Synthesis of methyl-1-(tert -butoxycarbonylamino)-2- vinylcyclopropanecarboxylate via a hofmann rearrangement utilizing trichloroisocyanuric acid as an oxidant
A trichloroisocyanuric acid (TCCA) mediated Hofmann rearrangement was utilized to synthesize methyl-1-(tert-butoxycarbonylamino)-2- vinylcyclopropanecarboxylate. A variety of functional groups are tolerated in this reaction including vinyl, cyclopropyl, pyridyl, aryl, benzyl, and nitro groups.
Crane, Zackary D.,Nichols, Paul J.,Sammakia, Tarek,Stengel, Peter J.
COMPOUNDS FOR INHIBITING TNIK AND MEDICAL USES THEREOF
The present disclosure provides the compound having inhibitory property against TNIK having a specific chemical structure or its pharmaceutically acceptable salt. The present disclosure also provides a composition comprising the compound or its pharmaceutically acceptable salt. The present disclosure also provides a medical use of the compound, its salt or the composition comprising the compound or its pharmaceutically acceptable salt for treating or preventing cancer. The present disclosure also provides a method of treatment or prevention of cancer comprising administering the compound, its salt or the composition comprising the compound or its salt to a subject in need of such treatment or prevention.
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Paragraph 604-607
(2019/08/29)
Quinone Imine Route to Benzimidazol-2-ylcarbamates. Part 1. Synthesis of Open-chain and Cyclic 5-Acylamino Derivatives.
The synthesis of the N',N''-bismethoxycarbonyl-N-(4-acylaminophenyl)guanidines (4) and (7) is described.Oxidation of these with LTA has led to the benzimidazol-2-ylcarbamates. (8), (9) and (10) through a regiospecific cyclisation of quinone imine intermediates.If the acylamino group is part of a ring, the yield of benzimidazoles (15) increases with the size of the lactam ring.The direction of ring closure may be controlled by electronic and steric factors.