Asymmetric Total Synthesis of (-)-Cribrostatin 4 (Renieramycin H)

摘要

The tetrahydroisoquinoline family of alkaloids that include the renieramycins (1, 2 a-c), ecteinascidin-743 (Et-743, 3), jorumycin (4), saframycins (5 a-c), safracins (6 a-b), bioxalomycins (7 a-b), quinocarcin (8), and tetrazomine (9, Scheme 1) has attracted significant attention from the synthetic community over the past 30 years because of the potent antitumor and antimicrobial activities that this family of agents displays.[1] Among them, Et-743 (3) is a highly potent antitumor agent which is currently in phase II/III human clinical trials.