Day: November 3, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.51640-36-9,2-Chlorothiazole-5-carbonitrile,as a common compound, the synthetic route is as follows.

To an NMP (1 mL) solution of (trans)- 3-(5-fluoro-2-methoxyphenoxy)-/V-(pyrrolidin-3- yl)cyclobutanecarboxamide hydrochloride (Intermediate 70) (38 mg, 0.1 1 mmol) and 2- chlorothiazole-5-carbonitrile (16 mg, 0.1 1 mmol) in a microwave reaction vial was added N,N- diisopropylethylamine (0.08 mL, 0.4 mmol). The reaction was heated in a microwave (135 C) for 3.5 h, concentrated and loaded onto a semi-prep HPLC (NH4OH as modifier) for purification to afford the title compound as a tan solid (31 mg, 62%). 1H NMR (400 MHz, CDCI3) delta 2.09 (dd, J = 13, 7 Hz, 1 H), 2.42 (dd, J = 13, 6 Hz, 1 H), 2.46-2.58 (m, 2 H), 2.74 (ddd, J = 14, 7, 4 Hz, 2 H), 2.95-3.04 (m, 1 H), 3.40 (dd, J = 1 1 , 4 Hz, 1 H), 3.57-3.69 (m, 2 H), 3.81 -3.89 (m, 1 H), 3.84 (s, 3 H), 4.64-4.74 (m, 1 H), 4.94 (t, J = 7 Hz, 1 H), 5.59-5.72 (m, 1 H), 6.47 (dd, J = 10, 3 Hz, 1 H), 6.59 (td, J = 8, 3 Hz, 1 H), 6.78 (dd, J = 9, 5 Hz, 1 H), 7.71 (s, 1 H); LC-MS (LC- ES) M+H = 417., 51640-36-9

51640-36-9 2-Chlorothiazole-5-carbonitrile 1485222, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; DEATON, David Norman; GUO, Yu; HANCOCK, Ashley Paul; SCHULTE, Christie; SHEARER, Barry George; SMITH, Emilie Despagnet; STEWART, Eugene L.; THOMSON, Stephen Andrew; (556 pag.)WO2018/69863; (2018); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2634-33-5,1,2-Benzothiazol-3-one,as a common compound, the synthetic route is as follows.,2634-33-5

General procedure: The acid 4 (5 mmol), EDC (1.2 g, 6.26 mmol), HOBt (0.9 g,5.88 mmol), NMM (1.2 mL, 10.74 mmol), and dichloromethane (10 mL) were mixed at ice-bath and stirred at 0 C for half an hour. 1,2-Benzisothiazol-3-one 1 (800 mg, 5.3 mmol) was added to NMM (1.6 mL, 14.32 mmol) in 10 mL of dichloromethane at 0 Ct hen the above mixture was added and stirred at room temperature overnight. After stirring overnight, the mixture was diluted with CH2Cl2, and then successively through washed with water, 5% KHSO4 solution, saturated NaHCO3 solution, and brine, the extract was dried with anhydrous Na2SO4 and evaporated under vacuum. The product was isolated by column chromatography (petroleum ether/CH2Cl2, 10:1) to yield the final compound. 4.2.19 2-(3-(2-Methoxyphenyl)propanoyl)benzo[d]isothiazol-3(2H)-one (23) Compound 23 was prepared through 3-(2-methoxyphenyl)propionic acid, obtained a white solid in 93% yield. Mp 149.5-150.7 C. 1H NMR (400 MHz, CDCl3) delta 8.00 (d, J = 8.0 Hz, 1H), 7.68 (t, J = 8.0 Hz, 1H), 7.51 (d, J = 8.0 Hz, 1H), 7.39 (t, J = 8.0 Hz, 1H), 7.25-7.17 (m, 2H), 6.89 (t, J = 8.0 Hz, 1H), 6.85 (d, J = 8.4 Hz, 1H), 3.82 (s, 3H), 3.47 (t, J = 7.6 Hz, 2H), 3.09 (t, J = 7.6 Hz, 2H). 13C NMR (101 MHz, DMSO-d6) delta 172.9, 163.5, 157.6, 141.4, 135.0, 130.2, 128.6, 128.1, 127.4, 126.5, 125.7, 122.5, 120.8, 111.1, 55.7, 37.5, 24.9. IR (KBr, cm-1): 1689, 1675. HRMS-ESI (m/z) calcd for C17H15NO3S [M+H+] 314.0851, found 314.0843.

The synthetic route of 2634-33-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Li, Zhenghui; Pan, Yang; Zhong, Weilong; Zhu, Yunpeng; Zhao, Yongle; Li, Lixin; Liu, Wei; Zhou, Honggang; Yang, Cheng; Bioorganic and Medicinal Chemistry; vol. 22; 24; (2014); p. 6735 – 6745;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

1452-15-9, 4-Cyanothiazole is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of 4-cyanothiazole (5.0 g, 45.0mmol) in o-dichlorobenzene (40.0 mL) was added the respective aniline (1) (49.0 mmol). The reaction mixture was heated at 135 C with purging excess dry HCl for 3 h. Then, cooled the reaction mixture to 40 C and the resulting solids were filtered, washed with more o-dichlorobenzene (10.0 mL). The solids were dried at 90 C under vacuum to give amidine hydrochlorides with yields in the 70-90% range., 1452-15-9

1452-15-9 4-Cyanothiazole 15069, athiazole compound, is more and more widely used in various fields.

