The Article related to pyrazolopyrimidine preparation ret kinase inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 1028092-65-0
On July 25, 2019, Blake, James F.; Dai, Donghua; Haas, Julia; Jiang, Yutong; Kolakowski, Gabrielle R.; Metcalf, Andrew T.; Moreno, David A.; Prigaro, Brett; Ren, Li published a patent.Recommanded Product: 1028092-65-0 The title of the patent was Preparation of substituted pyrazolo[3,4-d]pyrimidine compounds as RET kinase inhibitors. And the patent contained the following:
The invention is related to the preparation of compounds I [R1 = (un)substituted 5-membered heteroaryl ring having 2-3 ring heteroatoms independently selected from N, O and S, provided that when R1 is an isoxazolyl ring, then R1 is substituted with 2 specified substituents; R2 = H, alkyl, cyanoalkyl, etc.], their tautomers, stereoisomers, pharmaceutically acceptable salts and solvates, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase. Thus, II was prepared in 5 steps from 5-cyclopropylisoxazole-3-carboxylic acid and malononitrile using isopropylhydrazine hydrochloride, formamide, NBS and 1-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. I were screened for their ability to inhibit several RET kinase forms (wild type, V804M M918T, G810R, and G810S mutants) (data given for representative compounds I in an enzyme assay and/or cell assay). Pharmaceutical compositions comprising compound I, alone or in combination with an addnl. therapy or therapeutic agent, were disclosed. The experimental process involved the reaction of 3-Phenyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 1028092-65-0).Recommanded Product: 1028092-65-0
The Article related to pyrazolopyrimidine preparation ret kinase inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 1028092-65-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics