Patent ID: 7910737
Filing Date: 2011-03-22
Classification: C07D

Abstract:
1. A process for the preparation of 7-ethyl-10-hydroxy-camptothecin comprising the steps: a) charging a reaction vessel with a reaction mixture comprising (4S)-4-ethyl-7,8-dihydro-4-hydroxy-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione, 1-(2-amino-5-hydroxyphenyl)-propan-1-one, a catalyst and a reaction solvent, b) heating the reaction mixture to a reaction temperature greater than 100° C., wherein said heating is accomplished in less than 45 minutes, c) allowing the reaction to complete in said reaction mixture, d) adding a crystallization solvent to said reaction mixture to crystallize said 7-ethyl-10-hydroxy-camptothecin, and e) isolating the crystalline product from said reaction mixture which has said crystallization solvent added thereto.