Suriclone, RP-31264, 31264-RP, Suril

舒立克隆Chemical Name: 4-Methyl-1-piperazinecarboxylic acid 6-(7-chloro-1,8-naphthyridin-2-yl)-2,3,6,7-tetrahydro-7-oxo-5H-1,4-dithiino[2,3-c]pyrrol-5-yl ester; 4-Methyl-1-piperazinecarboxylic acid ester with (?-6-(7-chloro-1,8-naphthyridin-2-yl)-2,3,6,7-etrahydro-7-hydroxy-5H-p-dithiino[2,3-c]pyrrol-5-one; 6-(7-Chloro-1,8-naphthyridin-2-yl)-5-(4-methylpiperazin-1-ylcarbonyloxy)-2,3,6,7-tetrahydro-1,4-dithiino[2,3-c]pyrrol-7-one
CAS No. 53813-83-5
项目整合开发状态: Phase III
项目研究机构: Aventis Pharma (Originator)
合成路线: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.