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1. (WO1996002564) PROCESS FOR THE PREPARATION OF COMPOUNDS HAVING ACE INHIBITORY ACTION AS WELL AS NOVEL COMPOUNDS USEFUL AS STARTING MATERIALS OR INTERMEDIATES IN SAID PROCESS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1996/002564    International Application No.:    PCT/SI1995/000017
Publication Date: 01.02.1996 International Filing Date: 13.07.1995
IPC:
C07D 521/00 (2006.01), C07K 5/02 (2006.01)
Applicants: LEK, TOVARNA FARMACEVTSKIH IN KEMICNIH IZDELKOV, D.D. [SI/SI]; Ul. Verovs^¿kova 57, 61107 Ljubljana (SI) (For All Designated States Except US).
SERRA MORTES, Sonia [ES/ES]; (ES) (For US Only).
PALOMO COLL, Alberto [ES/ES]; (ES) (For US Only).
ZUPET, Rok [SI/SI]; (SI) (For US Only)
Inventors: SERRA MORTES, Sonia; (ES).
PALOMO COLL, Alberto; (ES).
ZUPET, Rok; (SI)
Agent: PATENTNA PISARNA D.O.O.; C^¿opova 14, P.O. Box 322, 61000 Ljubljana (SI)
Priority Data:
P-9400290 13.07.1994 SI
P-9400450 21.12.1994 SI
Title (EN) PROCESS FOR THE PREPARATION OF COMPOUNDS HAVING ACE INHIBITORY ACTION AS WELL AS NOVEL COMPOUNDS USEFUL AS STARTING MATERIALS OR INTERMEDIATES IN SAID PROCESS
(FR) PROCEDE DE PREPARATION DE COMPOSES A ACTIVITE INHIBITRICE D'ACE ET NOUVEAUX COMPOSES UTILES EN TANT QUE PRODUITS DE DEPART OU INTERMEDIAIRES DANS LEDIT PROCEDE
Abstract: front page image
(EN)There is disclosed a process for the preparation of compounds having ACE inhibitory action of formula (1) wherein R has the meanings as in claim 1, wherein the stereospecific amino acid N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine is carboxylically activated with a thionyl chloride derivative wherein at least one chlorine atom is replaced by the residue of a heterocylic ambident compound such as imidazole, benzimidazole, 2-methylimidazole or triazole, especially chlorothionylimidazole or thionyldiimidazole, in the presence of an organic solvent to the intermediate novel compound A or to the intermediate novel compound B and the obtained intermediate compound is reacted with an amino acid, preferably in the monosilylated form, most preferably in the disilylated form. Disclosed are also novel compounds useful as starting materials or intermediates in the present process.
(FR)Procédé de préparation de composés à activité inhibitrice d'ACE de formule (1) où R est défini dans la revendication 1, où l'acide aminé stéréospécifique N-[1-(S)-éthoxycarbonyl-3-phénylpropyl]-L-alanine est activé au niveau de son groupe carboxyle par un dérivé du chlorure de thionyle où au moins un atome de chlore est remplacé par le reste d'un composé hétérocyclique ambident tel que l'imidazole, le benzimidazole, le 2-méthylimidazole ou le triazole, et en particulier tel que le chlorothionylimidazole ou le thionyldiimidazole en présence d'un solvant organique des nouveaux composés intermédiaires A et B, on fait ensuite réagir le composé intermédiaire obtenu avec un acide aminé, de préférence de la forme monosilylée ou mieux de la forme disilylée. Sont également présentés de nouveaux composés servant de produits de départs ou d'intermédiaires dans le procédé susdit.
Designated States: AM, AU, BB, BG, BR, BY, CA, CN, CZ, EE, FI, GE, HU, IS, JP, KG, KP, KR, KZ, LK, LR, LT, LV, MD, MG, MN, MX, NO, NZ, PL, RO, RU, SG, SK, TJ, TM, TT, UA, US, UZ, VN.
African Regional Intellectual Property Organization (KE, MW, SD, SZ, UG)
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)