Metal-free Organocatalytic Alpha-amination Of Ketones With Tetrazoles

Tetrazoles and their derivatives are of importance in agrochemicals,coordination chemistry and medicinal chemistry,etc.Recently,Compounds containing the tetrazole motifs have been discovered with a wide range of biological properties,for example possessing anti-hypertensive,anti-inflammatory.Therefor,the research for these compounds has gained considerable attention by pharmaceutical chemists.Cross-dehydrogenative coupling(CDC)reactions have gained considerable attention by chemists in synthetic chemistry.Because of these reasons as follow:i)the atom and step economical.ii)the CDC protocols involving simple solvents.iii)the substrates do not require prefunctionalization or group protection.A metal-free,direct intermolecular C-N bond formation via cross-dehydrogenative coupling of various ketones with tetrazoles in the presence of TBAI as catalyst and TBHP as oxidation has been developed.The oxidative coupling of several structurally diverse alkyl ketones,acetophenones,and with phenyltetrazole gave the corresponding a-carbonyl tetrazole compounds in good to excellent yields,this protocol is a promising method for the synthesis of related pharmaceutical intermediates.