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With (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine; In N,N-dimethyl-formamide; at 50℃; for 3h;
Example 478(S)-5-[(3-[(l,3-dimethyl-lH-pyrazol-5-yl)amino]carbonyl}phenyl)ethynyl]-N- [methyl(oxido)phenyl-lambda4-sulfanylidene]nicotinamideStep 1 N-(2,5-Dimethyl-2H-pyrazol-3-yl)-3-ethynyl-benzamide 3-Ethynylbenzoic acid (0.1 g, 0.685 mmol) was added to a dry 50 mL round bottom flask and dissolved in DMF (6.85 mL). To the resulting solution was added l,3-dimethyl-lH-pyrazol-5- amine (0.076 g, 0.685 mmol), followed by BOP (0.393 g, 0.890 mmol), and 0.238 mL of DIPEA (1.37 mmol). This reaction mixture was heated to 50 0C for 3 h. After allowing the reaction to cool to room temperature it was taken up in EtOAc (15 mL) and extracted with brine (3 x 15 mL). The EtOAc layer was then washed with saturated aqueous NaHCtheta3 (2 x 15 mL). The organics were dried over anhydrous Na2SO^8), filtered and concentrated in vacuo. The crude residue was purified via column chromatography (silica gel, gradient eluant mixture of EtOAc in Hexanes: 0% to 100% EtOAc) affording N-(l,3-dimethyl-lH-pyrazol-5-yl)-3-ethynylbenzamide (0.128 g,
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