4-(4-CHLOROTHIAZOL-2-YL)MORPHOLINE synthesis

Yield:848841-68-9 76%

Reaction Conditions:

with potassium carbonate in acetonitrile at 40; for 0.5 h;Heating / reflux;

Steps:

19

Preparation 194-chloro-2-morpholino-thiazoleTo a mixture of 2,4-dichlorothiazole (34 g, 0.22 mol) in acetonitrile (425 mL) add potassium carbonate (60.9 g, 0.44 mol) and then morpholine (21.2 mL, 0.225 mol) dropwise over 30 min. Reflux the mixture at 40 ⁰C and then cool to 22 °C. Filter the mixture and evaporate the filtrate. Triturate the residue with /-propyl alcohol (60 mL) at 22 ⁰C for one hour. Filter the solids and dry under vacuum to a constant weight to afford the title compound (34.5 g, 76%). ES/MS m/z (³⁵Cl) 205 (M+l)⁺.

References:

WO2008/36579,2008,A1 Location in patent:Page/Page column 37