L. Tao
2012
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Journal
Strait Pharmaceutical Journal
Abstract
OBJECTIVE To adapt to the industrialized production,we improved the process for synthesizing Perindopril erbumine.METHODS Using(2S,3aS,7aS)-octahydroindole-2-carboxylic acid and N-((S)-1-carbethoxy-1-butyl)-(S)-alanine as the raw materials,Perindopril erbumine was synthesized via condensation,catalytic hydrogenation and salification reactions.RESULTS The structure of the product was characterized by IR,H-NMR and MS.Compared with the reported method,the reaction time was shortened,the total yield was increased by 16% and the product purity was increased from 94.26% to 99.51% in the improved synthetic process.CONCLUSION The synthetic process is optimized with simple operation and low cost.The purities are qualified and this method can be applied to industrial manufacture.