PROCESS FOR PREPARATION OF TADALAFIL

Process for the preparation of tadalafil of high pharmaceutical purity is characterized in that the sequence of reactions comprising acetylation of methyl (1R,3R)-1-(1,3-benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate with chloro acetyl chloride and cyclisation of the forme...

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Bibliographic Details
Main Authors KACZMAREK, LUKASZ, PYC, PAWEL, BADOWSKA-ROSLONEK, KATARZYNA
Format Patent
LanguageEnglish
French
German
Published 23.03.2011
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:Process for the preparation of tadalafil of high pharmaceutical purity is characterized in that the sequence of reactions comprising acetylation of methyl (1R,3R)-1-(1,3-benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate with chloro acetyl chloride and cyclisation of the formed intermediate with methyl amine, is performed as a 'one-pot' process, without isolating the intermediate methyl (1R,3R)-1-(1,3-benzodioxol-5-yl)-2-(chloroacetyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate.
Bibliography:Application Number: EP20090758588