반응 #2010696

반응 방정식

ammonium hydroxide

2-[2-(5-methyl-3-pyridin-2-yl-isoxazol-4-yl)-ethyl]-thiazole-5-carboxylic acid

1,1′-carbonyldiimidazole

→

title compound

수율 70.5%

2-[2-(5-Methyl-3-pyridin-2-yl-isoxazol-4-yl)-ethyl]-thiazole-5-carboxylic acid amide

수율 70.5%

용매

DMF

반응 조건

후처리

1. 1
   기타The resulting reaction mixture
2. 2
   workup.STIRRINGstirred overnight at room temperature
3. 3
   기타The reaction mixture was then evaporated
4. 4
   기타Purification by chromatography (silica, 0 to 10% methanol in dichloromethane)

실험 절차

To a solution of 2-[2-(5-methyl-3-pyridin-2-yl-isoxazol-4-yl)-ethyl]-thiazole-5-carboxylic acid (73 mg, 0.23 mmol) in DMF (3 mL) was added 1,1′-carbonyldiimidazole (45 mg, 0.28 mmol). The resulting reaction mixture was stirred for 1 h at 60° C. and then treated with an ammonium hydroxide solution (357 μL, 2.3 mmol) and stirred overnight at room temperature. The reaction mixture was then evaporated. Purification by chromatography (silica, 0 to 10% methanol in dichloromethane) afforded the title compound (51 mg, 70%) as an off white solid. MS: m/e=315.0 [M+H]+.

출처