On August 22, 2019, Chen, Yi published a patent.Category: pyrazines The title of the patent was Preparation of cyclopentapyrrolopyrazine derivatives as inhibitors of Btk and mutants thereof. And the patent contained the following:
The title compounds I [Q1 = 5-6 membered aryl or heteroaryl; Q2 = 5-7 membered heterocycloalkyl, or heteroaryl; Q3 = 5-membered heteroaryl; each of W, X, Y, Z1, independently, = C(Ra), or N; each of R1, and R5, independently, = H, D, alkyl, etc.; R2 = H or alkyl; R3 = H, halo, alkyl, haloalkyl, or hydroxyalkyl; R4 = H, halo, alkyl; two of R1 groups, taken together with the atom to which they are attached, may optionally form (un)substituted cycloalkyl or heterocycloalkyl; two of R5 groups, taken together with the atom to which they are attached, may optionally form (un)substituted cycloalkyl or heterocycloalkyl; Ra = H, D, alkyl, etc.; each of m, n = (independently) 0-4; Warhead = CH:CH2, CH:CHCH2NMe2, CCMe], useful for treating a neoplastic disease, autoimmune disease, and inflammatory disorder, were prepared E.g., a multi-step synthesis of N-[5-({6-[2-(7,7-dimethyl-1-oxo-1,3,4,6,7,8-hexahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-2-yl)-3-(hydroxymethyl)pyridin-4-yl]-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl}amino)-2-(4-methylpiperazin-1-yl)phenyl]acrylamide, starting from 4-fluoro-3-nitroaniline and 1-methylpiperazine, was described. Representative compounds I were evaluated in the biochem. enzymic assay (IC50) against WT and C481S BTK (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Category: pyrazines
The Article related to cyclopentapyrrolopyrazine preparation btk inhibitor antitumor antiinflammatory autoimmune disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazines