公开(公告)号：HRP20040490A2

公开(公告)日：2004-10-31

申请号：HRP20040490

申请日：2004-05-31

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： YOLANDE ,  BART ,  GEORGES ,  BROSSETTE THIERRY ,  MICHEL ,  MAO HUA ,  KOZLECKI TOMASZ

IPC: A61K31/34 ,  A61K31/343 ,  A61P25/06 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D307/93

Abstract: 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.