458-10-6Relevant articles and documents
Intermediate for synthesizing camptothecin derivative as well as preparation method and application thereof
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Paragraph 0105, (2020/08/09)
The invention relates to the technical field of organic compound synthesis, in particular to an intermediate for synthesizing a camptothecin derivative as well as a preparation method and applicationof the intermediate. An intermediate A can be obtained by acylation, bromination and cross coupling reaction of 3-fluoro-4-methylaniline. The intermediate A can be used for preparing an intermediate Bso as to further prepare Exatecan mesylate. The intermediate compound B can be obtained by rearrangement reaction of the intermediate A; Exatecan mesylate can be obtained by subjecting the intermediate compound B to alpha-site acetamido and amino deprotection, condensation reaction and hydrolysis reaction. The method has the advantages of low price of reaction initiators, mild reaction conditionsof each step, simplicity and convenience in operation, high yield and suitability for industrial production.
Human sialidase inhibitors: Design, synthesis, and biological evaluation of 4-acetamido-5-acylamido-2-fluoro benzoic acids
Magesh, Sadagopan,Savita, Vats,Moriya, Setsuko,Suzuki, Tohru,Miyagi, Taeko,Ishida, Hideharu,Kiso, Makoto
experimental part, p. 4595 - 4603 (2009/12/01)
Recent advances in the sialidase biology have clarified the role of human sialidases (NEU 1 to NEU4) in the development of various disease states such as cancer, diabetes and arteriosclerosis. Isoform selective human sialidase inhibitors could be a therap
Pd-catalyzed ortho-selective oxidative coupling of halogenated acetanilides with acrylates
Lee, George T.,Jiang, Xinglong,Prasad, Kapa,Repic, Oljan,Blacklock, Thomas J.
, p. 1921 - 1924 (2007/10/03)
Coupling of different halogenated acetanilides with acrylates using Pd-catalyzed ortho-selective C-H bond activation is reported. The yields of coupled products are low to high depending on the substrate. In general, arenes with electron-rich substituents like methoxy and methyl groups gave higher yields of the coupled products. The presence of the halogen substituent did not interfere with the activation process under these conditions.