Day: November 17, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4175-77-3,2,4-Dibromothiazole,as a common compound, the synthetic route is as follows.

A flask containing 238 mg of tetrakis(triphenylphosphine)palladium, 0.55 g of phenylboronic acid, and 1.00 g of 2,4-dibromothiazole was purged with nitrogen and then charged with 30 ml of toluene, 6.1 ml of ethanol, and 9.1 ml of a 2 M aqueous solution of sodium carbonate, and the mixture was stirred under reflux for 6 hours. After cooling to room temperature, 50 ml of water was added to the reaction mixture and two extractions were conducted with 50 ml of ethyl acetate. After being washed with 30 ml of saturated brine, the organic layer was dried over magnesium sulfate. After filtering the magnesium sulfate, the organic layer was concentrated and the residue was purified by column chromatography (Wakogel C-200; hexane:ethyl acetate=14:1) to give 0.71 g of 2-phenyl-4-bromothiazole., 4175-77-3

4175-77-3 2,4-Dibromothiazole 2763297, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; SDS Biotech K.K.; Sakai, Masaaki; Matsumura, Tomoaki; Midorikawa, Satohiro; Nomoto, Takashi; Muraki, Tomoko; Katsuki, Ryutaro; US2013/296271; (2013); 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.40004-69-1,2-Methyl-5-thiazolecarboxylic acid,as a common compound, the synthetic route is as follows.

Synthesis of (F); To a 0¡ã C. solution of Compound (D) (41 mmol) and 2-methyl-thiazole-5-carboxylic acid (E) (6.0 g, 42 mmol), HOBT (7.9 g, 50 mmol) and HBTU (18.0 g, 50 mmol) in tetrahydrofuran (800 mL) was added a solution of N,N-diethylisopropylamine (50 g) in tetrahydrofuran (200 mL) over 5 minutes until its pH reached approximately 8.5. The resulting mixture was stirred at same temperature overnight. It was then quenched with saturated aqueous sodium bicarbonate solution (200 mL), and most of the solvents were removed under reduced pressure. The residual mixture was extracted with ethyl acetate (3.x.400 mL). The combined organic layers were washed with saturated aqueous sodium bicarbonate (200 mL) and brine (100 mL), dried over sodium sulfate and filtered through Celite-545. The solvents were removed under reduced pressure and residue was purified by flash chromatography (silica gel, ethyl acetate with 2percent methanol). Compound (F) (17.1 g) was isolated and characterized by LC/MS (LRMS (MH) m/z: 436.15)., 40004-69-1

40004-69-1 2-Methyl-5-thiazolecarboxylic acid 98845, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Onyx Therapeutics, Inc.; US2010/240903; (2010); A1;,
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Thiazole | chemical compound | Britannica

131184-73-1, (2-Aminothiazol-5-yl)methanol is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a DMF (4 mL) solution of (frans)-3-(quinolin-8-yloxy)cyclobutanecarboxylic acid (Intermediate 79) (80 mg, 0.33 mmol) was added HATU (150 mg, 0.395 mmol) and N,N- diisopropylethylamine (0.17 mL, 1 .0 mmol). After 5 minutes, (2-aminothiazol-5-yl)methanol (51 .4 mg, 0.395 mmol) was added, and the mixture was stirred for 3 h, quenched with water, extracted with EtOAc, dried over Na2SC>4, filtered and concentrated. The residue was purified on silica gel, eluting with a 0%-100% EtOAc:EtOH (3:1)-hexanes gradient to give the title compound (26 mg, 21 %). 1H NMR (400 MHz, CD3SOCD3) delta 2.39-2.51 (m, 2 H), 2.79 (qd, J = 7, 5 Hz, 2 H), 3.40-3.48 (m, 1 H), 4.57 (d, J = 5 Hz, 2 H), 5.00-5.10 (m, 1 H), 5.35 (t, J = 5 Hz, 1 H), 6.97 (dd, J = 1, 2 Hz, 1 H), 7.26 (s, 1 H), 7.42-7.59 (m, 3 H), 8.29 (dd, J = 8, 2 Hz, 1 H), 8.84 (dd, J = 4, 2 Hz, 1 H), 12.00 (s, 1 H); LC-MS (LC-ES) M+H = 356.

131184-73-1, The synthetic route of 131184-73-1 has been constantly updated, and we look forward to future research findings.

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;,
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Thiazole | chemical compound | Britannica

14527-41-4, 5-Thiazolecarboxylic acid is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,14527-41-4

To a solution of 47 mg (0.36 mmol, 1.1 eq.) of thiazole-5-carboxylic acid in 3 mL of THF at0 C were added 72 mg (0.47 mmol, 1.5 eq.) of hydroxybenzotriazole hydrate and 103 mg(0.54 mmol, 1.7 eq.) of 1 -ethyl-3 -(3 -dimethylaminopropyl)carbodiimide hydrochloride. Theresulting mixture was stirred for 15 mm and 0.16 mL (0.9 mmol, 2.8 eq.) of N,Ndiisopropylethylamine was added, followed by 110mg (0.32 mmol, R:S1:4, 1 eq.) 4- amino-N-(3,4-diflurophenyl)chromane-8-carboxamide hydrochloride (XIIIa). The reaction mixture was allowed to warm to room temperature and stirred for 12 h. The mixture was then diluted with 20 mL of water, and extracted with 2 x 50 mL of methylene chloride. Thecombined organic extracts were dried (Na2SO4) and filtered, and the solvent was removed invacuo. The product was isolated by flash column chromatography (Si02, eluting with 50%EtOAc/hexanes) to provide 110 mg (83%) of N-(8-((3,4-difluorophenyl)carbamoyl)chroman-4-yl)thiazole-5-arboxamide (12). The enantiomers were subsequently separated by SFC(Waters SFC investigator). Method isocratic, Mobile phase MeOH: CO2 – 30:70. Column:CHIRALCEL 0TH (250 x 21) mm, 5 tim, flow rate: 50 g/min to provide 80 mg of (S)-N-(8-((3 ,4-difluorophenyl)carbamoyl)chroman-4-yl)thiazole-5-carboxamide (12). LCMS: m/z:416.5 [M+Hj LCMS, Method B: RT 2.05 mm; HPLC, Method E: RT 6.98 mm; 1H NMR(oH, 400 MHz, DMSO-d6) 2.08-2.15 (m, 1H), 2.17-2.23 (m, 1H), 4.42 (t, 2H), 5.31 (t, 1H),7.04 (t, 1H), 7.37-7.57 (m, 4H), 7.96 (t, 1H), 8.55 (s, 1H), 9.19 (d, 1H), 9.26 (s, 1H).

The synthetic route of 14527-41-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARBUTUS BIOPHARMA, INC.; COLE, Andrew G.; KULTGEN, Steven; (203 pag.)WO2018/52967; (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.2406-90-8,2-Chlorobenzo[d]thiazol-6-amine,as a common compound, the synthetic route is as follows.

Add oxalyl chloride (10 mL, 114.6 mmol) and DMF (4 drops) to a stirring suspension of4′-fluoro-biphenyl-4-carboxylic acid (4.9 g, 22.7 mmol) in CH2Cl2 (150 mL). Stir the reaction mixture at room temperature for 3 h. Concentrate the mixture in vacuo, add n-hexane, re- concentrate, and re-dissolve in CH2Cl2. Add the resultant 4′-fluoro-biphenyl-4-carbonyl chloride solution to a mixture of 2-chloro-benzothiazol-6-ylamine (3.31 g, 17.9 mmol) and pyridine (3.0 mL) in CH2Cl2 (150 mL). Stir the reaction mixture overnight at room temperature. Dilute the reaction mixture with CH2Cl2. Wash the reaction mixture twice with LOM HCl and once with LOM NaOH. Dry the mixture over Na2SO4, concentrate in vacuo, and triturate with MeOH to yield the desired product (6.34 g, 93%). 1H NMR (400 MHz, DMSO-d6): deltaltheta.59 (s, IH), 8.69 (d, J = 1.6Hz, IH), 8.09 (d, J= 8.0Hz, 2H), 7.96 (d, J = 8.8Hz, IH), 7.87-7.79 (m, 5H), 7.38-7.31 (m, 2H)., 2406-90-8

The synthetic route of 2406-90-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2006/66173; (2006); A2;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

88982-82-5,88982-82-5, 4-Bromo-1,3-thiazole-2-carboxylic acid is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 4-Bromothiazole-2-carboxylic acid (compound 1, 1 eq) and boronic acid derivatives (compound 2a-g, 1.5 eq) were suspended in dimethoxy ethane (DME)/H2O (16 volume, 3:1). Then, Pd(PPh3)4 (0.05 eq) and K2CO3 (1.5 eq) were added to the suspension. The obtained mixture was heated to about 100 C and stirred for about 24 h under nitrogen atmosphere. The solution was cooled to room temperature and acidified with concentrated hydrochloric acid. Then, the precipitate was filtered and washed with water. The obtained wet cake was redissolved in dichloromethane. The organic phase was washed with saturated sodium bicarbonate (NaHCO3) aqueous solution for 30 min. Then, the aqueous phase was acidified again with concentrated hydrochloric acid, and the precipitate was filtered to obtained compounds 3a-g.

The synthetic route of 88982-82-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Haibo; Cai, Zhengjiang; Zheng, Shan; Ma, Huidan; Lin, Haiming; Zheng, Xiaohe; Letters in drug design and discovery; vol. 15; 4; (2018); p. 388 – 397;,
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.61296-22-8,2-Amino-5-bromothiazole monohydrobromide,as a common compound, the synthetic route is as follows.,61296-22-8

5-(4-Methoxy-2-methyl-phenyl)-4-methyl-thiophene-2-sulfonyl chloride (95 mg, 0.30 mmol, 1.5 equiv.) was dissolved in 0.3 ml MeCN, followed by the addition of sodium cyanate (28.6 mg, 0.44 mmol, 2.2 equiv.). Under strong stirring, pyridine (0.055 ml, 0.68 mmol, 3.4 equiv.) was added dropwise to the reaction mixture which was further stirred for 4 hrs at rt. 2-Amino-5-bromothiazole. HBr (52 mg, 0.20 mmol, 1.0 equiv.), was added and the reaction stirred for 1 hour. Water (20 ml) and 70% acetic acid (2 ml) were added to the suspension which was filtered, washed with water and cold MeOH. The crude solid was dissolved in MeCN-DMSO and chromatographed on a HPLC 75*30 mm RP 18 5 mum column, with A=0.1% HCOOH and B=MeCN and with a gradient of 40% to 90% B in 10 min. The desired fractions were lyophilized to give N-[(5-bromo-1,3-thiazol-2-yl)carbamoyl]-5-(4-methoxy-2-methylphenyl)-4-methylthiophene-2-sulfonamide, 16 mg, m/e 499.9 (MH-).

61296-22-8 2-Amino-5-bromothiazole monohydrobromide 2723848, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Gubler, Marcel; Haap, Wolfgang; Hebeisen, Paul; Kitas, Eric A.; Kuhn, Bernd; Minder, Rudolf E.; Schott, Brigitte; Wessel, Hans P.; US2007/281979; (2007); A1;,
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

General procedure: One equivalent of appropriate heterocyclic derivative was dissolved in DMF. Three equivalents of potassium carbonate and 1.2 equivalent of the appropriate 3-chloropropan-1-amine derivative were added. The resulting mixture was heated at 70C until disappearance of the starting material. The reaction was monitored by TLC. After 24-96 h, the solvent was removed under reduced pressure, and water added to the residue. The crude product was extracted with dichloromethane. The combined organic fractions were washed with water and dried over magnesium sulphate. Purification by thick layer chromatography or column chromatography was performed.

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

Reference£º
Article; Donnier-Marechal, Marion; Carato, Pascal; Le Broc, Delphine; Furman, Christophe; Melnyk, Patricia; European Journal of Medicinal Chemistry; vol. 92; (2015); p. 575 – 582;,
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.161798-03-4,Ethyl 2-(3-formyl-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylate,as a common compound, the synthetic route is as follows.

172.8 g of formic acid and16.0 g of ethyl 2-(3-formyl-4-isobutoxy-phenyl)-4-methyl-thiazole-5-carboxylate (FBT-1) prepared in Example 1 were added to a 500 ml round bottom flask, 4.2g hydroxylamine hydrochloride and 4.1g sodium formate were added, and stirred at 105 ~ 110 C for 2h. After completion of the reaction, cooled to 20 ~ 30 C, heat crystallization was carried out for 1h, filtered, filter cake was washed with 25.3g ethanol, filtered, dried and 14.2 g of ethyl 2-(3-cyano-4-isobutoxy-phenyl)-4-methyl-thiazole-5-carboxylate (FBT-2) was obtained in a yield of 89.5%., 161798-03-4

The synthetic route of 161798-03-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hunan Fangsheng Pharmaceutical Co., Ltd.; Zhang Qinghua; Chen Bo; Yan Zhiyong; (6 pag.)CN109912531; (2019); A;,
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Thiazole | chemical compound | Britannica

71224-95-8, 2-Aminobenzo[d]thiazole-7-carboxylic acid is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

71224-95-8, Example 116, 2-amino-N-(5-(2,3-dihvdrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)benzo[d]thiazole-7-carboxamide[00153] HATU (0.201 g, 0.53 mmol) and DIPEA (0.230 mL, 1 .32 mmol) were added to a solution of 2-aminobenzo[d]thiazole-7-carboxylic acid (102 mg, 0.53 mmol) in DMA (3 mL) under an inert atmosphere and the reaction allowed to stir for 15 minutes. Compound 2 (0.125 g, 0.440 mmol) was added and the reaction stirred at ambient temperature for approximately 24 hours and then at 40 C overnight. No product was observed. Additional 2-aminobenzo[d]thiazole-7-carboxylic acid (102 mg, 0.53 mmol) was converted to the acid chloride by treatment with oxalyl chloride (approximately 1 .2 equivalents) and DMF (a few drops) in DCM and the acid chloride added to the reaction mixture. The reaction was diluted with water and the solids filtered. The solids were dissolved in DMF and purified by preparative HPLC. Fractions containing the desired compound were evaporated to dryness to afford the desired material as a white solid (0.043 g, 21 %).1H NMR (400 MHz, DMSO) delta 10.05 (s, 1 H), 10.04 (s, 1 H), 7.87 (d, J = 7.1 Hz, 1 H), 7.82 (d, J = 2.2 Hz, 1 H), 7.62 (dd, J = 2.2, 8.3 Hz, 1 H), 7.49 – 7.56 (m, 3H), 7.47 (s, 2H), 7.39 (t, J = 7.8 Hz, 1 H), 7.25 (d, J = 8.5 Hz, 1 H), 6.98 (d, J = 8.4 Hz, 1 H), 4.28 – 4.35 (m, 4H), 2.21 (s, 3H). m/z (ES+), (M+H)+ = 461 .

The synthetic route of 71224-95-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; JONES, Keith; RYE, Carl; CHESSUM, Nicola; CHEESEMAN, Matthew; PASQUA, Adele Elisa; PIKE, Kurt Gordon; FAULDER, Paul Frank; WO2015/49535; (2015); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica