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We report a procedure—economical method for the highly enantioselective and protecting-group free total syntheses of nonpeptidal CCK antagonists asperlicins C and E. Starting from l-tryptophan, the synthesis of asperlicin C has been achieved in three steps, which features the low-valent titanium (LVT: TiCl4–Zn combination)-mediated reductive cyclization of o-nitrobenzamide to construct the (3H)-quinazolin-4-one...
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