反应详情

To a suspension of the product of example 10 part a) (0.130 mg) and (4R)-4-methyl-4-isoxazolidinol hydrochloride (42 mg, prepared by the method of example 1 steps a) to d) using [(2R)-2-methyloxiran-2-yl]methyl 3-nitrobenzenesulfonate) in anhydrous THF (6 ml), was added triethylamine (120 mg) and the mixture was cooled in an icebath. O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetamethyluronium hexafluorophosphate (120 mg) was added and the mixture was allowed to warm to, whereupon it was stirred for 3 hr. All volatiles were removed in vacuo and the residue was chromatographed (SiO2/1:1 CH2Cl2-EtOAc) to effect primary purification. Further purification by RPHPLC afforded the title compound as a solid (35 mg).

1. customprepared by the method of example 1 steps a)
2. temperaturethe mixture was cooled in an icebath
3. temperatureto warm to, whereupon it
4. customAll volatiles were removed in vacuo
5. customthe residue was chromatographed (SiO2/1:1 CH2Cl2-EtOAc)
6. custompurification
7. customFurther purification by RPHPLC