93353-66-3Relevant academic research and scientific papers
A new approach to rapid parallel development of four neurokinin antagonists. Part 2. Synthesis of ZD6021 cyano acid
Moseley, Jonathan D.,Moss, William O.,Welham, Matthew J.,Ancell, Claire L.,Banister, John,Bowden, Sharon A.,Norton, Glenn,Young, Maureen J.
, p. 58 - 66 (2003)
The manufacture of ZD6021 cyano acid (1) using a new project approach is described. Research Department processes were scaled up to 100 L if process safety anal robustness were not compromised; other factors were treated according to the new approach. By using this strategy, we were able to manufacture a key intermediate on sufficient scale to support delivery of 1 kg quantities of bulk drug within 6 months of the start of lab work.
The mercury-mediated decarboxylation (Pesci reaction) of naphthoic anhydrides investigated by microwave synthesis
Moseley, Jonathan D.,Gilday, John P.
, p. 4690 - 4697 (2007/10/03)
The mercury-mediated decarboxylation (Pesci reaction) of several substituted naphthoic anhydrides has been investigated by microwave synthesis. A laboratory microwave reactor was found to be ideal for small-scale preparations of this slow reaction, reducing reaction times from typically four days to less than 1 h for the three-step process. The ionic reaction medium rapidly heated to high temperatures under microwave heating and could be efficiently maintained by low microwave power settings. Generation of stoichiometric CO2 was safely contained within the reaction tubes. A simplified reaction procedure has been developed. For substituted naphthoic anhydrides, 1H NMR analysis of the naphthoate ester derivatives indicated no change in the regioisomer ratio compared to previously reported thermal values.
