Day: October 23, 2020

In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 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, as follows.154127-42-1

Step H: 4(R)-ethylamino-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-l,2- thiazine-6-sulfonamide- 1,1 -dioxide (I); To a solution of IX (41 g, 0.12 moles) and triethylamine (33 ml. 0.24 moles) in anhydrous tetrahydrofuran (615 ml) cooled to 0 to 5 C was added a solution of tosyl chloride (44 g, 0.24 moles) in tetrahydrofuran (205 ml). The mixture was allowed to warm to room temperature and stirred for 18 hours. The reaction mixture was cooled to 0 to 50C and ethylamine gas was purged from its 70% aqueous solution (365 ml) below 10C. Reaction mixture was allowed to attain ambient temperature and stirred for 36 hours. The reaction mixture was concentrated and ethyl acetate (615 ml) was added to it. Further the organic layer was washed with water (410 ml). The concentrated ethyl acetate layer and MDC (615 ml) was added followed by cooling to temperature 0 to 50C and 6M hydrochloric acid (600 ml) was added. The reaction mixture was stirred for 1 h at 15 to 20C. Aqueous layer was washed with MDC (205 ml). pH of the aqueous solution was adjusted to 8 using sodium bicarbonate solution causing white solid to precipitate which was extracted with ethyl acetate (2 x 410 ml). The ethyl acetate layer was evaporated to dryness to yield crude Brinzolamide (29g, 66%). Material was recrystallized from ethanol. [Purity: greater than 99.5%, m.p. 125-1270C], 154127-42-1

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. 154127-42-1, We look forward to the emergence of more reaction modes in the future.

Reference£º
Patent; USV LIMITED; WO2008/62463; (2008); A2;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

37441-50-2,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.

To a mixture of 2,4-difluorobenzonitrile (10.0 g, 72 mmol) and 1,1-dioxo-1lambda6-[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) delta 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.

The chemical industry reduces the impact on the environment during synthesis, 37441-50-2,1,2-Thiazinane 1,1-dioxide,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; Bristol-Myers Squibb Company; US2007/111984; (2007); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 92-30-8,2-(Trifluoromethyl)-10H-phenothiazine, as follows.92-30-8

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%).

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. 2-(Trifluoromethyl)-10H-phenothiazine, We look forward to the emergence of more reaction modes in the future.

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

3080-99-7,A common heterocyclic compound, 3080-99-7,3,4-Dihydro-2H-benzo[b][1,4]thiazine, 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 manner similar to the method described in Example 1-1, using 3,4-dihydro-2H-benzo[1,4]thiazine in place of 1,2,3,4-tetrahydroquinoline, 239 mg (yield: 63%) of the captioned compound was obtained.1H-NMR (ppm) (300 MHz, CDCl3) 6.98 (1H, dd, J = 1.8, 7.9 Hz), 6.86 (1H, ddd, J = 1.8, 7.3, 8.5 Hz), 6.78 (1H, d, J = 8.2 Hz), 6.69-6.65 (2H, m), 6.61-6.5 (1H, ddd, J = 1.2, 7.6, 8.5 Hz), 4.61 (1H, d, J = 8.2 Hz), 3.85 (3H, s), 3.60-3.51 (3H, m), 3.14-2.96 (4H, m), 2.55-2.50 (1H, m), 2.41 (3H, s), 2.38-2.32 (1H, m), 2.23-2.12 (2H, m), 1.91-1.47 (5H, m), 1.12-1.00 (1H, m) IR (cm-1) (KBr) 2924, 1735, 1606, 1584, 1483, 1438, 1373, 1338, 1275, 1257, 1176, 1148, 1112, 1079, 1047, 1006, 937, 907, 891, 854, 793, 744

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand 3080-99-7 reaction routes.

Reference£º
Patent; TORAY INDUSTRIES, INC.; EP1555266; (2005); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

92-30-8,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.

Compound 2; 10-(3-Chloropropyl)-2-trifluoromethylphenothiazine; To a stirred solution of 2-trifluoromethyl phenothiazine (compound 1) (2g, 7.49 mmol) and sodium hydride (0.5 g, 10.42 mmol) in dry toluene (30 mL) was added l-bromo-3-chloropropane (1.57g, 10 mmol). 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 (3×50 mL) and the combined organic phase dried over anhydrous sodium sulphate. Final purification was performed by column chromatography (9:1 hexane: ethyl acetate) on silica gel to give 10-(3- chloropropyl)- 2-trifluoromethylphenothiazine (1.5 g, 58% ) as a solid.

