50735-34-7Relevant articles and documents
Directing Group Enables Electrochemical Selectively Meta-Bromination of Pyridines under Mild Conditions
Wu, Yanwei,Xu, Shanghui,Wang, Hong,Shao, Dongxu,Qi, Qiqi,Lu, Yi,Ma, Li,Zhou, Jianhua,Hu, Wei,Gao, Wei,Chen, Jianbin
, p. 16144 - 16150 (2021/07/19)
Without the use of catalysts and oxidants, a facile and sustainable electrochemical bromination protocol was developed. By introducing the directing groups, the regioselectivity of pyridine derivatives could be controlled at themeta-position utilizing the inexpensive and safe bromine salts at room temperature. A variety of brominated pyridine derivatives were obtained in 28-95% yields, and the reaction could be readily performed at a gram scale. By combining the installation and removing the directing group, the concept ofmeta-bromination of pyridines could be verified.
Synthesis and in vitro evaluation of diverse heterocyclic diphenolic compounds as inhibitors of DYRK1A
Zhou, Qingqing,Reekie, Tristan A.,Abbassi, Ramzi H.,Indurthi Venkata, Dinesh,Font, Josep S.,Ryan, Renae M.,Munoz, Lenka,Kassiou, Michael
, p. 5852 - 5869 (2018/11/10)
Dual-specificity tyrosine phosphorylation-related kinase 1A (DYRK1A) is a dual-specificity protein kinase that catalyses phosphorylation and autophosphorylation. Higher DYRK1A expression correlates with cancer, in particular glioblastoma present within the brain. We report here the synthesis and biological evaluation of new heterocyclic diphenolic derivatives designed as novel DYRK1A inhibitors. The generation of these heterocycles such as benzimidazole, imidazole, naphthyridine, pyrazole-pyridines, bipyridine, and triazolopyrazines was made based on the structural modification of the lead DANDY and tested for their ability to inhibit DYRK1A. None of these derivatives showed significant DYRK1A inhibition but provide valuable knowledge around the importance of the 7-azaindole moiety. These data will be of use for developing further structure-activity relationship studies to improve the selective inhibition of DYRK1A.
PHENYL-TRIAZOLO-PYRIDINE COMPOUNDS
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Paragraph 0034, (2017/02/24)
The present invention provides a compound of the Formula (I) below: wherein R1 is selected from the group consisting of H, CH3, CN, —CH2CN, —C(CH3)2CN, F, Cl, and Br; R2 is selected from the group consisting of H, —O(C1-C3alkylene)R4, —CH2CN, CN, —OCH3, CF2, —C(CH3)2CN, —C(CH3)2, —S(O)2CH3, —S(O)2NH2, and —OCF2; R3 is selected from the group consisting of H, CH3, and —OCH3; and R4 is selected from the group consisting of H, —C(CH3)2CN, —OCH3, —S(O)2CH3, CN, and —C(CH3)2OH; or a pharmaceutical salt thereof, methods of treating type two diabetes using the compound and a process for preparing the compound.
