Water → CGP-47292 methyl ester

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[N:1]([CH2:4][C:5]1[C:10]([F:11])=[CH:9][CH:8]=[CH:7][C:6]=1[F:12])=[N+:2]=[N-:3].Br[C:14](=[CH2:19])[C:15]([O:17][CH3:18])=[O:16].O>C(O)(C)(C)C>[F:12][C:6]1[CH:7]=[CH:8][CH:9]=[C:10]([F:11])[C:5]=1[CH2:4][N:1]1[CH:19]=[C:14]([C:15]([O:17][CH3:18])=[O:16])[N:3]=[N:2]1

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온도: 77.5 °C

실험 절차

A mixture of 2-(azidomethyl)-1,3-difluorobenzene in t-butanol prepared as per example 2, methyl 2-bromoacrylate (120 gms) and water (200 ml) were heated to 75-80° C. The contents was stirred at 75-80° C. for 24 hours. After the completion of reaction, the reaction mixture was cooled to room temperature. The solid obtained was filtered and then crude mass was added to cyclohexane (240 ml) and the mixture was stirred at room temperature for 2 hours. The solid was filtered and washed with cyclohexane (50 ml). The product was dried for 2 hours to give methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate. Yield: 120 gms