Ciba-geigy Corporation

Joseph Bach

Stephen K Boyer

Karl O Gelotte

Disclosed is a process for the preparation of a compound of the formula ##STR1## wherein Ar is 3- or 4-pyridyl or 3- or 4-pyridyl substituted by lower alkyl; R.sub.1 is hydrogen, halogen, trifluoromethyl, lower alkyl, hydroxy, acylated or etherified hydroxy, lower alkylthio; or two of R.sub.1 on adjacent carbon atoms represent alkylenedioxy; p is 1 or 2; R.sub.2 represents hydrogen or lower alkyl; E represents C.sub.1 -C.sub.11 alkylene, C.sub.1 -C.sub.6 alkylenephenylene, C.sub.1 -C.sub.6 alkylene-(thio or oxy)-lower alkylene, C.sub.1 -C.sub.6 alkylene-(thio or oxy)-phenylene, C.sub.1 -C.sub.6 alkylenephenylene-lower alkylene, phenylene-lower alkylene; or E represents a direct bond; and B represents carboxy, esterified carboxy or carbamoyl; which comprises deoxygenating the keto group in a compound of the formula ##STR2## wherein Ar, R.sub.1, R.sub.2, p, E and B have meaning as defined above.

3-keto-substituted-N-pyridylindoles

The invention concerns a novel process for the preparation of 3-(5-amino-1-carboxypentylamino)-tetrahydro-1-benzazepin-2-one-1-acetic acid by opening, preferably under acidic conditions, the caprolactam ring in a compound of formula II ##STR1## wherein COR represents carboxy or esterified carboxy, and hydrolyzing the esterified carboxy group if present. The preparation of the starting materials of formula II is described.

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Parsippany, NJ, United States of America

Joseph Bach