Tetrahedron

Regioselective hydroaminomethylation of 1, 1-diaryl-allyl-alcohols: a new access to 4, 4-diarylbutylamines

A Schmidt, M Marchetti, P Eilbracht

Index: Schmidt, Andreas; Marchetti, Mauro; Eilbracht, Peter Tetrahedron, 2004 , vol. 60, # 50 p. 11487 - 11492

Full Text: HTML

Citation Number: 19

Abstract

Pharmacologically active 4, 4-diarylbutylamines like Fluspirilene and 4-amino-1, 1- diarylbutan-1-ols like Difenidol were prepared in high yields via rhodium catalysed hydroaminomethylation of 1, 1-diaryl-allylalcohols. Conversion of these olefins with carbon monoxide, hydrogen and secondary amines proceeds with complete regioselectivity. This group can easily be removed under acidic and hydrogenating conditions, enabling the ...