Preparation of trans-fused...

C - Chemistry – Metallurgy – 07 – D

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C07D 307/93 (2006.01) A61K 31/34 (2006.01)

Patent

CA 2468038

The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I): in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans- fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.

La présente invention concerne des procédés de préparation de chacun des 4 diastéréomères représentés par la formule (I) sous forme stéréochimiquement pure à partir d'un de deux précurseurs enantiomériquement purs. Le système à noyau tétracyclique présentant des noyaux à cinq et sept chaînons à fusion trans est formé dans une réaction de cyclisation par catalyse acide. L'invention concerne également les intermédiaires d'alcool tétracycliques à fusion cis ainsi obtenus, les produits finaux de méthanamine, les produits finaux de méthanamine utilisés en tant que médicaments, en particulier en tant que médicaments actifs associés au SNC.

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