“…In particular, 1,2-dihydroisoquinoline derivatives act as delivery systems that transport drugs through the otherwise highly impermeable blood-brain barrier [4,5]. Isoquinoline derivatives also exhibit sedative [6], antidepressant [7,8], antitumor, and antimicrobial activities [9 -11]. Here we describe an efficient one-pot and method for the synthesis of 1,2-disubstituted 1,2-dihydroisoquinoline derivatives via the reaction of isoquinoline (1), a dialkyl acetylenedicarboxylate 3 and a N-phenylcarbamate 2 under solvent-free conditions at room temperature (Scheme 1).…”