The Synthesis Of Perindopril Eburmine And Para Selective Oxychlorination Of Toluene With Metal Chlorides And Oxidants

Part1The Synthesis of Perindopril EburminePerindopril, a non-thiohydroxy ACE inhibitor, is used for the treatment of hyperpiesia and congestive heart failure with high activity, less side-effect and better tolerance. The purpose of our present work is to discover a practical synthesis of perindopril. Perindopril eburmine was prepared from N-[(S)-1-carbethoxybutyl]-(S)-alanine and (2S,3aS,7aS)-octahydroindole-2-carboxylic acid, via protecting amine, acyl chlorination, amidation, forming salt. The product was confirmed by1H NMR and13C NMR, the purity was determined by HPLC. The synthesis process was simple、lower cost、 higher purity and suitable to industrial production.Part2Para Selective Oxychlorination of Toluene with Metal Chlorides and OxidantsIn the present work, we studied the preparation of para-chlorotoluene by using indirect oxychlorination of toluene. Oxone-LiCl system was found to be more selectivity for chlorination of toluene comparing with other oxychlorination system and conventional chlorine gas chlorination. The influence of various parameters, such as solvents, reaction temperature, reaction time, and Oxone/toluene mole ratio on the oxychlorination of toluene were investigated. A higher para-selectivity(75%) was obtained by using Oxone-LiCl system under optimized conditions.