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

Authors
Tremblay, MR Poirier, D
Citation
Mr. Tremblay et D. Poirier, Solid-phase synthesis of phenolic steroids: Towards combinatorial libraries of estradiol derivatives, TETRAHEDR L, 40(7), 1999, pp. 1277-1280
Citations number
25
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON LETTERS
ISSN journal
00404039 → ACNP
Volume
40
Issue
7
Year of publication
1999
Pages
1277 - 1280
Database
ISI
SICI code
0040-4039(19990212)40:7<1277:SSOPST>2.0.ZU;2-M
Abstract
The 16 beta-(azidopropyl) derivative of estradiol (7) was synthesized and c oupled to aminomethyl resin via a photolabile o-nitrobenzyl linker. Condens ation of the corresponding iminophosphorane with activated acids successful ly gave amides. Photocleavage resulted in good yield recovery of estradiol derivatives 15 and 16 in acceptable purities for biological screening. (C) 1999 Elsevier Science Ltd. All rights reserved.