Reference£º
Article; Patil, Vikrant; Barragan, Enrique; Patil, Shivaputra A.; Patil, Siddappa A.; Bugarin, Alejandro; Tetrahedron Letters; vol. 58; 35; (2017); p. 3474 – 3477;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78502-71-3,Ethyl 2-(bromomethyl)thiazole-4-carboxylate,as a common compound, the synthetic route is as follows.

78502-71-3, To a solution of ethyl2-(bromomethyl)-1,3-thiazole- 4-carboxylate (19, 2.4 g, 9.7 mmol) in toluene (20 mL) triphenylphosphine (2.7 g,10 mmol) was added at room temperature, and the resulting mixture was stirred at 100 C for 3 h. The reactionmixture was cooled to room temperature, and the precipitate was collected by filtration, washed with hexanes, anddried to afford ((4-(ethoxycarbonyl)-1,3-thiazol-2-yl)methyl)(triphenyl)phosphonium bromide (31, 3.7 g, 74%) as abrown powder, which was used without further purification. To a mixture of compound 30 (2.2 g, 5.5 mmol) andcompound 31 (3.7 g, 7.2 mmol) in N,N-dimethylformamide (20 mL) was added sodium ethoxide (0.75 g, 11 mmol)at room temperature, and the resulting mixture was stirred at room temperature for 3 h. The reaction mixture waspartitioned between ethyl acetate and water. The organic layer was separated, washed with brine, dried over MgSO4,and concentrated in vacuo. The residue was purified by column chromatography (silica gel, eluting with a gradientof 10-50% ethyl acetate in hexanes) to afford the title compound 20a (1.8 g, 60%) as a pale yellow powder.

78502-71-3 Ethyl 2-(bromomethyl)thiazole-4-carboxylate 11043146, athiazole compound, is more and more widely used in various fields.

Reference£º
Article; Maezaki, Hironobu; Tawada, Michiko; Yamashita, Tohru; Banno, Yoshihiro; Miyamoto, Yasufumi; Yamamoto, Yoshio; Ikedo, Koji; Kosaka, Takuo; Tsubotani, Shigetoshi; Tani, Akiyoshi; Asakawa, Tomoko; Suzuki, Nobuhiro; Oi, Satoru; Bioorganic and Medicinal Chemistry Letters; vol. 27; 15; (2017); p. 3565 – 3571;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

1247119-36-3, (S)-Ethyl 2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanoate oxalate is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 7: Preparation of cobicistat silicon dioxide Thiazole ethyl ester salt (formula 2) (150 g) in water (250 ml) was added to dichloromethane (800 ml), followed by a slow addition of aqueous potassium bicarbonate (220 g of potassium bicarbonate dissolved 1.250 1 of water). The resulting mixture was stirred for about 1 hour and the aqueous and organic layers were separated. The organic layer was washed with water and then concentrated under vacuum until the reaction mass volume reached about 350 ml. The reaction mass was cooled to about 5 C. An aqueous potassium hydroxide solution (about 23 g of KOH dissolved in 25 ml of water) was slowly added to the cooled reaction mass while maintaining a temperature not more than about 10 C. The mixture was then stirred for about 12 hours at the same temperature. Cobicistat intermediate of formula 3 (100 g) and dichloromethane (350 ml), were added to the mixture and the temperature was adjusted to about -20 C. Hydroxybenzotriazole hydrate (about 25 g) was then added to this mixture. A pre-cooled solution (about -20 C of N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (80 g) in dichloromethane (about 800 ml)) was added to the reaction mixture while the reaction mass temperature was maintained at not more than about -20 C. The reaction mixture was then stirred at about the same temperature for 24 hours. The reaction mass temperature was then adjusted to about 5 C and the reaction was quenched with an aqueous citric acid solution. The aqueous and organic layers were separated and the organic layer was washed once with aqueous potassium bicarbonate solution and water. The organic layer was concentrated under reduced pressure to give cobicistat (about 160 g) as a residue. The residue was dissolved in mixture of dichloromethane (160 ml) and n- hexane (160 ml) at room temperature. Silicon dioxide (150 g) was added to the mixture and stirred for 2-3 hours. The solution was concentrated, cooled, and filtered to give a cobicistat silicon dioxide product (300 g)., 1247119-36-3

The synthetic route of 1247119-36-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MYLAN LABORATORIES LTD.; VADALI, Lakshmana Rao; KONDA, Rameshbabu; DANDALA, Ramesh; WO2015/83066; (2015); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10200-59-6,2-Thiazolecarboxaldehyde,as a common compound, the synthetic route is as follows.

Manufacturing Example 88-1-1 Thiazole-2-yl-methanol; To a mixture of 2-formylthiazole (300 mg, 2.65 mmol) and methanol (30 mL) was added sodium borohydride (201.0 mg, 5.30 mmol) at 0 C., which was stirred for 1 hour at room temperature. Water was added to this reaction mixture, which was then extracted with ethyl acetate. The organic layer was separated, washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, and filtered. The filtrate was concentrated under a reduced pressure, and the residue was purified by NH silica gel column chromatography (diethyl ether) to obtain the title compound (251.2 mg, 82%).1H-NMR Spectrum (DMSO-d6) delta (ppm): 4.74 (2H, d, J=6.0 Hz), 6.04 (1H, t, J=6.0 Hz), 7.63-7.65 (1H, m), 7.73-7.75 (1H, m)., 10200-59-6

As the paragraph descriping shows that 10200-59-6 is playing an increasingly important role.

Reference£º
Patent; Tanaka, Keigo; Yamamoto, Eiichi; Watanabe, Naoaki; US2009/82403; (2009); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

19759-66-1, 2-Aminobenzothiazole-6-carbonitrile is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

0.88g (0.005 mol) 2-amino-6-cyanobenzothiazole was dissolved in 10 mL of N,N-dimethylformamide, 0.4 g (0.01 mol) of sodium hydroxide was added with stirring, After 10 minutes, 1.26 g (0.005 mol) of 2,6-dichloro-3,5-dinitrotoluene was added thereto, The reaction was continued at room temperature for 5 hours. After completion of the TLC monitoring reaction, the reaction solution was poured into 50 mL of saturated brine and extracted with ethyl acetate. The organic phase was extracted with anhydrous magnesium sulfate and evaporated under reduced pressure. The residue was subjected to column chromatography (eluent ethyl acetate and petroleum ether (Boiling range 60-90 C) in a volume ratio of 1:10) to give 0.40 g of compound 4405, Yellow solid. Melting point 229-231 C., 19759-66-1

The synthetic route of 19759-66-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SINOCHEM CORP; Shenyang Research Institute Of Chemical Industry Co., Ltd .; GUAN, AIYING; LI, HUICHAO; SUN, QIN; LIU, CHANGLING; WANG, JUNFENG; SUN, XUFENG; YANG, FAN; (21 pag.)CN104177310; (2016); B;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2933-29-1,2-Amino-4,5,6,7-tetrahydrobenzothiazole,as a common compound, the synthetic route is as follows.

30 mg (0.19 mmol) of 4,5,6,7-tetrahydrobenzo [d] thiazol-2-amine 53 mg (0.19 mmol) of 2, 4′-dibromoacetophenone was dissolved in 3 ml of ethanol and stirred in a microwave reactor at 150 C for 20 minutes. The residue was concentrated under reduced pressure and subjected to column chromatography (EtOAc: Hex = 1: 5) to obtain Compound 2c (14 mg, 22%)., 2933-29-1

2933-29-1 2-Amino-4,5,6,7-tetrahydrobenzothiazole 18046, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Chung-Ang University Industry-Academic Cooperation Foundation; Min, Kyung Hoon; Kwon, Ahra; Song, Ji Ho; (22 pag.)KR2017/23387; (2017); A;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

62266-82-4, 6-Bromobenzo[d]thiazol-2(3H)-one is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

62266-82-4, Example 12A 2-amino-5-bromothiophenol and its disulfide A mixture of 6-bromobenzothiazolone (CAS number 62266-82-4, Aldrich Chemical Company (12.9 g, 56.1 mmol), NaOH (33 g, 0.825 mol) and water (90 mL) was heated to 100 C. for 15 hours under nitrogen. The mixture was cooled to 0 C. and pH was adjusted to pH 5 using 5N acetic acid at 0-10 C. under nitrogen. The precipitate was filtered, washed with water and vac. dried at 45 C. to give the product as a mixture of 2-amino-5-bromothiophenol and its disulfide (11.47 g, 100%).

62266-82-4 6-Bromobenzo[d]thiazol-2(3H)-one 188444, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Cowart, Marlon D.; Ku, Yi-Yin; Chang, Sou-Jen; Fernando, Dilinie P.; Grieme, Timothy A.; Altenbach, Robert J.; US2004/224953; (2004); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

2516-40-7, 2-Bromobenzothiazole is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The corresponding halide reagent (1mmol) was added to a mixture of thiourea (1.1mmol) (compounds a) or selenourea (compounds b) in absolute ethanol or dry methanol (20mL) for compound 1b. The mixture was stirred at reflux for 0.5?15h. The product was isolated by filtration or by rotatory evaporation of the solvent under vacuum and purified by recrystallization, washing or column chromatography., 2516-40-7

As the paragraph descriping shows that 2516-40-7 is playing an increasingly important role.

Reference£º
Article; Alcolea, Veronica; Plano, Daniel; Encio, Ignacio; Palop, Juan Antonio; Sharma, Arun K.; Sanmartin, Carmen; European Journal of Medicinal Chemistry; vol. 123; (2016); p. 407 – 418;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica