Patent Number: 6,252,079

Title: Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof

Abstract: The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursor ##STR1## is reacted with an aryl isonitrile having the formula ##STR2## wherein X is Br or I, and R.sup.4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R.sup.16 is H, a C.sub.1 -C.sub.6 alkoxy group, a ##STR3## group wherein p is an integer between 4 and 12, or a C.sub.1 -C.sub.12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Inventors: Curran; Dennis P. (Pittsburgh, PA), Bom; David (Pittsburgh, PA)

Assignee: University of Pittsburgh

International Classification: C07F 7/08 (20060101); C07D 471/00 (20060101); C07F 7/00 (20060101); C07D 471/14 (20060101); C07D 491/22 (20060101); C07D 491/00 (20060101); C07D 487/22 (); C07D 211/46 (); C07D 295/205 (); C07D 401/04 ()

Expiration Date: 06/26/2018