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J Org Chem. 2015 Jun 19;80(12):6509-14. doi: 10.1021/acs.joc.5b00796. Epub 2015 Jun 05.

Synthesis of Spirocyclic Pyrazolones by Oxidative C-N Bond Formation.

The Journal of organic chemistry

Javier Agejas, Laura Ortega

Affiliations

  1. Centro de Investigación Lilly S.A., Avda. de la Industria, 30, Alcobendas, Madrid 28108, Spain.

PMID: 26018762 DOI: 10.1021/acs.joc.5b00796

Abstract

The two-step synthesis of spirocyclic pyrazolone derivatives from simple and commercially available reagents is described. The unusual reaction of 1,3-dicarbonyls with hydrazines and an iodine-mediated oxidative carbon-nitrogen bond formation, joined in a two-step, one-pot reaction, allows the straightforward synthesis of these spirocycles.

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