sulphate. Final purification was performed by column chromatography (9: 1 hexane: ethyl acetate) on silica gel to give 21 (3.5 g, 65% ) as an oil.

This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,92-30-8,2-(Trifluoromethyl)-10H-phenothiazine,its application will become more common.

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

A common heterocyclic compound, 37441-50-2,1,2-Thiazinane 1,1-dioxide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route. 37441-50-2

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., 37441-50-2

This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,1,2-Thiazinane 1,1-dioxide,37441-50-2,its application will become more common.

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.92-30-8,2-(Trifluoromethyl)-10H-phenothiazine,as a common compound, the synthetic route is as follows.,92-30-8

Compound 13; 10-[3-(N-Boc-4-piperidyl)propyl]-2-trifluoromethylphenothiazine; To a stirred solution of 2-trifluoromethylphenothizine 1 (400 mg, 1.5 mmol), sodium hydride (100 mg, 2 mmol) in DME (10 mL) at 90 C was added N- Boc-4-(3-bromopropyl)piperidine 12 (380 mg, 1.24 mmol) dropwise under an atmosphere of argon. The reaction mixture was stirred for 12h at reflux. The reaction mixture was filtered and the 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 silica gel column chromatography (8:2 hexane : ethyl acetate) on silica gel to give phenothiazine derivative 13 (425 mg, 70percent) as a solid. MS(ESI): m/z493 (M+H).

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

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

A common heterocyclic compound, 38642-74-9,2-Cyano-phenothiazine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route. 38642-74-9

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)., 38642-74-9

This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,2-Cyano-phenothiazine,38642-74-9,its application will become more common.

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

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

General procedure: Formyl chloride derivatives (7 mmol) was added to the solution ofvarious arylamines (7 mmol) in acetone (25 ml). After stirring at 60 Cfor 6 h, the reaction mixture was concentrated to remove acetone. Theresidue was purified by column chromatography with petroleum/ethylacetate (9:1) to afford the target compound 15-27 and 29-32.

92-30-8 2-(Trifluoromethyl)-10H-phenothiazine 7082, athiazines compound, is more and more widely used in various fields.

Reference£º
Article; Fu, Dong-Jun; Li, Miaomiao; Zhang, Sai-Yang; Li, Jiang-Feng; Sha, Beibei; Wang, Longhao; Zhang, Yan-Bing; Chen, Ping; Hu, Tao; Bioorganic Chemistry; vol. 92; (2019);,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

A common heterocyclic compound, 37441-50-2,1,2-Thiazinane 1,1-dioxide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route. 37441-50-2

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., 37441-50-2

This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,37441-50-2,1,2-Thiazinane 1,1-dioxide,its application will become more common.

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

2-(Trifluoromethyl)-10H-phenothiazine, cas is 92-30-8, it is a common heterocyclic compound, the thiazines compound, its synthesis route is as follows.,92-30-8

Compound 13; 10-[3-(N-Boc-4-piperidyl)propyl]-2-trifluoromethylphenothiazine; To a stirred solution of 2-trifluoromethylphenothizine 1 (400 mg, 1.5 mmol), sodium hydride (100 mg, 2 mmol) in DME (10 mL) at 90 C was added N- Boc-4-(3-bromopropyl)piperidine 12 (380 mg, 1.24 mmol) dropwise under an atmosphere of argon. The reaction mixture was stirred for 12h at reflux. The reaction mixture was filtered and the 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 silica gel column chromatography (8:2 hexane : ethyl acetate) on silica gel to give phenothiazine derivative 13 (425 mg, 70percent) as a solid. MS(ESI): m/z493 (M+H).

