141699-55-0Relevant articles and documents
Reaction Rates of Various N-Acylenamines in the Inverse-Electron-Demand Diels–Alder Reaction
Engelsma, Sander B.,van den Ende, Thomas C.,Overkleeft, Hermen S.,van der Marel, Gijsbert A.,Filippov, Dmitri V.
, p. 2587 - 2591 (2018)
In light of the bioorthogonal inverse-electron-demand Diels–Alder strategy, an extended investigation into the effects of ring strain and electron inductive effects on the reactivity of the N-acylenamine core towards tetrazine has been carried out. Through a comparative study between N-acylazetines, N-vinylcarbamates and an N-vinylamide it was shown that ring strain has a more significant effect on reaction rate than electron donation. A significantly improved synthetic route is reported for the preparation of an N-acylazetine biorthogonal tag we have invented previously.
A novel RET inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0312-0315, (2021/11/26)
The invention belongs to the field of medicines, and relates to a novel RET inhibitor, a pharmaceutical composition and application thereof. In particular, the invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I said compound and a pharmaceutical composition thereof for the manufacture of a medicament, in particular for the treatment and prophylaxis and RET of diseases and disorders associated with irritable bowel syndrome.
PROCESSES OF PREPARING A JAK1 INHIBITOR
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, (2021/12/17)
The present application provides processes for preparing 4-[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H, 1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide, and phosphoric acid salt thereof, which is useful as a selective (Janus kinase 1) JAK1 inhibitor, as well as salt forms and intermediates related thereto.
