Day: August 25, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.69812-29-9,2-Acetamido-4-methylthiazole-5-sulfonyl chloride,as a common compound, the synthetic route is as follows.

a) To a stirred solution of 2-(methylamino)-ethanol (0.44 g, 5.86 mmol) in THF (12 ml) was added at 0 C. (ice water bath) commercially available 2-acetamido-4-methylthiazole-5-sulfonyl chloride (1.0 g, 3.92 mmol) and triethylamine (0.6 ml, 4.32 mmol). The light yellow suspension was stirred at room temperature for 17 h, and evaporated. The crude product was further purified by flash chromatography on silica gel (dichloromethane/MeOH) and subsequent crystallization (dichloromethane/MeOH/hexane) to yield 2-acetamido-4-methyl-thiazole-5-sulfonic acid (2-hydroxy-ethyl)-methyl-amide (0.93 g, 81%) as a white solid. MS (ISP) 294.0 [(M+H)+]; mp 189 C.

As the paragraph descriping shows that 69812-29-9 is playing an increasingly important role.

Reference£º
Patent; Gatti McArthur, Silvia; Goetschi, Erwin; Wichmann, Juergen; Woltering, Thomas Johannes; US2006/183756; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3048-45-1,4-Chlorobenzo[d]thiazole,as a common compound, the synthetic route is as follows.

General procedure: To a solution of benzothiazoles or benzoxazoles (1, 1 mmol) in DMSO (3 mL), was added KOH (280 mg, 5 equiv) and 1,3-propanedithiol (207 muL, 2 mmol). The reaction mixture was heated under argon at 130 C for 12 h. After cooling to room temperature, water (10 mL) was added. The pH of the reaction mixture was adjusted to 3-4 using 5% HCl. The resulting mixture was extracted with ethyl acetate (15 mL ¡Á2). The organic layer was washed with water and brine, dried over anhydrous MgSO4 and concentrated using rotary evaporator. The crude product was purified by silica gel column chromatography using ethyl acetate/n-hexane as eluent to afford the corresponding heteroaryl thiols 3.

The synthetic route of 3048-45-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Xiao, Yan; Jing, Bing; Liu, Xiaoxia; Xue, Hongyu; Liu, Yajun; Beilstein Journal of Organic Chemistry; vol. 15; (2019); p. 279 – 284;,
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Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.432047-36-4,1-(2-Thiazolyl)ethylamine,as a common compound, the synthetic route is as follows.

Example 86: N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2,5-dimethylphenyl}-N’-[(1S)-1-(1,3-thiazol-2-yl)ethyl]urea 4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2,5-dimethylaniline (30 mg) was dissolved in chloroform (1 ml) and triethylamine (0.1 ml) to prepare a solution. A solution of triphosgene (35 mg) in chloroform (0.2 ml) was then added to the solution, and the mixture was stirred at room temperature for one hr. Next, a solution of (1S)-1-(1,3-thiazol-2-yl)-1-ethylamine (35 mg) in chloroform (0.2 ml) was added thereto, and the mixture was stirred at room temperature for 10 hr. The stirred mixture was purified by chromatography on silica gel using chloroform/methanol for development to give the title compound (30 mg, yield 68%). 1H-NMR (CDCl3, 400 MHz): delta 1.68 (d, J = 6.8 Hz, 3H), 2.10 (s, 3H), 2.30 (s, 3H), 4.09 (s, 3H), 4.11 (s, 3H), 5.33 – 5.39 (m, 1H), 6.29 (br, 1H), 6.47 (d, J = 6.1 Hz, 1H), 6.92 (s, 1H), 7.16 (br, 1H), 7.63 (s, 1H), 7.67 (d, J = 3.2 Hz, 1H), 7.75 (s, 1H), 7.84 (s, 1H), 8.38 (d, J = 6.1 Hz, 1H)

The synthetic route of 432047-36-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KIRIN BEER KABUSHIKI KAISHA; EP1535910; (2005); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5198-88-9,2-Bromothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

2-Bromo-l,3-thiazole-4-carboxylic acid (200.0 mg, 961 pmol), TEA (671 pL, 4.80 mmol), HATU (547.0 mg, 1.44 mmol) and (R)-N-((S)-l,3-dihydrospiro[indene-2,4′- piperidin]-l-yl)-2-methylpropane-2-sulfmamide (352.0 mg, 1.15 pmol, synthesized via Step a of Example 120) were placed into DMF(l5 mL). The reaction mixture was evacuated and refilled 3 times using N2, and the reaction mixture was stirred at 25 C for 1 hour. The mixture was then diluted with EtOAc (100 mL) and the mixture was washed with H20 (30 mL x 5), brine (50 mL), dried over anhydrous Na2S04, filtered and concentrated to give a residue. The residue was purified by silica gel chromatography (ethyl acetate in petroleum ether = 0% to 80%) to afford (S)-N-((S)- ‘-(2-bromothiazole-4-carbonyl)- 1 ,3- dihydrospiro[indene-2,4’-piperidin]-l-yl)-2-methylpropane-2-sulfmamide (458 mg, 96% yield) as yellow oil. LC-MS (ESI+) m/z: 498.0 (M+H)+.

The synthetic route of 5198-88-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; RELAY THERAPEUTICS, INC.; D.E. SHAW RESEARCH, LLC; TAYLOR, Alexander, M.; LESCARBEAU, Andre; KELLEY, Elizabeth, H.; SHORTSLEEVES, Kelley, C.; WALTERS, W., Patrick; MURCKO, Mark, Andrew; MCLEAN, Thomas, H.; GUNAYDIN, Hakan; GIORDANETTO, Fabrizio; THERRIEN, Eric; (607 pag.)WO2019/183367; (2019); A1;,
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1759-28-0, 4-Methyl-5-vinylthiazole is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1,3-bis(dicyclohexylphosphino)propane (dcypp: 20.0 mol%, 21.9mg) was dissolved in o-dichlorobenzene (1.0 mL) in a two-necked flask equipped under argon atmosphere. Then, RhH(CO)(PPh3)3 (10.0 mol%, 23.0 mg), 4-phenylthiazole 1a (0.25 mmol, 40.3 mg)and 2-methylthiothiazole 5 (0.75 mmol, 78 L) were added to the solution, and the mixture was heated at reflux for 3 h. Then, the solvent was removed under reduced pressure, and the residue was purified byflash columm chromatography on silica gel giving 2-(methylthio)-4-phenylthiazole 3a (38.5 mg, 74%). 3a11

The synthetic route of 1759-28-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Arisawa, Mieko; Nihei, Yuri; Yamaguchi, Masahiko; Heterocycles; vol. 90; 2; (2015); p. 939 – 949;,
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35272-15-2, 2-Methylthiazole-4-carboxylic acid is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General Procedure: To a 100 mL round bottom flask equipped with a stir bar were added 2- methyl-l,3-thiazole-4-carboxylic acid (1.0 g, 6.98 mmol), potassium carbonate (3.86 g, 27.9 mmol), N,N-dimethylformamide (20 mL) and iodomethane (0.52 mL 8.38 mmol). The reaction mixture was stirred at room temperature over the weekend, diluted with ethyl acetate (100 mL) and washed with water (100 mL). The aqueous layer was then extracted with ethyl acetate (3×75 mL). The combined organic layer was washed with brine (100 mL), dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The residue was purified on silica gel using hexanes:ethyl acetate = 80:20 to 50:50 in a gradient fashion, to give the desired product as an off-white solid (1.06 g, 97 percent). 1H NMR (300 MHz, CDCl3): delta 8.06 (s, IH), 3.95 (s, 3H), 2.78 (s, 3H).

As the paragraph descriping shows that 35272-15-2 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2007/87135; (2007); A2;,
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Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.80945-83-1,2-Chlorobenzothiazole-6-carbonitrile,as a common compound, the synthetic route is as follows.

Step B:; A solution of 2-chlorobenzothiazole-6-carbonitrile (14.9 g, 0.077 mol) in DMF (250 ml.) was added drop-wise at 100C to a mixture of anhydrous piperazine (60 g, 0.698 mol) and DMF (30OmL). Then the mixture was stirred for 2 h. Water (1 ,550 ml.) was added and the mixture was extracted with dichloromethane (5 x 500 ml_). The combined organic extracts was washed with water (6 x 500 ml_), dried (Na2SO4), filtered and evaporated to give a residue which was re-crystallised from ethyl acetate. This afforded 10.5 g (56 percent) of 2-(piperazin-1- yl)benzothiazole-6-carbonitrile. A mixture of this piperazine derivative (19.4 g, O.Odeltamol), sodium iodide (1.94 g), triethylamine (9.6 g, 0.095mol) and DMF (8OmL) was heated with stir- ring to give a red liquid. A solution of 2-bromopropane (14.7 g, 0.12mol) in DMF (8OmL) was added drop-wise at 117 0C within in 1 h. The reaction mixture was stirred at 1 10-117 0C for another 3 h and then allowed to cool to room temperature. Water (110 ml.) was added and the mixture was filtered. The filter cake was washed until the filtrate was colourless and then dried. The solid was dissolved in DMF (250 ml.) and filtered to remove a solid residue. Water (1000 ml.) was added to the filtrate with stirring to give a precipitate. The solid was isolated, washed with water and dried to give 9.4 g (41 percent) of 2-(4-lsopropylpiperazin-1-yl)benzo- thiazole-6-carbonitrile.1H-NMR delta 8.25 (s, 1 H), 7.61 (d, 1 H), 7.45 (d, 1 H), 3.55 (t, 4H), 2.68 (m, 1 H), 2.51 (m, 4H), 0.93 (d, 6H).