As the rapid development of chemical substances, we look forward to future research findings about 92-30-8

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

3939-23-9 A common heterocyclic compound, 3939-23-9,3-Bromo-10H-phenothiazine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

In a nitrogen-flushed 250 mL round-bottom flask with a magnetic stir bar and septum 3-bromo-10H-phenothiazine (4.95 g, 17.8 mmol) was dissolved in dry THF (50 mL) under nitrogen. The colorless solution was deaerated by a constant stream of nitrogen through a syringe for 10 min and cooled to 0 C (ice bath/water). Potassium tert-butanolate (2.40 g, 21.4 mmol) was added to the reaction mixture under nitrogen and the reaction mixture was allowed to come to room temperature and then stirred for 1 h. To this solution 1-bromo hexane (3.00 mL, 21.4 mmol) was slowly added by syringe and stirring at room temp was continued for 16 h. The solvents were removed in vacuo and the residue was adsorbed onto celiteand purified by chromatography on silica gel (n-hexane) to give 5.83 g (90%) of 3-bromo-10-hexyl-10H-phenothiazine (1a) as a yellow resin, Rf (n-hexane) = 0.43. The NMR spectra were in excellent agreement with the literature. 1H NMR (300 MHz, acetone-d6): delta = 0.84 (t, 3J = 7.1 Hz, 3 H), 1.23-1.33 (m, 4 H), 1.44 (dt, 3J = 7.2 Hz, 3J = 6.8 Hz, 2 H), 1.77 (dt, 3J = 7.5 Hz, 3J = 7.5 Hz, 2 H), 3.92 (t, 3J = 7.0 Hz, 2 H), 6.95 (d, 3J = 8.7 Hz, 2 H), 7.03 (dd, 3J = 8.2 Hz, 4J = 0.9 Hz, 1 H), 7.14 (dd, 3J = 7.6 Hz, 4J = 1.4 Hz, 1 H), 7.21 (ddd, 3J = 8.2 Hz, 3J = 7.3 Hz, 4J = 1.6 Hz, 1 H), 7.27 (d, 4J = 2.2 Hz, 1 H), 7.32 (dd, 3J = 8.6 Hz, 4J = 2.3 Hz, 1 H). -13C NMR (75 MHz, acetone-d6): delta = 14.2 (CH3), 23.2 (CH2), 27.0 (CH2), 27.4 (CH2), 32.1 (CH2), 47.9 (CH2), 114.7 (Cquat), 116.9 (CH), 118.1 (CH), 123.6 (CH), 124.7 (Cquat), 128.1 (Cquat), 128.1 (CH), 128.6 (CH), 130.0 (CH), 130.9 (CH), 145.7 (Cquat), 145.9 (Cquat).

This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,3939-23-9,3-Bromo-10H-phenothiazine,its application will become more common.

Reference£º
Article; Urselmann, Dominik; Deilhof, Konstantin; Mayer, Bernhard; Mueller, Thomas J. J.; Beilstein Journal of Organic Chemistry; vol. 12; (2016); p. 2055 – 2064;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

Name is 2-(Trifluoromethyl)-10H-phenothiazine, as a common heterocyclic compound, it belongs to thiazines compound, and cas is 92-30-8, its synthesis route is as follows.,92-30-8

To a solution of 2-(trifluoromethyl)-10H-phenothiazine (5.0g, 18.8mmol) and DMF (15mL) at RT was added finely powdered KOH (2.1g, 37.5mmol) and (¡À)-epibromohydrin (3.9mL, 48.9mmol). The reaction mixture was stirred at RT for 48h. Once no starting material was observed by analytical LCMS, EtOAC (250mL) and brine (250mL) were added. The organic layer was separated, and the aqueous layer was washed with EtOAC (3 chi lOOmL). The combined organic extracts were washed with brine (2 chi lOOmL), dried over MgSOzi, and concentrated to afford the title compound

With the complex challenges of chemical substances, we look forward to future research findings about 2-(Trifluoromethyl)-10H-phenothiazine

Reference£º
Patent; INCEPTION 1, INC.; CHEN, Austin, Chih-Yu; SCOTT, Jill, Melissa; STEARNS, Brian, Andrew; STOCK, Nicholas, Simon; TRUONG, Yen, Pham; WO2013/43744; (2013); A2;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem