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54001-17-1

2-(4-CHLOROPHENYL)-4-METHYL-1,3-THIAZOLE-5-CARBOXYLIC ACID synthesis

4synthesis methods
-

Yield:54001-17-1 83%

Reaction Conditions:

with lithium hydroxide monohydrate in methanol;ethanol;lithium hydroxide monohydrate; for 3 h;

Steps:

2-(4-Chlorophenyl)-4-methylthiazole-5-carboxylic acid (3a)

LiOH (1.27 g, 53.4 mmol) was added to a solution of ethyl 2-(4-chlorophenyl)-4-methylthiazole-5-carboxylate (2.5 g, 8.9 mmol) in a 1:1:1 mixture of H2O/EtOH/MeOH (45 ml). The solution was then stirred for 3 h under reflux. After returning to ambient temperature, the solution was filtered and the filtrate was reduced under reduced pressure. Water (50 ml) was added and the pH was adjusted to 3-4 with HCl. The solid was filtered, washed with water and dried under vacuum for 15 h to give 1.87 g of acid 3a (7.4 mmol, 83%) as a white solid. 1H NMR (400 MHz, (CD3)2SO) δ 7.98 (d, J = 8.4 Hz, 2H), 7.57 (d, J = 8.4 Hz, 2H), 2.67 (s, 3H). 13C NMR (100, MHz, (CD3)2SO) δ 167.5, 163.3, 160.1, 136.3, 131.6, 129.9, 128.6, 123.8, 17.5.

References:

Chouha, Nora;Abou-Hamdan, Hussein;Yurugi, Hajime;Yoshii, Riku;Ii, Hiromi;Najem, Ahmad;Ghanem, Ghanem E.;Nakata, Susumu;Rajalingam, Krishnaraj;Peng, Yu;Wang, Dong;Nebigil, Canan G.;Désaubry, Laurent [European Journal of Medicinal Chemistry,2022,vol. 242,art. no. 114635] Location in patent:supporting information

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