63936-02-7Relevant articles and documents
Development of a practical synthesis to PI3K α-selective inhibitor GDC-0326
Koenig, Stefan G.,Green, Keena L.,Müller, Barbara,Sowell, C. Gregory,Askin, David,Gosselin, Francis
, (2020/12/29)
A practical route to PI3K α-selective inhibitor GDC-0326 is reported. The synthesis leverages an existing scheme to a key tetracyclic benzoxazepine intermediate and optimizes it for robustness and scalability, including removing numerous undesired conditions and reagents, as well as eliminating chromatographic purification steps. The process endgame is streamlined to utilize a single-step, stereocontrolled alkylation of the key phenol with a chiral lactamide mesylate, followed by recrystallization of the lactamide ether product, to deliver the desired enantiomer of the active pharmaceutical ingredient (API) GDC-0326.
AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
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Paragraph 0229, (2016/06/21)
Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
BENZPYRAZOL DERIVATIVES AS INHIBITORS OF PI3 KINASES
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Page/Page column 99-100, (2009/12/28)
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 PI3-kinase activity.