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. 2014 Jan 13;16(3):832–835. doi: 10.1021/ol4035947

Scheme 2. Scope of 4- and 3-Bromo-1H-pyrazoles Coupling with Aliphatic, Aromatic, and Heteroaromatic Amines.

Scheme 2

Reaction conditions: HetArBr (1.0 mmol), amine (1.2 mmol), LHMDS (2.2 mmol). Isolated yields are an average of two runs.

P4 (1 mol %), L4 (1 mol %), 50 °C.

P4 (2 mol %), L4 (2 mol %), 80 °C.

12 h.

Amine (1.4 mmol).

16 h.

P4 (4 mol %), L4 (4 mol %).