Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, 215123, P. R. China.
Org Biomol Chem. 2011 Oct 21;9(20):7065-70. doi: 10.1039/c1ob05791j. Epub 2011 Aug 19.
An efficient and convenient method for the preparation of cis-bispyrimidodiazepinone derivatives has been described. A variety of substrates can participate in the process with good yields, making this methodology suitable for library synthesis in drug discovery efforts. The mechanistic course of the reaction suggests the involvement of reduction, coupling which determine the products' configuration and cyclization by one-pot.
描述了一种高效、便捷的顺式双嘧啶并二氮杂卓衍生物的制备方法。多种底物可以参与该过程，收率良好，使得该方法适用于药物发现工作中的库合成。反应的机理过程表明了还原、偶联的参与，这决定了产物的构型，并且通过一锅法实现了环化。
