189321-63-9Relevant articles and documents
Oxidation of Primary Alcohols and Aldehydes to Carboxylic Acids via Hydrogen Atom Transfer
Tan, Wen-Yun,Lu, Yi,Zhao, Jing-Feng,Chen, Wen,Zhang, Hongbin
supporting information, p. 6648 - 6653 (2021/09/08)
The oxidation of primary alcohols and aldehydes to the corresponding carboxylic acids is a fundamental reaction in organic synthesis. In this paper, we report a new chemoselective process for the oxidation of primary alcohols and aldehydes. This metal-free reaction features a new oxidant, an easy to handle procedure, high isolated yields, and good to excellent functional group tolerance even in the presence of vulnerable secondary alcohols and tert-butanesulfinamides.
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels
Qu, Chunrong,Ding, Mingmin,Zhu, Yingmin,Lu, Yungang,Du, Juan,Miller, Melissa,Tian, Jinbin,Zhu, Jinmei,Xu, Jian,Wen, Meng,Er-Bu,Wang, Jule,Xiao, Yuling,Wu, Meng,McManus, Owen B.,Li, Min,Wu, Jilin,Luo, Huai-Rong,Cao, Zhengyu,Shen, Bing,Wang, Hongbo,Zhu, Michael X.,Hong, Xuechuan
, p. 4680 - 4692 (2017/06/13)
Transient receptor potential canonical 3/6/7 (TRPC3/6/7) are highly homologous receptor-operated nonselective cation channels. Despite their physiological significance, very few selective and potent agonists are available for functional examination of these channels. Using a cell-based high throughput screening approach, a lead compound with the pyrazolopyrimidine skeleton was identified as a TRPC6 agonist. Synthetic schemes for the lead and its analogues were established, and structural-activity relationship studies were carried out. A series of potent and direct agonists of TRPC3/6/7 channels were identified, and among them, 4m-4p have a potency order of TRPC3 > C7 > C6, with 4n being the most potent with an EC50 of 20 nM on TRPC3. Importantly, these compounds exhibited no stimulatory activity on related TRP channels. The potent and selective compounds described here should be suitable for evaluation of the roles of TRPC channels in the physiology and pathogenesis of diseases, including glomerulosclerosis and cancer.
A pyrazolo [1,5-a] pyrimidine derivative and its anti-tumor use
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Paragraph 0055, (2017/01/19)
The present invention relates to a pyrazolo[1,5-a]pyrimidine derivative of general formula 1 and a pharmaceutically acceptable salt thereof. The present invention also relates to use of compounds of formula 1 in the preparation of an anti-tumor medicament.