Synthesis of acrivastine
SHI Jing-bo
LI Rong
PENG Lei
LU Wei-li
Abstract：Objective:To synthesize the antihistamine drug aerivastine. Methods:Started from 2,6-dibro-mopyridine, acrivastine was synthesized by acylation reaction, HECK reaction to obtain (E)-3-[6-(4-Methyl-benzo-yl)-pyridin-2-yl]-acrylic acid ethyl ester, which was reacted by Wittig condensation affords a cis: trans mixture of (E)-6-[3-(1-Pyrrolidinyl)-1-p-tolyl-propenyl]-2-pyridin-eacrylic acid ethyl ester; then treated with acid, hydrol-ization and recrystallization. Results and Conclusion: The total yield of aerivastine was over 17%. The new process has the advantages,including short reaction period, mild reaction condition,with a good prospect for industrial appli-cation.
Keywords：acrivastinehistamine H_1 antagonistssynthesis
Publication Date：2009-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：3( 2176-2178 )