NOVEL INTERMEDIATE AND PROCESSES FOR ITS PREPARATION AND CONVERSION INTO A PHARMACOLOGICALLY-ACTIVE AGENT

Processes for the preparation of Venlafaxine (IX) via the novel epoxy- nitrile intermediate (I), which when subjected to hydrogenation forms compound (X), and may subsequently be reduced to yield the desired product (IX). The epoxy-nitrile intermediate (I) itself may be synthesised via vario us alte...

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Bibliographic Details
Main Authors GHARPURE, MILIND MORESHWAR, PATEL, NISHANT MAHENDRA, RENGARAJU, SRINIVASAN, DEOAHAR, MANDAR MANOHAR, RATHOD, DHIRAJ MOHANSINH
Format Patent
LanguageEnglish
French
Published 10.10.2002
Edition7
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:Processes for the preparation of Venlafaxine (IX) via the novel epoxy- nitrile intermediate (I), which when subjected to hydrogenation forms compound (X), and may subsequently be reduced to yield the desired product (IX). The epoxy-nitrile intermediate (I) itself may be synthesised via vario us alternative reaction strategies, from a range of starting materials. E.g. 4- methoxy-benzaldehyde (VI), upon treatment with cyclohexyl magnesium bromide yields compound (V). This in turn may be oxidised to yield compound (III), which forms compound (II) on treatment with an .alpha.-keto- halogenation agent. Cyanation of compound (II), then yields the desired epoxy nitrile intermediate (I), from which Venlafaxine (IX) may be synthesised.
Bibliography:Application Number: CA20022381334