摘要
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.
出处
《中国药师》
CAS
2009年第10期1370-1372,共3页
China Pharmacist
关键词
普拉地平
钙拮抗药
合成
Pranidipine
Calcium antagonist
Synthesis