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

โœ Scribed by Martin R Tremblay; Donald Poirier

Publisher
Elsevier Science
Year
1999
Tongue
French
Weight
255 KB
Volume
40
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

The 16p-(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.

๐Ÿ“œ SIMILAR VOLUMES

Solid-phase synthesis of small molecule
Solid-phase synthesis of small molecule libraries using double combinatorial chemistry
โœ John Nielsen; Flemming R. Jensen ๐Ÿ“‚ Article ๐Ÿ“… 1997 ๐Ÿ› Elsevier Science ๐ŸŒ French โš– 196 KB

The first synthesis of a combinatorial library using double combinatorial chemistry is presented. Coupling of unprotected Fmoc-tyrosine to the solid support was followed by Mitsunobu O-alkylation. Introduction of a diacid linker yields a system in which the double combinatorial step can be demonstra