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Free keywords:
Indoles, 2-aryl-; Titanium graphite; Zindoxifene; Tumor-growth inhibitors; Alkylidenation, intramolecular
Abstract:
Highly reactive titanium on graphite is used to reductively cyclize electron-rich acylamino carbonyl compounds 7, 8, 12, 14, and 16 to the corresponding indole derivatives 9, 10, 13, 15, and 17. Compound 9b is a known precursor of the mammary tumor-inhibiting compound zindoxifene (2). The other products are new analogues of this anticancer drug, exhibiting the substitution pattern previously recognized to be essential for high pharmacological activity.
