Synthesis and Biological Evaluation of Pyridooxazine-Tetrahydroisoquinoline Derivatives as MDR Modulators
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Pyridooxazine–tetrahydroisoquinoline derivatives were designed and synthesized for MDR modulating activity. Pyridooxazin-2-one scaffolds were constructed in a one-pot annulation of <I>N</I>-substituted-2-chloroacetamides with 2-bromo-3-hydroxy pyridine via Smiles rearrangement. The Pictet–Spengler cyclization to form tetrahydroisoquinoline ring afforded target compounds in 17–37% overall yields. Some of these compounds exhibited multidrug resistance (MDR) reversing activity.
- Chemistry Letters
Chemistry Letters 35(9), 1010-1011, 2006-09-05
The Chemical Society of Japan