1,3-Dimethyl-1H-pyrazol-5-amine → 2-(2-(1,3-dimethyl-1H-pyrazol-5-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-6-methoxy-N-methylbenzamide

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

_2-(2-chloro-5-(trifluoromethyl)pyridin-4-ylamino)-6-methoxy-N-methylbenzamide (1.66 g, 4.61 mmol)_ _,_ _1,3-dimethyl-1H-pyrazol-5-amine (0.523 g, 4.71 mmol)_ _,_ _diacetoxypalladium (0.083 g, 0.37 mmol)_ _,_ _(9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (0.427 g, 0.74 mmol)_ _and_ _cesium carbonate (1.804 g, 5.54 mmol)_ _were mixed together in_ _dioxane (30 mL)_ _. Reaction was degassed with argon and was stirred at_ _90 °C_ _for 3 hours under argon.The mixture was filtered ,the filtrate was concentrated and purified by flash chromatography on silica gel 15-40µm eluting with __0_ _to_ _4_ _% methanol in CH2Cl2/AcOEt (60/40).The product obtained was not enough pure so the product was repurified by flash chromatography on silica gel 15-40µm eluting with 0 to 4% methanol in CH2Cl2/AcOEt (60/40).The solvent was evaporated to dryness to afford _2-(2-(1,3-dimethyl-1H-pyrazol-5-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-6-methoxy- N-methylbenzamide (0.882 g, 44.0 %) _as a _beige __ solid _._ _EN 02814-27-01_

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