C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
260/284, 260/317
C07K 5/06 (2006.01) C07D 209/52 (2006.01) C07D 217/26 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1338162
The invention relates to a process for the pre- paration of compounds of the formula I Image (I) in which n is 1 or 2, R denotes hydrogen or an organic radical, R1 denotes an organic radical, R2 and R3 are identical or different and denote hydrogen or an organic radical, and R4 and R5, together with the atoms bearing them, form a monocyclic, bicyclic or tricyclic hetero- cyclic ring system having 5 to 15 carbon atoms, which process comprises reacting compounds of the formula II defined in the description with compounds of the formula III defined in the description, in the presence of alkane- phosphonic anhydrides, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se. The process provides for an economic synthesis of the compounds of the formula I. The compounds of the formula I are inhibitors of angiotensin converting enzyme or are intermediates in the preparation of inhibitors of this type, and they can be employed to control high blood pressure of a variety of etiologies.
463071
Henning Rainer
Teetz Volker
Urbach Hansjorg
Wissmann Hans
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Sanofi-Aventis Deutschland Gmbh
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