Processes for preparing morphinans and intermediates thereof

Details Processes for preparing morphinans and intermediates thereof Processes for preparing morphinans and intermediates thereof

C - Chemistry, Metallurgy

07

D

C07D 221/28 (2006.01) C07D 217/20 (2006.01) C07D 489/02 (2006.01) C07D 491/10 (2006.01)

Patent

CA 2600687

The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ~,.gamma.-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ~,.gamma.- bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting a,~-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ~,.gamma.- bicyclic ketone compounds, wherein the ~,.gamma.-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.

L'invention se rapporte à des procédés de synthèse de morphinanes, plus précisément à un procédé de cyclisation d'un composés de cétone ß,?-bicyclique afin de former un produit de nordihydrothebainone au moyen de la réaction de cyclisation de Grewe, lequel est amélioré par formation d'un mélange de réaction contenant un composé de cétone ß,?-bicyclique, un acide de cyclisation et un adjuvant de cyclisation de balayage d'eau. Dans un mode de réalisation, la transformation de Grewe se produit en présence d'un anhydride acide en tant qu'adjuvant de cyclisation. De plus, cette invention porte sur des procédés de conversion de composés de cétone ß-bicyclique (par exemple des sous-produits de la réaction de cyclisation de Grewe) en composés de cétone ß,?-bicyclique, les composés de cétone ß,?-bicyclique peuvent être récupérés afin de se soumettre à une cyclisation de Grewe et former le produit de nordihydrothebainone.

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