Abstract: The present invention provides a process for the asymmetric synthesis of camptothecin analogues as well as novel chemical intermediates of Formula I, II, and III. In general, the present process comprises conversion of a cis dioxolanone, having the same desired absolute configuration as the desired camptothecin analogue, to a compound of Formula I, II, or III, which compound is then converted to the desired camptothecin analogue.
Type:
Grant
Filed:
June 10, 1993
Date of Patent:
April 11, 1995
Assignee:
SmithKline Beecham Corporation
Inventors:
Joseph Fortunak, John Kitteringham, Nicholas Sisti, Jeffery Wood
Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR.sub.1 where R.sub.1 is hydrogen or lower alkyl; n is 0-5; R is H or lower alkyl and A is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.2 or a ketal derivative thereof where R.sub.2 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt.
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