反应详情

1-(2′-Acetylaminobiphenyl-4-ylmethyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-carboxylic acid tert-butyl ester 17 was synthesized by the Suzuki coupling of 1-(4-bromobenzyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-carboxylic acid tert-butyl ester 1 with 2-acethylaminophenylboronic acid 16 using Palladium(II) acetate, triphenylphosphine, and Na2CO3 in anhydrous isopropanol. Reaction of compound 17 with 2 M HCl solution in diethylether yielded N-[4′-(6,7-dimethoxy-1,2,3,4-tetrahydro-isoquinolin-1-ylmethyl)-biphenyl-2-yl]acetamide hydrochloride salt 18 (Scheme-5).