[reaction: see text]. Alpha-carbolines are interesting core structures for designing DNA-interacting small molecules. However, these compounds are not commercially available and their synthetic methods are low yielding or time consuming. The shortest synthetic route, the modified Graebe-Ullmann reaction, has been optimized by using microwave heating in four different types of apparatus to give shorter reaction times and enhanced yields. Optimized conditions enabled the preparation of a small library of alpha-carbolines.

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Fused pyridine derivatives R 0450An Improved Synthesis of α-Carbolines under Microwave Irradiation. -Synthesis of α-carbolines from benzotriazoles and azines bearing a leaving group at the C-2 position through the modified Graebe-Ullmann reaction is performed more efficiently and more rapidly using microwave irradiation. -(VERA-LUQUE, P.; ALAJARIN*, R.; ALVAREZ-BUILLA, J.; VAQUERO, J. J.; Org. Lett. 8 (2006) 3, 415-418; Dep. Quim. Org., Univ. Alcala, E-28871 Alcala de Henares, Madrid, Spain; Eng.) -R. Steudel 24-152

VERA-LUQUE, P.; ALBERICIO, F.; ALVAREZ*, M.; J. Comb. Chem. 9 (2007) 4, 521-565; Inst. Res. Biomed.,