Abstract

A facile procedure for the preparation of the imine form of the pyrrolo[2,1- c][1,4]-benzodiazepine ring system by the oxidation of cyclic secondary amine with catalytic amounts of tetra-n-propylammonium perruthenate (TPAP) and N-methylmorpholine N-oxide (NMO) as a co-oxidant is described. This oxidative method is devoid of side-products and is thus a significant improvement over the Swern oxidation previously reported.

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