普拉地平合成工艺研究

Study on Synthesis Process of Pranidipine

目的：合成新型二氢吡啶类钙拮抗药普拉地平。方法：以双乙烯酮、肉桂醇为原料，通过酯化得到乙酰乙酸肉桂醇酯（3），3与3-硝基苯甲醛缩舍得到3-（3-硝基苯基）之一氧代-3_-戊烯酸肉桂醇酯（2），再与3-氨基-2-丁烯酸甲酯环化得到普拉地平（1）。结果：反应总收率为66．8％。目标化合物的结构经IR、MS和^1H—NMR确证。结论：该工艺路线简单，反应试剂和原料价廉易得，操作方便，适合于工业化生产。

Objective： To synthesize novel dihydropyridine calcium antagonist the pranidipine （1）. Method： Diketene and cinnamyl alcohol as the starting material were transformed to cinnamyl acetoaeetate （3） via esterifieation. And 3 with 3-nitrobenzaldehyde was condensed to form 3-（ 3-nitrophenyl）- 2-oxo-pentanoic acid- cinnamyl ester （2）. 2 with 3-amino-2-butenoic acid methyl ester was cyelized to produce new calcium antagonist pranidipine. Result： The total yield was 66.8%. Pranidipine synthesized had eharaeterized by IR, ^1H-NMR, and MS spectral measurements. Conclusion ： This improved procedure has several advantages of low consumption, mild condition, convenient operation, and is suitable for industrial production.