Department of Chemistry, Indian Institute of Technology, Bombay, Mumbai 400 076, India.
Org Lett. 2012 Aug 17;14(16):4070-3. doi: 10.1021/ol301695e. Epub 2012 Aug 2.
A one-pot, two-step, three-component method for the conversion of commercially available aldehydes to phosphonylpyrazoles has been developed, demonstrating, for the first time, the dual reactivity of the Bestmann-Ohira reagent (BOR) in a single-pot transformation. This method, extended to the synthesis of sulfonylpyrazoles by employing BOR in the first step and a diazomethyl sulfone in the second step, is complementary, with regard to regioselectivity, to the previous methods for the synthesis of such functionalized pyrazoles.
一种一锅、两步、三组分的方法被开发出来，用于将商业可得的醛转化为膦酰基吡唑，这首次证明了 Bestmann-Ohira 试剂（BOR）在单一锅转化中的双重反应性。这种方法通过在第一步中使用 BOR 并在第二步中使用重氮甲基砜来扩展到磺酰基吡唑的合成，在区域选择性方面与之前合成此类官能化吡唑的方法互补。
