Patent ID: 6194579
Filing Date: 2001-02-27
Classification: A61P,C07D,Y02P

Abstract:
A process for synthesizing a Camptothecin derivative having the formula: ##STR7##wherein R.sub.1 is C.sub.2 -C.sub.8 alkenyl or C.sub.2 -C.sub.8 alkynyl optionally substituted by one or more halogen atoms or OR.sub.4 or lower alkyl for a corresponding hydrogen atom therein; halo; oxo; --X--C.sub.6 -C.sub.14 aryl optionally substituted by one or more halogen atoms; --X--aryl--lower alkyl; --X--aryl--lower alkenyl; --X--aryl--lower alkynyl; heterocycle; SR.sub.5 ; --S(O)--lower alkyl; --OSO.sub.2 CF.sub.3 ; --lower alkylene--P(O)R.sub.6 R.sub.7 ; or --X--(C.sub.0 -C.sub.6 alkylene, alkenylene, or alkynylene)--SiR.sub.8 R.sub.9 R.sub.10 ;R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are each individually hydrogen or lower alkyl;R.sub.11 is hydrogen, hydroxy, acetoxy or acyloxy; andX is sulfur or X is absent; said process comprising the steps of:(a) providing a quantity of 7-keto Camptothecin;(b) selectively substituting a leaving group at the C7 carbon of the 7-keto Camptothecin; and(c) selectively derivatizing the C7 carbon to produce the formula I compound.