The formation of 2-benzyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline through stepwise synthesis reactions involving homoveratrylamine and p-nitro-, m-bromo-, o-methoxybenzaldehyde is described. The reaction stages include imine formation using a Dean-Stark apparatus, reduction in the presence of sodium borohydride, and cyclization in the subsequent stage in the presence of formalin and concentrated hydrochloric acid. The structure of the products was determined based on 1H NMR spectral results. This work is significant for the efficient synthesis of isoquinoline derivatives and obtaining their pharmacologically promising analogues.