893428-72-3Relevant academic research and scientific papers
Development of an efficient and practical route for the multikilogram manufacture of the SRC kinase inhibitor AZD0530
Ford, J. Gair,OKearney-Mcmullan, Anne,Pointon, Simon M.,Powell, Lyn,Siedlecki, Paul S.,Purdie, Mark,Withnall, Jane,Frances Wood, Phil OKeefe
, p. 1088 - 1093 (2011/04/15)
In a previous publication (Org. Process Res. Dev. 2010, 14, DOI:10.1021/op100161y) we described the process research and development of a manufacturing route for the potent SRC kinase inhibitor AZD0530. While the route was successfully used to manufacture 4.5 kg of AZD0530 difumarate, it was still relatively long, used two Mitsunobu couplings, and was, in our opinion, undesirable for manufacture on a larger scale. Herein we describe the research and development of a shorter, more practical synthesis of AZD0530 difumarate. The new route, which required fewer steps, scaled well to produce >80 kg of AZD0530 difumarate in an overall yield of 38%.
Process research and development for the kilogram manufacture of the SRC kinase inhibitor AZD0530
Ford, J. Gair,Pointon, Simon M.,Powell, Lyn,Siedlecki, Paul S.,Baum, John,Chubb, Richard,Fieldhouse, Robin,Muxworthy, James,Nivlet, Alex,Stenson, Rachel,Warwick, Eleanor
experimental part, p. 1078 - 1087 (2011/04/12)
Process research and development of a synthetic route towards a novel SRC kinase inhibitor is described. The Medicinal Chemistry route was very long and suffered from extensive use of chlorinated solvents and chromatography. A number of steps in the Medic
CHEMICAL PROCESS
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Page/Page column 61-63, (2008/06/13)
The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]- 5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermed
