NEW PRODUCTION OF NICARDIPINE HYDROCHLORIDE AND NEW SYNTHETIC INTERMEDIATE

PURPOSE: To obtain the subject compound useful as an antihypertensive, an anticonvulsant, etc., in a high purity and in a good yield by reacting a specific methyl acetoacetate derivative with β-amino-crotonate ester and subsequently reacting the obtained compound with an acid catalyst. CONSTITUTION:...

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Hauptverfasser:	TOKUNAGA TATSUHIRO, FUJIMOTO MASAHARU, YOKOI TAKAKO
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	PURPOSE: To obtain the subject compound useful as an antihypertensive, an anticonvulsant, etc., in a high purity and in a good yield by reacting a specific methyl acetoacetate derivative with β-amino-crotonate ester and subsequently reacting the obtained compound with an acid catalyst. CONSTITUTION: (A) Highly pure methyl 2-(3'-nitrobenzylidene)acetoacetate ester not containing an acid as an impurity is reacted with (B) β-(N-benzyl-N- methylamino)ethyl K&B-amino-crotonate ester, and the obtained 2-hydroxy-2,6- dimethyl-4-(m-nitrophenyl)1,2,3,4-tetrahydropyridine-3,5-dicarboxylic acid 5-[2-(N- benzyl-N-methylamino)ethyl] ester 3-methyl ester is reacted with an acid catalyst to obtain the objective compound.