Solid-phase synthetic method of amantadine derivative
2013
The invention provides a solid-phase organic synthetic method used for preparing arylamine, hetero arylamine or polynitrogen azole substituted amantadine derivative III by reacting amantadine derivative I with arylamine, hetero arylamine or polynitrogen azole. The reaction equation is represented in the invention, wherein R1, and R2 represent hydrogen, alkyl and polynitrogen azole; X represents Cl, Br and I; amine comprises arylamine and hetero arylamine compounds; and azole comprises polynitrogen azole compounds. Solid-phase organic synthetic grinding method is employed. At room temperature and in the absence of solvents, the one-step reaction is capable of realizing saturation of amantadine and direct amination of C-H bands so as to obtain the amantadine derivative. The solid-phase synthetic method possesses high atom efficiency, selectivity, and yield, and is simple and safe for operation; and no waste solvent is caused.
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