The cyclization of 5,6-dihydro-1,4-dithiine-2,3-dicarboxylic acid anhydride (I) with 2-amino-7-hydroxy-1,8-naphthyridine (II) by means of acetic acid in refluxing diphenyl-diphenyl ether gives 6-(7-hydroxy-1,8-naphthyridin-2-yl)-2,3,6,7-tetrahydro-1,4-dithiino[2,3-c]pyrrole-5,7-dione (III), which is treated with POCl3 in hot DMF to yield 6-(7-chloro-1,8-naphthyridin-2-yl)-2,3,6,7-tetrahydro-1,4-dithiino[2,3-c]pyrrole-5,7-dione (IV). The reduction of (IV) with NaBH4 in methanol affords 6-(7-chloro-1,8-naphthyridin-2-yl)-5-hydroxy-2,3,6,7-tetrahydro-1,4-dithiino[2,3-c]pyrrol-7-one (V), which is finally condensed with 1-chlorocarbonyl-4-methylpiperazine (VI) by means of NaH in DMF.