156785-63-6Relevant articles and documents
Syntheses of Zindoxifene and Analogues by Titanium-Induced Oxo-Amide Coupling
Fuerstner, Alois,Jumbam, Denis N.,Seidel, Guenter
, p. 1125 - 1130 (2007/10/02)
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. - Key Words: Indoles, 2-aryl- / Titanium graphite / Zindoxifene / Tumor-growth inhibitors / Alkylidenation, intramolecular