Addition Of Carbamoylsiane To Isation: Synthesisi Of 3-hydroxy-3-aminocarbony-2-oxind Oles Derivatives

This paper includes two parts: 1.Since the pioneering work of palladium-catalyzed aminocarbonylation reaction discovered by Heck and co-workers in 1974,the response received extensive attention of the researchers,there are a large number of literature reports the method of this kind of reaction,however,these methods used in one carbon unit is a highly toxic carbon monoxide gas,and there are highly toxic,there are many restrictions in the practical application,development and its equivalent of one carbon unit is a difficult problem to be solved.Carbamoylsilane is a kind of have extremely extensive application in the field of organic synthesis of the very important organosilicon reagents.Previously,our lab has carried out some work about on carbamoylsilane in the field of organic synthesis,efficient preparation of carbamoylsilane reagents,and the study found that the reagent can be efficient and aldehydes,ketones,imines substrates such as addition reaction.At present,the development of new reaction type carbamoylsilane reagents,extend the class application of reagent,is our main research content.2.3-Hydroxy-3-aminocarbonyl-2-oxindoles derivatives is a kind of very important skeleton,exists in many natural products and drugs active ingredient.The current literature can get involved in the synthesis of the skeleton method basically has two kinds,one is a three-component Passerini reaction by employing isatins as the carbonyl compound component under solvent-free conditions.The reaction resulted in the synthesis of biologically important3-hydroxy-3-aminocarbonyl-2-oxindoles in high yields after hydrolysis.The other is a cycloaddition reaction.Directly using ammonia formylation reagent and oxidation of indole addition reaction has not been reported.As a result,this experiment wasdesigned using organosilicon reagents and oxidative addition reaction of indole,get a3-hydroxy-3-aminocarbonyl-2-oxindoles derivatives.The whole experiment have mild reaction conditions and do not need to add the catalyst,one step synthesis product,the production rate is higher,the experimental operation simple and easy to repeat,expand production which can be promoted.