60946-74-9Relevant academic research and scientific papers
Enantioselective Formal C(sp3)?H Bond Activation in the Synthesis of Bioactive Spiropyrazolone Derivatives
Li, Houhua,Gontla, Rajesh,Flegel, Jana,Merten, Christian,Ziegler, Slava,Antonchick, Andrey P.,Waldmann, Herbert
supporting information, p. 307 - 311 (2018/12/13)
Herein, we report the first enantioselective annulation of α-arylidene pyrazolones through a formal C(sp3)?H activation under mild conditions enabled by highly variable RhIII-Cpx catalysts. The method has a wide substrate scope and proceeds with good to excellent yields and enantioselectivities. Its synthetic utility was demonstrated by the late-stage functionalization of drugs and natural products as well as the preparation of enantioenriched [3]dendralenes. Preliminary biological investigations also identified the spiropyrazolones as a novel class of Hedgehog pathway inhibitors.
A convenient microwave-assisted propylphosphonic anhydride (T3P mediated one-pot pyrazolone synthesis
Desroses, Matthieu,Jacques-Cordonnier, Marie-Caroline,Llona-Minguez, Sabin,Jacques, Sylvain,Koolmeister, Tobias,Helleday, Thomas,Scobie, Martin
supporting information, p. 5879 - 5885 (2013/09/23)
This paper describes a facile, efficient, and clean synthesis of various pyrazolones by employing T3P as a catalyst and performing the reaction under microwave irradiation. This two-step, one-pot reaction proceeded readily and tolerated a variety of functional groups. A wide range of pyrazolone derivatives were obtained in good to excellent yields. A one-pot, two-step procedure for the synthesis of pyrazolones is presented. This method, which uses T3P and microwave irradiation, is particularly easy to carry out and offers a notable alternative to the strongly acidic conditions that are generally employed with other synthetic approaches. Copyright
