73075-67-9

Upstream product

• 73075-66-8 1,2-Dichloro-3-(2-isocyanato-ethyl)-benzene 
• 69392-63-8 3-(2,3-dichloro-phenyl)-propionyl chloride 
• 69392-62-7 methyl 2-bromo-3-(2,3-dichlorophenyl)propionate 
• 69426-58-0 methyl 3-(2,3-dichlorophenyl)propionate 
• 608-27-5 2,3-dichloroaniline 
• 57915-79-4 3-(2,3-dichlorophenyl)propionic acid 

Downstream Products

• 1302581-19-6 (S,E)-tert-butyl 4-(4-(5,6-dichloro-1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)styryl)-2,2-dimethyloxazolidine-3-carboxylate 

Relevant academic research and scientific papers

Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis: I. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines

In a search for inhibitors of epinephrine biosynthesis as potential therapeutic agents, a series of 13 ring-chlorinated 1,2,3,4-tetrahydroisoquinolines was prepared. These compounds were tested initially for their ability to inhibit rabbit adrenal phenylethanolamine N-methyltransferase (PNMT) in vitro. Enzyme-inhibitor dissociation constants, determined for the six most potent members of the series, indicated the following order of decreasing potency: 7,8-Cl2>6,7,8-Cl3>7-Cl~8-Cl>5,6,7,8-Cl4>5,7,8-Cl3. These compounds were subsequently examined for PNMT-inhibiting activity in intact rats and mice. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (SK&F 64139) was the most potent member of the series both in vitro and in vivo and is currently undergoing clinical investigation.