7267-26-7Relevant articles and documents
Lysophosphatidic acid receptor antagonists and preparation method thereof
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Paragraph 0709-0710; 0712-0714, (2020/07/29)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to lysophosphatidic acid receptor antagonists and a preparation method thereof. The applicant surprisinglyfinds that compounds provided by the invention have high LPAR1 antagonistic activity and selectivity, low toxicity, good metabolic stability and good drug development prospect, and can be used for preventing or treating diseases or symptoms related to LPAR1. The applicant also accidentally finds that the IC50 value of part of the compounds can be as low as 300 nM or below and even 50 nM or below.Moreover, the compounds disclosed by the invention have better safety, and the CC50 range of the compounds can reach 200 [mu]M or above. In addition, the compounds of the present invention have goodmetabolic stability in humans, rats, and mice, such excellent inhibitory activity being very desirable for their use as LPAR1 inhibitors in the above diseases or disorders. In addition, the preparation method of the compounds is simple, mild in reaction condition, high in product yield and suitable for industrial production.
Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions
Ruff, Yves,Berst, Frédéric
supporting information, p. 1188 - 1193 (2018/08/01)
Herein, we describe the development of copper-catalyzed cross-coupling of DNA-conjugated aryl iodides with aliphatic amines. This protocol leverages a novel ligand, 2-((2,6-dimethoxyphenyl)amino)-2-oxoacetic acid, to effect the transformation in aqueous D
Dibutyltin oxide catalyzed aminolysis of oxalate to carbamate, oxamate and derivatives of imidazolidine trione
Kunde, Lalita B.,Kalyani, Vishwanath S.,Gupte, Sunil P.
experimental part, p. 402 - 407 (2010/08/06)
Catalytic aminolysis of oxalates by simple and substituted ureas has been shown to give carbamates, oxamates and derivatives of imidazolidine trione. Various substituted ureas and oxalates were screened to verify the applicability of the protocol. The rol