| 1,3,4-oxadiazole and vinyl sulfone compounds are present in a wide variety of pharmaceutical molecules and natural product fragments,have a very wide range of biological and pharmacological activities,while in organic synthesis and materials and other fields also have a lot of applications.Thus,they play an important role in people's life and production.However,the most of traditional methods have some drawbacks on their synthesis.For example,for the synthesis of 1,3,4-oxadiazole compounds,some methods require the addition of expensive metal catalysts,some methods require the addition of large amounts of oxidants,etc.;for the synthesis of vinyl sulfone compounds,some traditional method requires complex synthesis route,or need to use expensive metal catalysts and toxic and volatile organic solvents,low yield,poor selectivity.Therefore,developing a new and effective synthetic method is very crucial and valuable.Focus on this,the contents of this study include the following two parts:(1)We have developed a sulfur powder to promote hydrazides and isocyanides synthetic method of 2-amino-1,3,4-oxadiazoles compounds.The reaction material is simple and easy to obtain,the reaction condition is simple,the functional group is good adaptability,wide range of substrates.The reaction does not require the addition of additional catalysts,oxidants,etc..This approach circumvents some of the obvious drawbacks of traditional methods.(2)We have developed a novel water to promote the direct sulfonylation of propiolate.The reaction is carried out directly in water by a simple and readily available sulfonylhydrazides and propiolates starting material to give(Z)-?-sulfonyl enoates having a high degree of region selectivity and stereoselectivity.The reaction is simple,mild conditions,regional stereoselectivity is good,substrate adaptability,high yield.The reaction does not require the use of a metal catalyst and an organic solvent.Water as a solvent is environmentally friendly. |
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