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Study On The Synthesis Of Aprepitant

Posted on:2015-01-29Degree:MasterType:Thesis
Country:ChinaCandidate:M Y YuanFull Text:PDF
GTID:2251330425984694Subject:Pharmaceutical Engineering
Abstract/Summary:PDF Full Text Request
In this paper, Aprepitant was prepared in14steps of reactions (10steps for main route and4steps for side chains) with R-(+)-a-methyl-phenethylamine as starting material. Preliminary optimization on the process was carried out. The structure of final API was identified and characterized.The reported synthetic routes of Aprepitant were summarized and analyzed. Based on the availability and cost of raw materials as well as feasibility of chemical synthesis, the route was studied using R-(+)-a-methyl-phenethylamine as starting material and also chiral auxiliary reagent. Crude Aprepitant could be prepared by some chemical procedure such as amide formation, amide reduction, cyclization, chiral inductive reduction and ether formation, etc. The quality of the final product can meet API specification after crude product was recrystallized. Optimization on the whole process were carried out, especially the amide reduction, ether formation and later elimination. The yield and cost were significantly improved. In addition, the asymmetric reduction for the preparation of chiral alcohol side chain was also investigated. The overall yield was about12%. The process is suitable for lab preparation and industrial production.
Keywords/Search Tags:Aprepitant, route summary, synthesis, process optimization, Industrialproduction
PDF Full Text Request
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