Citation:
WU Xiao-Yun, HU Ai-Xi, TAN Ying. Synthesis Improvement of Calcium Antagonist Pranidipine[J]. Chinese Journal of Applied Chemistry,
;2003, 20(10): 1015-1017.
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The reaction of diketene and cinnamyl alcohol gave cinnamyl acetoacetate. Cinnamyl acetoacetate was ammoniatzed to give cinnamyl 3-aminocrotonate. Methyl acetoacetate condensed with 3-nitrobenzaldehyde to form methyl 2-(3-nitrobenzylidene)acetoacetate which then via. Hantzsch cyclization with cinnamyl 3-aminocrotonate produced new calcicum antagonist pranidipine under mild conditions. The total yield was 69% based on cinnamyl alcohol. Pranidipine synthesized has been characterized by IR、1H NMR、13C NMR and MS spectral measurements.
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Keywords:
- pranidipine,
- synthesis,
- diketene,
- Hantzsch cyclization
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