反应详情

At room temperature, cyclohexanol (82 mg), dimethylaminopyridine (10 mg) and 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide (150 mg) are added to a solution of 2-(4-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperazin-1-yl)-1,3-thiazole-4-carboxylic acid (XXXIV-1, 300 mg) in dichloromethane (5 ml). The mixture is stirred overnight, and water is then added. The aqueous phase is separated off and extracted with ethyl acetate. The combined organic phases are dried with sodium sulphate. The solid is filtered off and the solvent is removed by distillation. The residue is purified chromatographically. This gives cyclohexyl 2-(4-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperazin-1-yl)-1,3-thiazole-4-carboxylate (45 mg, 12%).

1. customThe aqueous phase is separated off
2. extractionextracted with ethyl acetate
3. dry with materialThe combined organic phases are dried with sodium sulphate
4. filtrationThe solid is filtered off
5. customthe solvent is removed by distillation
6. customThe residue is purified chromatographically