Synthesis of (±) Combretastatin

Abstract

Combretastatin (1) is a new plant product isolated recently by Pettit et al ¹. from the South African tree, Combretum caffrum that possesses central nervous system antineoplastic activity and is being evaluated against several of National Cancer Institute's key evaluation systems. The structure of 1 was established on the basis of its spectral properties and confirmed by X-ray analysis. However, the absolute configuration and the synthesis of 1 have not been reported so far. As combretastatin is present in the plant in only 0.0008% and the isolation technique is much tedious, there is an urgent need for the synthesis of 1 for further evaluation of its activity. This prompted us t o report the first synthesis of (±)1.