156079-90-2Relevant 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.
Preparation of the key intermediate in a novel synthesis of ZD9063P: The chemical component of ADEPT, a targeted cytotoxic therapy
Martin, David M. G.,Siedlecki, Pawel S.
, p. 259 - 263 (2013/09/07)
A novel regioselective opening of the cyclic anhydride of a urethane derivative of glutamic acid using 4-(dimethylamino)-pyridine (DMAP) as the catalyst has greatly simplified the synthesis of the target compound, ZD9063P, 5-(N-[(S)-N-{N,N-bis(2-chloroeth
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
