反应详情

4-Methoxy-7-(tetrahydro-pyran-4-yl)-benzothiazol-2-ylamine (69 mg, 0.26 mmol) is first reacted with phenyl chloroformate as described for (4-methoxy-7-phenyl-benzothiazol-2-yl)-carbamic acid benzyl ester in WO01/97786 and then with N-ethyl-diisopropylamine (0.090 ml, 0.52 mmol) and (trans)-cyclohexane-1,4-diol (60 mg, 0.52 mmol) in dimethyl sulfoxide (10 ml) at 50° C. for 2 h. Then 100 ml dichoromethane are added, the mixture is extracted with saturated aqueous sodium carbonate and the organic phase is dried and evaporated. Flash-chromatographic purification (silica, eluting with dichloromethane/methanol) yielded the title compound as white solid (7% yield). MS: m/e=407(M+H+), mp 282-284° C. Following the general method of example 1 the compounds of examples 2 to 11 were prepared.

1. extractionthe mixture is extracted with saturated aqueous sodium carbonate
2. customthe organic phase is dried
3. customevaporated
4. customFlash-chromatographic purification (silica, eluting with dichloromethane/methanol)