PROCESS FOR PREPARING 3-AMINO-(1)BENZAZEPIN-2-ONE-1-ALKANOIC ACIDS

PROCESS FOR PREPARING 3-AMINO-(1)BENZAZEPIN-2-ONE-1-ALKANOIC ACIDS

The title cpds. of formula (I) or their stereoisomers or salts are prepd. by alkylating (II) with RA-Z or R1-CO-Ro in the presence of reductant. Pri. and sec. amine (may exist in one of substits. X, RA, RB, R1, R3, R4 and R5), hydroxyl and oxo gp. are temporarily protected while alkylation is perfor...

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Bibliographische Detailangaben
1. Verfasser: WATTHEY, JEFFREY W.H
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Zusammenfassung:The title cpds. of formula (I) or their stereoisomers or salts are prepd. by alkylating (II) with RA-Z or R1-CO-Ro in the presence of reductant. Pri. and sec. amine (may exist in one of substits. X, RA, RB, R1, R3, R4 and R5), hydroxyl and oxo gp. are temporarily protected while alkylation is performed. In the formulas, RA=- CHR1R0, R0=COR6; RB=-CHR2R0, R0=COR7=OH or lower alkoxy; R1, R2 and R5=H or lower alkyl; R3 and R4=H, lower alkyl, OH or halo; X=oxo, two H or H/OH. (I) is useful as an inhibitor for angiotensin conversion enzyme.