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US 5,516,910 AGranted
N--2--chlorobenzyl--2--oxo and n--2--chlorobenzyl--2,2--dioxo--1,2,3--oxathiazolidine derivatives, their preparation and synthesis of thieno[3,2--c]pyridine derivatives therefrom
AssigneeSyntex (U.S.A.) Inc.
InventorsGary F. Cooper, Keith E. McCarthy
Life of this patent
Estimating the term…
Abstract
Compounds of the formula: ##STR1## wherein: A is oxo or dioxo; R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl of one to six carbon atoms; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo; are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
Claims11
A process for preparing a compound of the formula:
- ##STR8## wherein:
- R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl;
- and
- R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, acyl, or halo;
- said process comprising:
- a) contacting a compound of the formula:
- ##STR9## wherein A is dioxo, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined above;
- with thienyllithium, to give an intermediate compound of the formula:
- ##STR10## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined above;
- followed by:
- b) contacting said intermediate compound with formaldehyde or a formaldehyde equivalent.
8 more elements
Dependencies are inferred from the claim text.