反应详情

939 mg (3.0 mmol) of tert-butyl 4-(5-carboxythiazol-2-yl)piperazine-1-carboxylate [Precursor BBB61] were dissolved in DMF (15 ml) together with 534 mg (3.3 mmol) of CDI and the solution was stirred at RT 4 h. Subsequently, 243 mg (3.3 mmol) of N-hydroxyacetamidine were added and the mixture was stirred at 120° C. a further 4 h. The reaction solution was then poured onto water and the resulting precipitate was filtered off and washed with water. By means of CC (DCE/ethanol mixture) of the residue, 220 mg (0.63 mmol, 21%) of tert-butyl 4-[5-(3-methyl-[1,2,4]-oxadiazol-5-yl)-thiazol-2-yl]piperazine-1-carboxylate were obtained.

1. stirringthe mixture was stirred at 120° C. a further 4 h
2. additionThe reaction solution was then poured onto water
3. filtrationthe resulting precipitate was filtered off
4. washwashed with water