| abstract |
The invention discloses a method for synthesizing axial chiral arylindole by organocatalysis: using chiral phosphoric acid as a catalyst, compound 1 and compound 2 are reacted: Wherein, R is hydrogen ; R is selected from tert-butyl, 1 -methylcyclopropyl, 1-methylcyclobutyl, tert-amyl, aryl, heteroaryl; R represents any substituent, n represents an integer from 1 to 4 , and when n is 2 or more, two or more R3s present are the same or different; R4 is selected from CO2R, and R is an alkyl or benzyl group; R5 represents any substituent , m represents an integer of 1 to 4, and when m is 2 or more, two or more R 5 present are the same or different. The synthesis method of the invention is applicable to azobenzene derivatives of various esters, obtains axial chiral arylindole with good yield and excellent enantioselectivity, and has mild reaction conditions. The method of the invention opens up a new way for organocatalytic asymmetric aryl functionalization. |