Stereoselective reaction for hexahydro-6-arylpyrrolo(2,1-A) isoquinolines

摘要

A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): <IMAGE> +TR <IMAGE> whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuration (II) over the cis configuration (III) as defined in the following formulae: <IMAGE> The preferred reaction conditions include use of a borane complex as the reducing agent and an acidic solvent such as trifluoroacetic acid.