"processo aprimorado de preparação de composto farmacêtico"

"processo aprimorado de preparação de composto farmacêtico"

The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-brom...

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Hauptverfasser: KALMÁN NAGY, BALÁZS VOLK, JOZSEF BARKÓCZY, ENIKÖ MOLNÁR, ERIKA SZILÁGYI, GYORGY RUZSICS, GÁBOR NÉMETH, ANGÉLA PANDUR, MÁRTA MAKKAY, TIBOR MEZEI, TAMÁS GREGOR, PÉRTE SLÉGEL, BÁLINT NYULASI, JOZSEF DE BRECZENI
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Sprache:por
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator KALMÁN NAGY
BALÁZS VOLK
JOZSEF BARKÓCZY
ENIKÖ MOLNÁR
ERIKA SZILÁGYI
GYORGY RUZSICS
GÁBOR NÉMETH
ANGÉLA PANDUR
MÁRTA MAKKAY
TIBOR MEZEI
TAMÁS GREGOR
PÉRTE SLÉGEL
BÁLINT NYULASI
JOZSEF DE BRECZENI
description The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-1-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents.
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The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. 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The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title "processo aprimorado de preparação de composto farmacêtico"
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