Difluoromethyl silver compound, single crystal, synthetic method and application

Abstract

The invention discloses a difluoromethyl silver compound, a single crystal, a synthetic method and an application. The invention provides a difluoromethyl silver compound (1a) or a difluoromethyl silver compound (1b), wherein R and R' are independently a phenyl group or a naphthyl group having substituent groups at any position of the phenyl group or the naphthyl group. The substituent group is one or more in number and is an alkyl group with the carbon number of 1-6, an alkoxy group with carbon number of 1-6 or an alkyl-substituted amino group with the carbon number of 1-6, wherein the substituent groups on the phenyl group or the naphthyl group are same or different and the R and R' are same or different. The invention also provides the synthetic method of the difluoromethyl silver compound (1a) or the difluoromethyl silver compound (1b), which includes following steps: carrying out a reaction with aza-carbene complexed silver chloride and trimethyl silyl difluoromethane. The difluoromethyl silver compound is good in stability, can be subjected to an electrophilic substrate through a difluromethylated reaction, is mild in reaction condition, is good in group compatibility and is excellent in market development prospect.

Description

technical field [0001] The invention relates to a difluoromethyl silver compound, single crystal, synthesis method and application. Background technique [0002] Since the introduction of fluorine atoms and fluoroalkyl groups into drug molecules can enhance their lipid solubility and metabolic stability, the introduction of fluorine atoms and fluoroalkyl groups into molecules has become an important goal in the design of drug molecules in recent years. . (a) Kirsch, P. Modern Fluoroorganic Chemistry: Synthesis, Reactivity, Applications; Wiley–VCH: Weinheim, 2004. b) Hiyama, T. Organofluorine Compounds: Chemistry and Properties; Springer-Verlag: Berlin, 2000. c) Uneyama, K.Organofluorine\Chemistry;Blackwell:Oxford,U.K.,2006.(d)O'Hagan,D.Chem.Soc.Rev.2008,37,308.d)Leroux,F.;Jeschke,P.;Schlosser,M.Chem .Rev.2005,105,827.e)Ma,J.-A.;Cahard,D.Chem.Rev.2004,104,6119;f)Ma,J.-A.;Cahard,D.Chem.Rev.2008 ,108,PR1;g)Nie,J.;Guo,H.-C.;Cahard,D.;Ma,J.-A.Chem.Rev.2011,111,455.) where difl...

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to provide a difluoromethyl silver compound, single crystal, synthetic Method and application, the difluoromethylsilver compound of the present invention has good stability, and can undergo difluoromethylation reactions with substrates such as diaryl iodides, acyl chloride substrates, and active halogenated hydrocarbons, and this type The reaction conditions are mild, the group compatibility is good, and it has good market development prospects

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