82938-20-3Relevant articles and documents
Discovery of Novel 3-Amino-4-alkoxyphenylketones as PDE4 Inhibitors with Improved Oral Bioavailability and Safety against Spatial Memory Impairments
Feng, Kai-Wen,He, Jia-Peng,Liu, Lu,Wang, Hai-Tao,Xia, Chuang,Xu, Jiang-Ping,Zheng, Lei,Zhou, Zhong-Zhen
, p. 390 - 405 (2022/02/07)
To realize PDE4 inhibitors with good developmental potentiality for the treatment of dementia, structure-based optimizations of lead compound FCPR03 resulted in novel aminophenylketones 9c and 9H with low nanomolar potency, which displayed comparable acti
Aminophenone compounds as well as preparation method and application thereof
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, (2021/02/06)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to aminophenone compounds as well as a preparation method and application thereof. The aminophenone compounds provided by the invention have a good inhibition effect on PDE4, also have good bioavailability, can be applied to preparation of drugs for treating PDE4-related diseases, and increase the optionsof drugs for treating PDE4-related diseases; and the effect of a part of the aminophenone compounds is equivalent to the effect of positive drugs, and the aminophenone compounds have good developmentpotential.
DABCO-promoted photocatalytic C-H functionalization of aldehydes
Cardozo, Thiago Messias,Da Silva Santos, Bruno Maia,Finelli, Fernanda Gadini,de Souza, Cauê Paula,dos Santos Dupim, Mariana
supporting information, p. 2959 - 2967 (2022/01/12)
Herein we present a direct application of DABCO, an inexpensive and broadly accessible organic base, as a hydrogen atom transfer (HAT) abstractor in a photocatalytic strategy for aldehyde C-H activation. The acyl radicals generated in this step were arylated with aryl bromides through a well stablished nickel cross-coupling methodology, leading to a variety of interesting aryl ketones in good yields. We also performed computational calculations to shine light in the HAT step energetics and determined an optimized geometry for the transition state, showing that the hydrogen atom transfer between aldehydes and DABCO is a mildly endergonic, yet sufficiently fast step. The same calculations were performed with quinuclidine, for comparison of both catalysts and the differences are discussed.