Application of C-H Functionalization in the Development of a Concise and Convergent Route to the Phosphatidylinositol-3-kinase Delta Inhibitor Nemiralisib
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.
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)
Formation of 6-Azaindoles by Intramolecular Diels-Alder Reaction of Oxazoles and Total Synthesis of Marinoquinoline A
A new variant of the intramolecular Diels-Alder oxazole (IMDAO) cycloaddition that provides direct access to 6-azaindoles was developed. The IMDAO reaction was applied in a total synthesis of the aminophenylpyrrole-derived alkaloid marinoquinoline A, also
Jhaveri, Dishit P.,Osano, Mana,Wipf, Peter
supporting information
p. 2215 - 2219
(2020/04/09)
CHEMICAL COMPOUNDS
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
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Page/Page column 49
(2018/03/06)
PROCESSES TO MAKE INDAZOLE DERIVATIVES
The present invention provides novel processes for preparing compounds of formula (IV) and salts thereof, novel intermediates,and a novel salt and polymorph thereof.
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Page/Page column 21
(2016/12/22)
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