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Synthesis of 14C- and 14C3-labelled Org 37462

✍ Scribed by P. H. G. Wiegerinck; L. W. H. Hofstede; F. M. G. M. Sperling; J. F. Vader

Publisher: John Wiley and Sons
Year: 2008
Tongue: French
Weight: 237 KB
Volume: 51
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1499

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✦ Synopsis

Abstract

Org 37462 (1) is the active ingredient in Orgalutran^®^, an innovative product that reduces the time of treatment in in vitro fertilization from four to less than two weeks. Org 37462 is a synthetic decapeptide containing several amino acids that are unnatural in stereochemistry and/or in structure. The synthesis, starting with a ProtectingGroup‐D‐Ala‐resin, is a typical solid state synthesis. For the conduction of several metabolism studies, Org 37462 had to be labelled with carbon 14. It was decided to label D‐3‐(2‐naphthyl)alanine, the last amino acid to be coupled to the resin. We report the synthesis of [^14^C]‐ and [^14^C~3~]‐Org 37462, starting from 2‐bromo‐[^14^C‐methyl]‐naphthalene and [^14^C~2~]‐tert‐butyl glycinate. Copyright © 2008 John Wiley & Sons, Ltd.

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