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 (2.12 g.), N,N'-dicyclohexylcarbodiimide (2.05 g.) in anhydrous methylene chloride (50 cc.) and trifluoroacetic acid (1.71 g.). The crude product, after it has been filtered off, is washed with diethyl ether (50 cc.). The product is then dissolved in methylene chloride (110 cc.). The solution is filtered and concentrated to dryness and the residue is washed again with diethyl ether (45 cc.). 2-(7-Chloro-1,8-naphthyridin-2-yl)-3-(4-trifluoroacetylpiperazin-1-yl)carbonyloxy-isoindolin-1-one (0.91 g.), which melts at 218° C., is thus obtained.

1. filtrationThe crude product, after it has been filtered off
2. washis washed with diethyl ether (50 cc.)
3. dissolutionThe product is then dissolved in methylene chloride (110 cc.)
4. filtrationThe solution is filtered
5. concentrationconcentrated to dryness
6. washthe residue is washed again with diethyl ether (45 cc.)