DHPCOOH的合成改进

Improved Synthesis of DHPCOOH

盐酸乐卡地平(Lercanidipinehydrochloride)为第三代1,4—二氢比啶类血管选择性L—型钙通道阻断药,本文对母核DHPCOOH合成进行改进,选择对称酯水解法,用价格便宜相转移催化剂三乙胺(TEA)代替价格较贵四丁基溴化胺,并考察了三乙胺用量和氢氧化钠浓度等因素的影响。粗品收率为76%,用甲醇精制收率80%,含量98%(HPLC)。

Lercanidipine was the third 1,4-dihydropyridines blood vessel selective L-calcium channel blocks drug.The synthesis of the mother DHPCOOH was improved,selecting symetry ester hydrol-sis,using lower price of phase turn catalyst TEA to take place higher price of TBAB,and inspecting the effects of amount of and sodium hydroxide concentration and other factors.The crude yield was 76%,purify with methanol was 80%,and content was 98%（HPLC）.