AN IMPROVED PROCESS FOR THE MANUFACTURE OF ISRADIPINE

The present invention relates to an improved method for the manufacture of Isradipine, 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester. which, involves reacting 2,1,3-benzoxadiazole-4-carboxaldehyde with methyl acetoacetate in the presence of ac...

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Hauptverfasser: MULLAIYUR, RADHAKRISHNAN, SELVARAJU, SENTHIL, KUMAR, MINOR, THAKASHINAMOORTHY, CHANDIRAN, PALANIVEL, KALIYAPERUMAL
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creator MULLAIYUR, RADHAKRISHNAN, SELVARAJU
SENTHIL, KUMAR, MINOR
THAKASHINAMOORTHY, CHANDIRAN
PALANIVEL, KALIYAPERUMAL
description The present invention relates to an improved method for the manufacture of Isradipine, 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester. which, involves reacting 2,1,3-benzoxadiazole-4-carboxaldehyde with methyl acetoacetate in the presence of acetic acid and piperidine in diisopropyl ether. To obtain the product 2-acetyl-3-benzofurazan-4-yl-acrylic acid methyl ester which is then reacted with isopropyl-ß-aminocrotonate in ethanol at 25 to 35°C to obtain the product. La présente invention concerne un procédé amélioré de fabrication d'Isradipine, ester de méthyle 1-méthylethyle d'acide 4-(4-benzofurazanyl)-1,4-dihydro-2,6-diméthyl-3,5-pyridinedicarboxylique. Elle consiste à faire réagir 2,1,3-benzoxadiazole-4-carboxaldéhyde avec un acétoacétate de méthyl en présence d'acide acétique et de pipéridine dans un éther diisopropylique. Pour obtenir le produit, on utilise l'ester de méthyle d'acide 2-acétyl-3-benzofurazan-4-yl-acrylique, qu'on fait ensuite réagir avec isopropyl-ss-aminocrotonate dans de l'éthanol à 25 - 35 DEG C.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title AN IMPROVED PROCESS FOR THE MANUFACTURE OF ISRADIPINE
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