156079-89-9Relevant academic research and scientific papers
A higher yielding synthesis of the clinical prodrug ZD2767P using di-protected 4-[N,N-bis(2-hydroxyethyl)amino]phenyl chloroformate
Niculescu-Duvaz, Dan,Scanlon, Ian,Niculescu-Duvaz, Ion,Springer, Caroline J.
, p. 6919 - 6922 (2007/10/03)
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.
High purity N-(4-[N,N-bis(2-iodoethyl)amino]phenoscycarbonyl)-L-glutamic acid
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, (2008/06/13)
A new salt of a prodrug useful in antibody directed enzyme prodrug therapy (ADEPT) is disclosed. A hydrogen iodide salt of the prodrug N-(4-[N,N-bis(2-iodoethyl)amino]phenoxycarbonyl)-L-glutamic acid is prepared which can be obtained in crystalline form. Preparation of the crystalline form of the prodrug enables preparation of the prodrug in highly pure form.
Optimization of Alkylating Agent Prodrugs Derived from Phenol and Aniline Mustards: A New Clinical Candidate Prodrug (ZD2767) for Antibody-Directed Enzyme Prodrug Therapy (ADEPT)
Springer, Caroline J.,Dowell, Robert,Burke, Philip J.,Hadley, Elma,Davies, D. Huw,et al.
, p. 5051 - 5065 (2007/10/03)
Sixteen novel potential prodrugs derived from phenol or aniline mustards and their 16 corresponding drugs with ring substitution and/or different alkylating functionalities were designed.The 4-bis(2-bromoethyl)-(1a), 4-bis(2-iodoethyl)-(1b), and
