A facile two-step sequence (9→ 10→ 1) of regioselective assembly of 3, 4- dihydroisoquinoline derivatives 1 is reported. The halogen derivatives provide opportunity for Suzuki, Buchwald, and related coupling reactions useful for expanding the scaffold and lead optimization in drug discovery.
[Augelli-Szafran, Corinne E.; Jaen, Juan C.; Moreland, David W.; Nelson, Carrie B.; Penvose-Yi, Jan R.; Schwarz, Roy D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1991 - 1996]
[Augelli-Szafran, Corinne E.; Jaen, Juan C.; Moreland, David W.; Nelson, Carrie B.; Penvose-Yi, Jan R.; Schwarz, Roy D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1991 - 1996]