The chemical industry reduces the impact on the environment during synthesis, 92-30-8,2-(Trifluoromethyl)-10H-phenothiazine,I believe this compound will play a more active role in future production and life.

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

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 92-30-8,2-(Trifluoromethyl)-10H-phenothiazine, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.92-30-8

92-30-8, 2-Trifluoromethylphenothiazine (2.00 g, 7.4831 mmol) was placed in a 500 mL flask, THF (100 mL) dried overanhydrous K2CO3 was added, and then 60% NaH was added sequentially under N2 protection. Mineral oil(1.1973 g, 29.9323 mmol) and 1-bromo-3-chloropropane (2.9601 mL, 29.9323 mmol) were refluxed overnightat a bath temperature of 65 C. After cooling to room temperature, the reaction mixture was poured into EtOAc EtOAc (EtOAc)EtOAc. Ethylacetate (50 mL) was added to dissolve, and silica gel powder (20 g) was added to the solution to dryness, and theresidue was applied to a silica gel column, eluted with ethyl acetate and petroleum ether, and the product wascollected, dried, and dried in vacuo. Product 2-10 (4.9444 g, yield 69.8%).

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 2-(Trifluoromethyl)-10H-phenothiazine.

Reference£º
Patent; Dalian University of Technology; Li Gaoquan; Xie Aiyun; Zhang Cuifang; Chen Maofen; (23 pag.)CN104829554; (2018); B;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

154127-42-1,Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide,154127-42-1, This compound has unique chemical properties. The synthetic route is as follows.

Prepare a 1L three-vial bottle equipped with a mechanical stirrer, a constant pressure dropping funnel, and an ice water bath.Added compound of formula A (50 g, 0.14 mol) and acetonitrile (250 mL),Under N2 protection, stirring and cooling to 5 ~ 10 C,Then DMF-DMA (17.5 g, 0.147 mol) was added dropwise thereto.The rate of addition is such that the stability of the system does not exceed 15C.After the addition, cooling was removed and the reaction was continued for 1 hour. TLC detected the disappearance of the starting material.Concentrate at normal pressure, recover the solvent and add the residue to DCM.Rotary evaporation is replaced by desolvation, and the mixture is finally dried under high vacuum for 1 hour. The residue is the compound of formula B-2.Can be directly after the subsequent reaction without purificationThe crude product B-2 was obtained in equivalent yield.

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 154127-42-1.

Reference£º
Patent; Shanghai Bo Shirui Life Technology Co., Ltd.; Wang Dong; Wang Fangdao; Wang Meng; Cai Maojun; (16 pag.)CN107722043; (2018); A;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

92-30-8 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.

General procedure: A stirred mixture of phenothiazine (100 mg, 0.5 mmol),3,5-dimethylphenol (183 mg, 1.5 mmol), and K2CO3 (69 mg,0.5 mmol) in ODCB (1.5 mL) was heated to 130 oC for 6 h under O2 balloon atmosphere. After the usual aqueous extractive workup and column chromatographic purification process (hexanes/EtOAc, 20:1) para-3a (103 mg, 64%) and ortho-3a (34 mg, 21%) were obtained as white solids. Other compounds were synthesized similarly, and the spectroscopic data of 3a-3m and the sulfoxide of 3g are as follows.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand 92-30-8 reaction routes.

Reference£º
Article; Yu, Jin; Moon, Hye Ran; Kim, Su Yeon; Kim, Jae Nyoung; Bulletin of the Korean Chemical Society; vol. 36; 11; (2015); p. 2765 – 2768;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem

In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 3939-23-9,3-Bromo-10H-phenothiazine, as follows.3939-23-9

2, under the protection of nitrogen will be prepared in step 1 aromatic diamine 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.

According to the analysis of related databases, 3-Bromo-10H-phenothiazine, the application of this compound in the production field has become more and more popular.

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

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a downstream synthesis route of the compound 37441-50-2,37441-50-2

To a mixture of 2,4-difluorobenzonitrile (10.0 g, 72 mmol) and 1,1-dioxo-1lambda6-[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) delta 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

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 37441-50-2.

Reference£º
Patent; Bristol-Myers Squibb Company; US2007/111984; (2007); A1;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem