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1. (WO1992010485) A PROCESS FOR THE PREPARATION OF DILTIAZEM
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/010485 International Application No.: PCT/EP1991/002353
Publication Date: 25.06.1992 International Filing Date: 09.12.1991
Chapter 2 Demand Filed: 17.06.1992
IPC:
C07D 281/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
281
Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
02
Seven-membered rings
04
having the hetero atoms in positions 1 and 4
08
condensed with carbocyclic rings or ring systems
10
condensed with one six-membered ring
Applicants:
LUSOCHIMICA S.P.A. [IT/IT]; Via Giotto, 1 I-22050 Lomagna, IT (AllExceptUS)
MANGHISI, Elso [IT/IT]; IT (UsOnly)
PEREGO, Bruno [IT/IT]; IT (UsOnly)
Inventors:
MANGHISI, Elso; IT
PEREGO, Bruno; IT
Agent:
BIANCHETTI, Giuseppe; Studio Consulenza Brevettuale Via Rossini, 8 I-20122 Milano, IT
Priority Data:
22340 A/9011.12.1990IT
Title (EN) A PROCESS FOR THE PREPARATION OF DILTIAZEM
(FR) PROCEDE DE PREPARATION DE DILTIAZEM
Abstract:
(EN) (+)-Cis-3-(acetoxy)-5-[2-(dimethylamino)-ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one hydrochloride is prepared by N-alkylation of (+)-cis-3-hydroxy-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one with dimethylaminoethyl chloride and K2CO3 in toluene/water, addition of a solubilizing agent and in the presence of a phase-transfer catalyst, the toluene phase being directly subjected to the final O- acetylation.
(FR) On prépare l'hydrochlorure de (+)-Cis-3-(acétoxy)-5-[2-(diméthylamino)-éthyl]-2,3-dihydro-2-(4-méthoxyphényl)-1,5-benzothiazepin-4(5H)-one par la N-alkylation du (+)-cis-3-hydroxy-2,3-dihydro-2-(4-méthoxyphényl)-1,5-benzothiazepin-4(5H)-one avec le chlorure de diméthylaminoéthyle et le K2CO3 dans le toluène et l'eau, et par l'addition d'un agent de solubilisation en présence d'un catalyseur à transfert de phase, la phase toluène étant directement soumise à la O-acétylation finale.
Designated States: AU, BB, BG, BR, CA, CS, FI, HU, JP, KP, KR, LK, MG, MN, MW, NO, PL, RO, SD, SU, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, MC, NL, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0561861US5382663JP3152658CA2098114AU1991090366