Tetrahedron letters

New strategy for the synthesis of phosphatase inhibitors TMC-69-6H and analogs

N Brondel, B Renoux, JP Gesson

Index: Brondel, Nicolas; Renoux, Brigitte; Gesson, Jean-Pierre Tetrahedron Letters, 2006 , vol. 47, # 52 p. 9305 - 9308

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Citation Number: 11

Abstract

An efficient method for the synthesis of antitumor TMC-69-6H and related analogs which have been demonstrated to be phosphatase (PTP1B, VHR, and PP1) inhibitors, is reported. This strategy involves two key steps: a diastereoselective aldol reaction and a one-pot tandem ring-closing and cross metathesis for the construction of the pyran moiety.