Preparation of cis-fused...

Details Preparation of cis-fused... Preparation of cis-fused...

C - Chemistry, Metallurgy

07

D

C07D 307/93 (2006.01) A61K 31/34 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2468040

The present invention concerns a process for preparing each of the 4 individual diastereomers of formula (I) in stereochemically pure form from a single enantiomerically pure precursor. The tetracyclic ringsystem having cis- fused five and seven membered rings is formed in a base-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates and methanamine end-products, and the methanamine end-products for use as a medicine, in particular as CNS active medicines.

L'invention concerne un procédé de préparation de chacun des 4 diastéréoisomères individuels de formule (I) dans une forme stéréochimiquement pure à partir d'un précurseur unique énantiomériquement pur. Le système tétracyclique, qui comporte des cycles à cinq et à sept membres fusionnés en cis, est obtenu au moyen d'une réaction de cyclisation à catalyse basique. L'invention concerne aussi les alcools tétracycliques fusionnés en cis intermédiaires et les méthanamines finaux, ainsi que l'utilisation de ces méthanamines en tant que médicaments actifs, en particulier du SNC.

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