An effective, diversity oriented,
one-pot reaction of 4-amino-2-(het)aryl/alkyl-5-functionalized
thiazoles has been disclosed, utilizing aryl/heteroaryl/alkyl dithioesters
as thiocarbonyl coupling partners in a modified Thorpe–Ziegler
type cyclization. The reaction proceeds at room temperature, under
mild conditions, in excellent yields, displaying broad functional
group compatibility at 2 and 5 positions of thiazoles. This synthetic
strategy has been further expanded for the one-pot construction of
two highly potent tubulin polymerization inhibitors, i.e., 2-(het)aryl-4-amino-5-(3,4,5-trimethoxyaroyl)
thiazoles, in high yields.
An efficient one-pot synthesis of xanthene and chromene derivatives by three-component reactions of aryl aldehydes, cyclic 1,3-diketones, and 2-naphthol/ 4-hydroxy coumarin catalyzed by ionic liquid (IL) [bmim] [PF 6 ] under microwave irradiation is described. The present scheme provides several advantages such as short reaction time, mild reaction conditions, good yields, convenient operation, and reuse of IL. In vitro antioxidant activity was evaluated for the synthesized compounds by DPPH method. Compounds 6a, 6h, 6c, 6b, 4k, and 4a showed the highest antioxidant potency.
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