AN IMPROVED PROCESS FOR THE PREPARATION OF 4-[2-(DI-N-PROPYLAMINO)ETHYL]-1,3-DIHYDRO-2H-INDOL-2-ONE

摘要

PURPOSE: A novel method for preparing 4-[2-(di-N-propylaminoe)ethyl]-1,3-dihydro-2H-indole-2-one is provided to manufacture a target compound in improved yeild and high yield. CONSTITUTION: A method for preparing 4-[2-(di-N-propylaminoe)ethyl]-1,3-dihydro-2H-indole-2-one comprises a step of reducing 2-methyl-3-nitrophenyl-N,N-di-n-propylacetide(III) by alkali metal borohydride under the presence of iodine to obtain 2-methyl-3-nitrophe-N,N-di-n-propylamine(Ropinirole). 2-(2-(2-di-propylamino-ethyl)-6-nitrophenyl)ethanol or salt compound thereof is obtained by reacting 2-methyl-3-nitrophenylethyl-N,N-di-n-propylamine with paraformaldehyde.