1-(difluoromethyl)-1h-pyrazol-4-amine synthesis

Yield:1174309-16-0 95%

Reaction Conditions:

with palladium 10% on activated carbon;hydrogen in ethyl acetate at 20;

Steps:

Intermediate 56 1 -(difluoromethyl)pyrazol-4-amine
[00561] Intermediate 56 1 -(difluoromethyl)pyrazol-4-amine[00562] 1 -(difluoromethyl)-4-nitro-pyrazole (0 .59g, 3.Sgmmol) in EtOAc (72mL) was hydrogenatedby circulating through an H-Cube reactor using a 10% Pd/C CatCart overnight. The reaction mixturewas then concentrated in vacuo to give 1-(difluoromethyl)pyrazol-4-amine (455mg, 3.42mmol, 95% yield) as a pale yellow oil.1H NMR (CDCI3, 400MHz) O: 7.35 (2H, 5), 7.08 (1H, t, J 60.8Hz).

References:

REDX PHARMA PLC;ARMER, Richard;BELFIELD, Andrew;BINGHAM, Matilda;JOHNSON, Alice;MARGATHE, Jean-Francois;AVERY, Craig;HUGHES, Shaun;MORRISON, Angus WO2016/51193, 2016, A1 Location in patent:Paragraph 00558; 00561; 00562

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