【摘要】 以邻氟苄溴为原料,经格氏缩合、溴代反应得中间体α-环丙羰基-2-氟苄溴(3)。3与2-氧代-2,4,5,6,7,7a-六氢噻吩并[3,2-c]吡啶盐酸盐进行缩合,再经乙酰化反应,得目标产物普拉格雷(1)。对反应物配比、催化剂用量、反应温度、反应时间等因素进行了优化研究。该合成工艺反应条件温和、易控制、后处理简单,产物总收率可达30.9%,其结构经~1H NMR和MS确证。更多还原

【Abstract】 Fluorobenzyl bromide was used as the starting material to generate 3 via Grignard reaction and bromination reaction. Compound 3 was treated with 2-oxo-2,4,5,6,7,7a-hexahydrothieno [3,2-c]pyridine hydrochloride through condensation, acetylation reaction to give the target compound 1. The target compund 1 was obtained with an overall yield of 30.9%. Reaction conditions including the ratio of the raw materials, the amount of catalyst, reaction time were evaluated to make the reaction conditions mild and easy to control with less side effects. The structure of compound 1 was confirmed by IR,~1H NMR and MS.更多还原