On January 4, 2018, Kim, In Woo; Han, Mi Ryeong; Yoo, Jakyung; Oh, Yun Ju; Kim, Ji Duck; Kim, Nam Youn; Jun, Sun Ah; Lee, Jun Hee; Park, Joon Seok published a patent.Electric Literature of 16230-24-3 The title of the patent was Pyrazolopyrimidine derivatives as kinase inhibitor and their preparation. And the patent contained the following:
The invention relates to a pyrazolopyrimidine derivative of formula I, or a pharmaceutically acceptable salt thereof. The compound according to the invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions. Compounds of formula I wherein R1 is (un)substituted C6-10 aryl and (un)substituted C2-10 heteroaryl; R2 is H, C1-4 alkyl and halo; R3 is (un)substituted C1-4 alkyl, (un)substituted C2-6 alkenyl and (un)substituted C2-6 alkynyl; X1 is CR4 and N; R4 is H, C1-4 alkyl and halo; X2 is CR5 and N; R5 is H, C1-4 alkyl, C1-4 alkoxy, halo, etc.; X3 is NH and derivatives, O and S; X4 is CH and N; X5 is a bond and NH; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with tert-Bu (R)-3-aminopiperidin-1-carboxylate followed by Boc-deprotection; the resulting (R)-2-chloro-N-(piperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride underwent N-acylation with acryloyl chloride followed by amination with 4-(4-methylpiperazin-1-yl)aniline to give compound II. The invention compounds were evaluated for their kinase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 3.73 nM and 10.7 nM towards JAK3 and BTK, resp. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3
The Article related to pyrazolopyrimidine preparation kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 16230-24-3
Referemce:
Amide – Wikipedia,
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