4.4 Article

Construction of highly substituted pyrazole derivatives with P-C bond: access to racemic and enantioselective forms by conjugate addition of diarylphosphane oxides to α,β-unsaturated pyrazolones

期刊

TETRAHEDRON
卷 70, 期 2, 页码 417-426

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2013.11.038

关键词

Diarylphosphane oxide; alpha,beta-Unsaturated pyrazolone; Catalyst-free; Organo-catalysis; Isosteviol derived thiourea

资金

  1. National Natural Science Foundation of China [21072145, 21272166]
  2. Program for New Century Excellent Talents in University [NCET-12-0743]
  3. Major Basic Research Project of the Natural Science Foundation of the Jiangsu Higher Education Institutions [13KJA150004]
  4. Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)

向作者/读者索取更多资源

The synthesis of organophosphorus compounds is of great importance to industrial, agricultural, and pharmaceutical chemistry. In this paper, we have reported the synthesis of highly substituted pyrazole derivatives through P-C bond formation under catalyst-free conditions. On the other hand, the first catalytic asymmetric version of this reaction has also been developed under catalysis by an isosteviol derived thiourea organocatalyst. The optically active phosphorus-containing compounds have been obtained in good chemical yields with moderate enantioselectivities. (C) 2013 Elsevier Ltd. All rights reserved.

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