121432-12-0Relevant articles and documents
Application of C-H Functionalization in the Development of a Concise and Convergent Route to the Phosphatidylinositol-3-kinase Delta Inhibitor Nemiralisib
Bream, Robert N.,Clark, Hugh,Edney, Dean,Harsanyi, Antal,Hayler, John,Ironmonger, Alan,Mc Cleary, Nadine,Phillips, Natalie,Priestley, Catherine,Roberts, Alastair,Rushworth, Philip,Szeto, Peter,Webb, Michael R.,Wheelhouse, Katherine
, p. 529 - 540 (2021/03/01)
This paper describes the development of an improved and scalable method for the manufacture of nemiralisib, a phosphatidylinositol-3-kinase delta inhibitor. Incorporation of three consecutive catalytic reactions, including a palladium-catalyzed C-H functionalization and an iridium-catalyzed borylation, significantly simplified and shortened the synthetic sequence. The revised route was successfully implemented in a pilot plant on a multikilogram scale to deliver >100 kg of product.
A NEW PROCESS FOR THE SYNTHESIS OF 2-AMINOXAZOLE COMPOUNDS
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Page/Page column 10, (2008/06/13)
The present invention relates to a process for synthesizing in good yield substituted 2- aminoaryloxazole compounds of formula I which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit, bcr-abl, Flt-3 and mutant forms thereof