Br[C:2]1[CH:7]=[CH:6][C:5]([CH:8]2[O:13][CH2:12][CH2:11][N:10]([C:14]([O:16][C:17]([CH3:20])([CH3:19])[CH3:18])=[O:15])[CH2:9]2)=[CH:4][CH:3]=1.C([Li])CCC.CN(C)[CH:28]=[O:29]>C1COCC1>[CH:28]([C:2]1[CH:7]=[CH:6][C:5]([CH:8]2[O:13][CH2:12][CH2:11][N:10]([C:14]([O:16][C:17]([CH3:20])([CH3:19])[CH3:18])=[O:15])[CH2:9]2)=[CH:4][CH:3]=1)=[O:29]tert-Butyl 2-(4-bromophenyl)morpholine-4-carboxylate (684 mg, 2 mmol, CAS 1131220-82-0) in THF (6 ml) was cooled to −78° C., treated dropwise with n-butyllithium (1.88 ml, 3 mmol, 1.6 M solution in hexane) and stirred 30 min at −78° C. Dimethylformamide (1 ml, 2 mmol) was added dropwise and the mixture was stirred for 2 h at −78° C., and then allowed to warm up to −10° C. The reaction mixture was quenched by addition of saturated ammonium chloride solution (4 ml) and water (4 ml) and the resulting mixture was partitioned between water and ethyl acetate.
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