反应详情

The procedure of Example 14 is followed but starting with 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(piperazin-1-yl)carbonyloxy-isoindolin-1-one (4.23 g.), N,N'-dicyclohexylcarbodiimide (3.1 g.) in anhydrous methylene chloride (100 cc.) and cyclohexylcarboxylic acid (1.92 g.). After having filtered off the precipitate, the organic solution is washed with an 8% aqueous solution of sodium bicarbonate (20 cc.) and then dried over anhydrous potassium carbonate (10 g.). After the solution has been filtered and the filtrate concentrated to dryness, the residue is recrystallised from ethanol (300 cc.). 2-(7-Chloro-1,8-naphthyridin-2-yl)-3-(4-cyclohexylcarbonylpiperazin-1-yl)carbonyloxy-isoindolin-1-one (3.7 g.), which melts at 240° C., is thus obtained.

1. filtrationAfter having filtered off the precipitate
2. washthe organic solution is washed with an 8% aqueous solution of sodium bicarbonate (20 cc.)
3. dry with materialdried over anhydrous potassium carbonate (10 g.)
4. filtrationAfter the solution has been filtered
5. concentrationthe filtrate concentrated to dryness
6. customthe residue is recrystallised from ethanol (300 cc.)