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Solid phase synthesis of 5-aminopyrazoles and derivatives

✍ Scribed by Stephen P. Watson; Richard D. Wilson; Duncan B. Judd; Stephen A. Richards

Publisher: Elsevier Science
Year: 1997
Tongue: French
Weight: 209 KB
Volume: 38
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(97)10436-1

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✦ Synopsis

The development of a novel solid phase synthesis of some 5-aminopyrazoles and derivatives is described. Reaction of hydrazines with solid supported p-keto-nitrile (1) affords 5-aminopyrazoles (2) the amino group of which is readily acylated or sulphonylated. Generation of the solid supported 13-keto-nitrile (1) is non trivial and represents a key step in the overall synthesis.

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