834-67-3Relevant articles and documents
Nickel-Catalyzed Decarboxylative Cross-Coupling of Bicyclo[1.1.1]pentyl Radicals Enabled by Electron Donor-Acceptor Complex Photoactivation
Polites, Viktor C.,Badir, Shorouk O.,Keess, Sebastian,Jolit, Anais,Molander, Gary A.
supporting information, p. 4828 - 4833 (2021/06/30)
The use of bicyclo[1.1.1]pentanes (BCPs) as para-disubstituted aryl bioisosteres has gained considerable momentum in drug development programs. Carbon-carbon bond formation via transition-metal-mediated cross-coupling represents an attractive strategy to generate BCP-aryl compounds for late-stage functionalization, but these typically require reactive organometallics to prepare BCP nucleophiles on demand from [1.1.1]propellane. In this study, the synthesis and Ni-catalyzed functionalization of BCP redox-active esters with (hetero)aryl bromides via the action of a photoactive electron donor-acceptor complex are reported.
AEROBIC OXIDATIVE SYNTHESIS OF SULFONAMIDE USING Cu CATALYST
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Paragraph 0033-0037; 0039-0054; 0066-0069; 0151-0152, (2021/04/06)
The present invention relates to a method for oxidative synthesis of sulfonamides using copper catalysts. , Oxygen (O) is used. 2 The oxidative synthesis of sulfonamides (1) comprises reacting a 2 th or sulfonyl hydrazide primary amine with a sulfonyl hydrazide (sulfonamide) with a copper catalyst on a solvent under the conditions in which the sulphonamide is fed. The oxidation coupling of the present invention showed extensive substrate ranges in an amine comprising a 2 primary amine, 1 primary amine and amine hydrochloride salt. It is worth notable that non-reactive aliphatic sulfonyl hydrazides in previously reported anaerobic systems can be used for the aerobic oxidation coupling of the present invention. The oxidation coupling of the present invention has been more effective on large scale.
Synthesis method of sulfonyl secondary amine compound
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Paragraph 0037-0041, (2021/04/21)
The invention belongs to the technical field of organic chemistry, and particularly relates to a preparation method of a sulfonyl secondary amine compound. The structure of the compound is characterized by 1H NMR, 13C NMR and HRMS and is confirmed. According to the method, acetonitrile and tetrahydrofuran are used as a mixed solvent, corresponding secondary amine, sulfonyl chloride and boric acid react under the heating condition in the presence of a palladium catalyst, a ligand and alkali, the secondary amine and the sulfonyl chloride firstly generate corresponding amino sulfonyl chloride, and then the amino sulfonyl chloride and the boric acid are subjected to a palladium-catalyzed Suzuki-Miyaura coupling reaction to obtain the target sulfonyl secondary amine compound. The preparation method of the compound has the advantages that corresponding sulfonyl chloride is prevented from being prepared in advance, meanwhile, the conditions are mild, the compatibility of functional groups is high, separation and purification are convenient, and good application value is achieved.