反应详情

N-(2-(3,3-Difluoropyrrolidin-1-yl)-3-fluorobenzylidene)-3,3-dimethylbutan-1-amine (400.2 mg, 1.281 mmol) was taken in toluene and (S)-2-mercaptosuccinic acid (192.3 mg, 1.281 mmol) was added. The reaction mixture was refluxed overnight with a Dean Stark trap to remove the water. Then the reaction mixture was concentrated, triturated with ether and dried overnight to give 2-((5S)-2-(3-fluoro-2-(3,3-difluoropyrrolidin-1-yl)phenyl)-3-(3,3-dimethylbutyl)-4-oxothiazolidin-5-yl)acetic acid which was used directly in the next step. The product was identified by LC/MS. LC/MS: m/z=445.5M+1.

1. temperatureThe reaction mixture was refluxed overnight with a Dean Stark trap
2. customto remove the water
3. concentrationThen the reaction mixture was concentrated
4. customtriturated with ether
5. customdried overnight