681484-59-3Relevant articles and documents
Preparation method of alpha-deuterated olefine aldehyde
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Paragraph 0026; 0097-0100; 0105; 0106, (2022/03/27)
The invention relates to a preparation method of alpha-deuterated olefine aldehyde, which comprises the following steps: by taking alpha, beta-olefine aldehyde as a raw material, carrying out a reversible Michael addition mechanism under the action of deuterium water, a nucleophilic reagent and an organic catalyst to obtain an alpha-deuterated olefine aldehyde compound. The method has high selectivity, and does not generate deuterated by-products at other positions. The alpha-deuterated olefine aldehyde compound prepared by the invention has great application value, can be further widely converted to prepare mono (poly) deuterated olefin and derivatives, olefine acid, conjugated olefine aldehyde, eneyne and other compounds, and has important significance in drug synthesis.
Palladium-Catalyzed Cascade Double C—N Bond Activation: A New Strategy for Aminomethylation of 1,3-Dienes with Aminals
Qiao, Cuifang,Chen, Anrong,Gao, Bingjian,Liu, Yang,Huang, Hanmin
supporting information, p. 929 - 933 (2018/09/22)
A new palladium-catalyzed selective aminomethylation of conjugated 1,3-dienes with aminals via double C—N bond activation is described. This simple method provides an effective and rapid approach for the synthesis of linear α,β-unsaturated allylic amines with perfect regioselectivity. Mechanistic studies disclosed that one palladium catalyst cleaved two distinct C—N bond to furnish a cascade double C—N bond activation, in which an allylic 1,3-diamine and allylic 1,2-diamine were initially formed as key intermediates through the palladium-catalyzed C—N bond activation of aminal and the α,β-unsaturated allylic amine was subsequently produced via palladium-catalyzed C—N bond activation of the allylic diamines.
Tubulin inhibitor
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Paragraph 0061; 0062; 0063, (2017/08/28)
The invention provides a novel tubulin inhibitor and an application thereof. The novel tubulin inhibitor is a series of substituted heterocyclic skeleton-based compounds with colchicine binding sites in tubulins as targets. The compounds have the following structure as shown in the specification, wherein the formula is as shown in the specification; n independently represents an integer of 0-5 under the condition that n is less than or equal to 5; A represents a monosubstituted or polysubstituted group; and the group is selected from H, C1-C20 acylamino, C1-C20 acyloxy, C1-C20 alkanoyl, C1-C20 alkoxycarbonyl, C1-C20 alkoxy, C1-C20 alkylamino, C1-C20 alkylcarboxy amino, aroyl, arylalkanoyl, carboxyl, cyano, halogen, hydroxyl, nitro and methylthienyl.
Structure-activity relationships of antitubercular nitroimidazoles. 2. determinants of aerobic activity and quantitative structure-activity relationships
Kim, Pilho,Kang, Sunhee,Boshoff, Helena I.,Jiricek, Jan,Collins, Margaret,Singh, Ramandeep,Manjunatha, Ujjini H.,Niyomrattanakit, Pornwaratt,Zhang, Liang,Goodwin, Michael,Dick, Thomas,Keller, Thomas H.,Dowd, Cynthia S.,Barry III, Clifton E.
experimental part, p. 1329 - 1344 (2009/12/07)
The (S)-2-nitro-6-substituted 6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines have been extensively explored for their potential use as new antituberculars based on their excellent bactericidal properties on aerobic whole cells of Mycobacterium tuberculosis. A
