Title of article
A higher yielding synthesis of the clinical prodrug ZD2767P using di-protected 4-[N,N-bis(2-hydroxyethyl)amino]phenyl chloroformate
Author/Authors
Niculescu-Duvaz، نويسنده , , Dan and Scanlon، نويسنده , , Ian and Niculescu-Duvaz، نويسنده , , Ion and Springer، نويسنده , , Caroline J.، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2005
Pages
4
From page
6919
To page
6922
Abstract
A novel synthesis is described of the prodrug ZD2767P (in Phase I/II clinical trials) that improves the overall yield from 13% to 45%. The method involves the synthesis of 4-[N,N-bis(2-hydroxyethyl)amino]phenyl chloroformate protected as the bis-silyl ether, coupled with di-tert-butyl glutamate. There are clear advantages of this method compared to the literature procedure.
Keywords
Antibody-directed enzyme prodrug therapy , Silyl protection , Scale-up synthesis , Chloroformate , Prodrug
Journal title
Tetrahedron Letters
Serial Year
2005
Journal title
Tetrahedron Letters
Record number
1846820
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