4.4 Article

One-pot to fused pyrazoles by a double cyclization of o-alkynylaldehydes with ketones and hydrazine under metal-free condition

Journal

TETRAHEDRON
Volume 70, Issue 24, Pages 3782-3787

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2014.04.032

Keywords

One-pot synthesis; Pyrazoles; o-Alkynylaldehydes; Ketones; Hydrazine

Funding

  1. National Natural Science Foundation of China [91017005, 81172935, 81373255]
  2. Key Project of Ministry of Education [313040]
  3. Hubei Province's Outstanding Medical Academic Leader Program

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An efficient one-pot synthesis of fused pyrazoles has been developed. The procedure involved three components reaction of o-alkynylaldehydes 1a-s with ketones 2a-m and hydrazine under mild, metal-free reaction conditions. The desired products were obtained in one-step up to 85% yield. The molecular structure was confirmed by the X-ray crystallographic analysis. (C) 2014 Elsevier Ltd. All rights reserved.

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