Tetrahydrofuran → 1-[5-(4-Methyl-5-trifluoromethyl-isoxazol-3-yl)-thiophene-2-carbonyl]piperidine-3-carboxylic acid amide

Beteiligte Stoffe

Reaktionsschritte

Prepared from 5-(5-Trifluoromethyl-4-methyl-isoxazol-3-yl)-thiophene-2-carboxylic acid and 3-piperidinecarboxamide by the method described in Example 2 Method B reversing the order of addition such that solid acid chloride was added to a THF solution of triethylamine and piperidine derivative. The reaction mixture was evaporated to a solid, triturated and filtered with the aid of water, then washed with a 1 N aqueous hydrochloric acid solution followed by water. The solid was air dried to afford product as a colorless solid (120 mg, 97%). 1H NMR (DMSO-d6) 1.36-1.49 (m, 1H), 1.55-1.75 (m, 2H), 1.89-1.93 (m, 1H), 2.35 (d, J=1.8, 3H), 3.03 (br s, 2H), 4.10 (br s, 2H), 6.90 (s, 1H), 7.37 (s, 1H), 7.51 (d, J=4.0, 1H), 7.67 (d, J=4.0, 1H). 19F NMR −62.2. LC/MS 5.54 min, [M+1]+ 388.

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