专利号:US-2007088086-A1 优先权日:1999-08-16 标题 :Method of using synthetic L-Se-methylselenocysteine as a nutriceutical and a method of its synthesis 发明人:SPALLHOLZ JULIAN E; REID TED W; WALKUP ROBERT D 权利人:PHARMASE INC 摘要:A synthesis of and use for L-Se-methylselenocysteine as a nutriceutical is described, based upon the knowledge that L-Se-methylselenocysteine is less toxic than L-selenomethionine towards normal cells. The synthesis proceeds by mixing N-(tert-butoxycarbonyl)-L-serine with a dialkyl diazodicarboxylate and at least one of a trialkylphosphine, triarylphosphine, and phosphite to form a first mixture that includes N-(tert-butoxycarbonyl)-L-serine β-lactone. Methyl selenol or its salt is mixed with the N-(tert-butoxycarbonyl)-L-serine β-lactone to form a second mixture that includes N-(tert-butoxycarbonyl)-Se-methylselenocysteine. The tert-butoxycarbonyl group is removed from the N-(tert-butoxycarbonyl)-Se-methylselenocysteine to form L-Se-methylselenocysteine. This synthesis significantly improves the manufacturability, manufacturing efficiency, and utility of this naturally occurring rare form of organic-selenium. L-Se-methylselenocysteine formed, for example, in this manner may be used as a nutriceutical for supplementation into the diets of humans or animals for various beneficial purposes, such as, for example, to prevent or reduce the risk of developing cancer.
参考标题:Synthesis Of Sulfonylhydrazine-1,2-Dicarboxylates From Thiols And Dialkyl Azodicarboxylates 作者:Jiaxi Xu,Bingnan Zhou,Xiao Yang 摘要:Thiols/thiophenols To Dialkyl Azodicarboxylates And Subsequent Oxidation With Mcpba. The Protocol Represents The First Application Of Sulfenylhydrazines As Precursors To Sulfonylhydrazine Derivatives, Leading To A Novel And Effective Method For The Synthesis Of Sulfonylhydrazines. 1-Sulfonylhydrazine-1,2-Dicarboxylates Are Efficiently Prepared Via Nucleophilic Addition Of Thiols/thiophenols To Dialkyl Azodicarboxylates
合成参考文献
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