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一锅法合成普拉格雷

DOI: 10.3969/j.issn.1671-7627.2010.05.017, PP. 77-81

Keywords: 普拉格雷,制备工艺,一锅法

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Abstract:

研究优化了普拉格雷(化合物1)的制备工艺,以4,5,6,7四氢噻吩并[3,2c]吡啶盐酸盐为原料通过氨基的三苯基保护、噻吩环的氧化、脱三苯基保护成盐得到2氧2,4,5,6,7,7a六氢噻吩并[3,2c]吡啶盐酸盐(化合物2),以环丙基2氟苄基酮为原料溴代得到α环丙基羰基2氟苄基溴(化合物3),化合物2与化合物3在碱性条件下发生亲核取代反应后,不经后处理直接进行乙酰化,一锅法得到普拉格雷,收率60%(以化合物2计),高于文献收率(30%),化合物通过质谱(msesi),氢谱(1hnmr)确证.

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