University of Pittsburgh

University of Kentucky Research Foundation

Wu Du

Dennis Patrick Curran

Thomas G Burke, Deceased

Lori Latus, Legal Representative

The present invention relates to novel intermediates and prodrugs of camptothecin and related analogs.

Camptothecin intermediates and prodrugs and methods of preparation thereof

The present invention relates to novel, highly lipophilic silatecan intermediates and prodrugs of DB-67 and other silatecans.

Highly lipophilic camptothecin intermediates and prodrugs and methods of preparation thereof

A method of synthesizing 7-silyl camptothecins and 7-silyl homocamptothecins includes the step of mixing a camptothecin or a homocamptothecin having hydrogen at the C7 position with a silyl radical generator and a silyl radical precursor under conditions to generate a silyl radical. SiR R R wherein R , R and R are independently a C alkyl group, a C alkenyl group, a C alkynyl group, an aryl group, &mdash;(CH ) R or SiR R R , wherein m is an integer within the range of 1 through 10 and R is a hydroxy group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, F, Cl, a cyano group, &mdash;SR or a nitro group, and wherein R , R and R are independently the same or different an alkyl group or an aryl group.

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Wu Du