Reaktion #659463

Reaktionsgleichung

5-(4-Methyl-5-trifluoromethyl-isoxazol-3-yl)-thiophene-2-carboxylic acid

4-hydroxypiperidine

→

product

Ausbeute 78.0%

(4-Hydroxy-piperidin-1-yl)-[5-(4-methyl-5-trifluoromethyl-isoxazol-3-yl)-thiophen-2-yl]-methanone

Ausbeute 78.0%

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe reaction mixture was evaporated to a solid
2. 2
   Sonstigetriturated
3. 3
   Filtrationfiltered with the aid of water
4. 4
   Waschenwashed with a 1 N aqueous hydrochloric acid solution
5. 5
   Sonstigedried

Vorschrift

Prepared from 5-(4-Methyl-5-trifluoromethyl-isoxazol-3-yl)-thiophene-2-carboxylic acid and 4-hydroxypiperidine by the method described in Example 2 Method B. 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 (141 mg, 78%). 1H NMR (CDCl3) 1.58-1.69 (m, 2H), 1.93-2.00 (m, 2H), 2.26 (br s, 1H), 2.37 (s, 3H), 3.44-3.52 (m, 2H), 4.00-4.12 (m, 3H), 7.33 (d, J=4.0, 1H), 7.46 (d, J=3.5, 1H). 13C NMR 7.9, 34.4, 42 (br), 66.9, 114.8, 118.7 (q, J=271), 128.0, 129.2, 131.2, 140.1, 155.2 (q, J=40), 158.1, 162.8. 19F NMR −63.1. LC/MS 5.71 min, [M+1]+ 361.

Quelle