| abstract |
The invention discloses 2-(alpha-hydroxypentyl)benzamide derivatives and a preparation method, preparation and application thereof. The 2-(α-hydroxypentyl) benzamide derivative has the following structural formula: Wherein: R1 is a linking group; R2 is a functional group containing a carboxyl group. The preparation method comprises the following steps: the ring-opening reaction of raw material butylphthalide to obtain the intermediate product a, and the condensation reaction with the compound containing carboxyl group to obtain the target product. The preparation is prepared by adding pharmaceutically acceptable auxiliary materials into powder, tablet, capsule, granule, drop pill, honeyed pill, freeze-dried preparation or water injection. The application is in the preparation of prevention/treatment of cardio-cerebral ischemic diseases, cardio-cerebral arterial obstructive diseases and anti-Parkinson's disease and anti-senile dementia drugs. The invention connects ring-opening butylphthalide with drugs with anti-platelet aggregation effects such as ozagrel or clopidogrel through amide bonds, and designs and synthesizes butylphthalide prodrugs with multiple pharmacological effects. |