Tetrahedron letters

Solid-phase synthesis of phenolic steroids: towards combinatorial libraries of estradiol derivatives

MR Tremblay, D Poirier

Index: Tremblay, Martin R.; Poirier, Donald Tetrahedron Letters, 1999 , vol. 40, # 7 p. 1277 - 1280

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Citation Number: 21

Abstract

The 16β-(azidopropyl) derivative of estradiol (7) was synthesized and coupled to aminomethyl resin via a photolabile o-nitrobenzyl linker. Condensation of the corresponding iminophosphorane with activated acids successfully gave amides. Photocleavage resulted in good yield recovery of estradiol derivatives 15 and 16 in acceptable purities for biological screening.