As the paragraph descriping shows that 80945-83-1 is playing an increasingly important role.

Reference£º
Patent; NOVO NORDISK A/S; WO2007/110364; (2007); 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.41731-83-3,Ethyl 2-bromothiazole-5-carboxylate,as a common compound, the synthetic route is as follows.

To a mixture of ethyl 2-bromo-1 ,3-thiazole-5-carboxylate (1.01 g, 4.29 mmol), K2CO3 (2.0 g, 14.47 mmol) and Pd(Pt-Bu3)2 (280 mg, 0.548 mmol) in 1 ,4-dioxane (8 ml.) and water (1.6 ml.) was added 1 -methyl-5-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)- 1 H-pyrazole (1.76 g, 8.47 mmol) [prepared in Preparation 2]. The reaction was stirred at 120 0C for 45 min in a microwave reactor and cooled to room temperature. The mixture was partitioned between CHCI3 / H2O and the aqueous layer was washed several times with CHCI3. The combined organic fractions were dried over Na2SO4, concentrated, and purified via column chromatography (silica, 0-50%EtOAc/hexanes) affording the title compound (0.7 g, 61%) as a yellow solid: LC-MS (ES) m/z = 238 (M+H)+.

41731-83-3 Ethyl 2-bromothiazole-5-carboxylate 3614103, athiazole compound, is more and more widely used in various.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/158372; (2009); A1;,
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Thiazole | chemical compound | Britannica

53332-78-8, Thiazol-2-ylmethanamine dihydrochloride is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 24.2-Chloro-7-methyl-8-propoxy-N-(thiazol-2-ylmethyl)-7H-purin-6- amine A mixture of 2,6-dichloro-7-methyl-8-propoxy-7H-purine (28 mg, 0.11 mmol), thiazol-2-ylmethanamine dihydrochloride (70 mg, 0.37 mmol) and triethylamine (0.16 mL, 1.14 mmol) in DMSO (1.5 mL) was stirred at 60 C for 2 h. After this time the mixture was cooled to room temperature, diluted with EtOAc and washed with water and brine. The organic layer was concentrated and the resulting residue was purified by column chromatography (silica, 0-5% MeOH in CH2Cl2) to provide 2-chloro-7-methyl- 8-propoxy-N-(thiazol-2-ylmethyl)-7H-purin-6-amine (21 mg, 56%): ESI MS (M+H) 339; 1H NMR (500 MHz, DMSO-d6) G 7.93 (s, 1H), 7.73 (d, J = 3.3 Hz, 1H), 7.61 (d, J = 3.3 Hz, 1H), 4.90 (s, 2H), 4.44 (t, J = 6.5 Hz, 2H), 3.73 (s, 3H), 1.84-1.76 (m, 2H), 0.99 (t, J = 7.4 Hz, 3H).

As the paragraph descriping shows that 53332-78-8 is playing an increasingly important role.

Reference£º
Patent; THE GENERAL HOSPITAL CORPORATION; UNITED STATES DEPARTMENT OF HEALTH AND HUMAN SERVICES; SLAUGENHAUPT, Susan, A.; JOHNSON, Graham; PAQUETTE, William, D.; ZHANG, Wei; MARUGAN, Juan; (306 pag.)WO2016/115434; (2016); 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.302964-24-5,2-Amino-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide,as a common compound, the synthetic route is as follows.

5mmol N,N-dimethylglycine,2mmol CuI,20mmol 4,6-dichloro-2-methylpyrimidine is soluble100 mL of N,N-dimethylformamide (DMF),22 mmol of N-hydroxyethylpiperazine was added with stirring.40mmol K3PO4, stir at room temperature for 40min,22 mmol of 2-amino-N-(2-chloro-6-methylphenyl)-5-thiazolecarboxamide was added with stirring.Passing N2 and reacting at 120 C for 6 h,The copper salt was dissolved in 50 mL of aqueous ammonia, and extracted with 50 mL of EtOAc (EtOAc).The crude product was added to 100 mL of an 80% aqueous ethanol solution, and stirred.2 g of activated carbon was added, refluxed for 30 min, filtered while hot, and the filtrate was recrystallized overnight, filtered, and the filter cake was washed with ice-cold 80% aqueous ethanol solution and dried.That is, 8.64 g of a white solid was obtained, the yield was 88.41%, and the purity was 99.92%.

As the paragraph descriping shows that 302964-24-5 is playing an increasingly important role.

Reference£º
Patent; Shandong Luoxin Pharmaceutical Group Co., Ltd.; Shandong Luoxin Pharmaceutical Group Hengxin Pharmaceutical Co., Ltd.; Shandong Yuxin Pharmaceutical Co., Ltd.; Gao Hongjun; Ren Qingwei; Zhang Qingdong; (12 pag.)CN109879869; (2019); A;,
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Thiazole | chemical compound | Britannica