Societe De Conseils De Recherches Et D'applications Scientifiques

Societe De Conseils De Recherches Et D'applications Scientifiques (s.c.r.a.s.)

Charles Eck

Andre Esanu

Marc Bonato

Separation of isomers of furo (3,4-C) pyridine derivatives

The invention relates to a method for the preparation of a non-racemic furo [3,4-c] pyridine derivatives of the formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 stand for various substitutents, comprising adding a concentrated strong acid to a solution of a non-racemic compound of the formula II ##STR2## in an amount sufficient to catalyze a deprotection/cyclodehydration. These compounds are known antihypertensives.

Asymmetric synthesis of furo(3,4-c) pyridine derivatives

The present invention relates to stereospecific processes for the preparation of enantiomers of 3-substituted-furo[3,4-c]pyridine of formula I, wherein R.sub.3, R.sub.4 and R.sub.6 stand for various substituents, comprising the steps of: oxidation of a racemic pyridine derivative of formula II, reduction of the resulting ketone with a reducing agent, sterospecific locking or blocking of the OH group of the enantiomer alcohol, opening of the acetonide ring and cyclization of the resulting compound. ##STR1##

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Shrewsbury, MA, United States of America

Charles Eck