Abstract: This invention relates to a process of making a compound of formula I ##STR1## where R.sub.1 contains an .alpha.,.beta.-unsaturated carbonyl group & R.sub.n is hydrogen or nonhydrogen radicals which do not have a functional group which interferes with the coupling reaction, which process comprises coupling a thiolphenol or phenylalkylmercaptan with a chloromethylpyridine in the presence of DBU under an inert atmosphere. These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.
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