Abstract
With the object of synthesis of benzyl derivatives of heterocyclic amines, we have investigated the reaction of amines 1, 2, 10-12 and arylaldehydes 3, 4 in the presence of different reducing agents. The improved procedure for the reductive alkylation of heterocycle containing primary amines or heterocyclic secondary amines has been elaborated for synthesis of new benzyl derivatives 7-9 and 16-18. These benzyl amines have been obtained in 50-75% yields by direct reductive amination of arylaldehydes with sodium borohydride - acetic acid reducing system.
Highlights
Amines and their derivatives are important functionalities in various natural and synthetic biomolecules
Due to its unique biological properties the amine moiety plays a central role in chemotherapeutics of numerous diseases.[1]
The results of reductive amination of arylaldehydes with secondary heterocyclic amines (1methylpiperazine, morpholine and others) with HCOOH, NaCNBH3, NaBH4-NiCl2 as reducing agents we described earlier.[8]
Summary
Amines and their derivatives are important functionalities in various natural and synthetic biomolecules. One-pot reductive amination procedure was carried out as follows: a mixture of arylaldehyde and amine in methanol or benzene in the presence of acetic acid was stirred for one hour and sodium borohydride was added at 0 – -5 0C followed by being stirred for [10,11,12] h.
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