Synfacts 2006(11): 1104-1104  
DOI: 10.1055/s-2006-949412
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart · New York

A Classical but Short One-Pot Synthesis of Pyrazoles

Contributor(s): Victor Snieckus, Heiko Scharl
S. T. Heller*, S. R. Natarajan
Merck Research Laboratories, Rahway, USA
Further Information

Publication History

Publication Date:
24 October 2006 (online)

Significance

Pyrazoles are a bread-and-butter class of heterocycles of the pharmaceutical industry (see book below). The reported method uses a conventional synthesis of 1,3-dicarbonyl derivatives, easily accessible ketones and acid chlorides, followed by hyrazinolysis, to deliver a range of pyrazoles in moderate to good yields. A broad scope, especially with respect to aryl substituents R1 and R2, was established.