On December 27, 2018, Cho, Seong Yun; Kim, Pil Ho; Lee, Jeong Ok; Kim, Hyeong Rae; Ha, Jae Du; Jung, Hui Jeong; Yoon, Chang Su; Park, Ji Hun; Hwang, Jong Yeon published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Fused pyrimidine derivative as Bruton’s tyrosine kinase inhibitor, and method for the preparation thereof. And the patent contained the following:
Disclosed are compound I [n = 0 or 1; A = single bond, -NH- or -O-; D1 = CR4 or N; R4 = H or alkyl; D2 = CH or N; D3 = N or NH; a dotted line accompanied by a solid line represents a single bond or a double bond; R1 = (un)substituted aryl; R2, R3 = independently H, (un)substituted aryl, (un)substituted cycloalkyl, etc.; or its optical isomer or pharmaceutically acceptable salt] and pharmaceutical compositions For example, compound II was prepared from malononitrile via conversion to 4,6-dichloro-3-methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine followed by treatment with K2CO3/N-(1s,4s)-(4-aminocyclohexyl)acrylamide and Pd2(dba)3-catalyzed reaction with 4-morpholinoaniline. The invention compound showed high inhibitory activity for Bruton’s tyrosine kinase (BTK), e.g., IC50 value of II was 0.001 μM. Compound I is claimed useful for the treatment of cancer or autoimmune disease. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide
The Article related to fused pyrimidine preparation bruton tyrosine kinase inhibitor, cancer autoimmune disease treatment fused pyrimidine btk inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics