Ahamad Shakir, Gupta Ashis Kumar, Kant Ruchir, Mohanan Kishor
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, P.O. Box 173, Lucknow 226031, India.
Org Biomol Chem. 2015 Feb 7;13(5):1492-9. doi: 10.1039/c4ob02365j.
A mild, efficient and rapid domino reaction involving the Bestmann-Ohira reagent (BOR) and α,β-unsaturated aldehydes has been developed for the synthesis of densely functionalized vinylpyrazoles. This reaction demonstrates the dual reactivity of BOR as a homologation reagent as well as a cycloaddition partner, thus constituting a domino reaction in an operationally simple procedure. The application of this efficient synthesis of pyrazoles has been demonstrated for the synthesis of phosphonyl analogues of pyrrolopyrazole alkaloids.
已开发出一种温和、高效且快速的多米诺反应，该反应涉及贝斯曼-大平试剂（BOR）和α,β-不饱和醛，用于合成功能密集的乙烯基吡唑。此反应展示了BOR作为同系化试剂以及环加成伙伴的双重反应性，从而在操作简单的过程中构成了一个多米诺反应。这种高效的吡唑合成方法已被证明可用于合成吡咯并吡唑生物碱的膦酰类似物。
