
Tetrahedron Letters p. 9065 - 9068 (1997)
Update date:2022-08-05
Topics: Cyclization Purification and Analysis Fmoc Deprotection
Watson, Stephen P.
Wilson, Richard D.
Judd, Duncan B.
Richards, Stephen A.
The development of a novel solid phase synthesis of some 5-aminopyrazoles and derivatives is described. Reaction of hydrazines with solid supported β-keto-nitrile (1) affords 5-aminopyrazoles (2) the amino group of which is readily acylated or sulphonylated. Generation of the solid supported β-keto-nitrile (1) is non trivial and represents a key step in the overall synthesis.
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