A new two-step, one-pot alternative protocol for preparation of 1H-pyrazole-5-amines from 3-oxoalkanenitriles utilizing readily available acetylhydrazine has been developed. Typical by-products formed in traditional reactions of 3- oxoalkanenitriles with hydrazine are not formed when the present method is used, thus facilitating purification on a large scale. The method was used to prepare a medicinally important heterocycle on a kilogram scale.
Keywords: 3-oxoalkanenitriles, acetylhydrazine, aminopyrazoles, kilogram scale, process chemistry
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