首页>
外国专利>
Process for the preparation of EPIPODOPHYLOTOXIN GLUCOSIDE 4'-PHOSPHATE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THAT CONTAINS THEM
Process for the preparation of EPIPODOPHYLOTOXIN GLUCOSIDE 4'-PHOSPHATE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THAT CONTAINS THEM
展开▼
机译：制备EPIPODOPHYLOTOXIN葡糖苷4'-磷酸酯衍生物和包含它们的药物组合物的方法
展开▼
页面导航
摘要
著录项
相似文献
摘要
Phosphorus-contg. derivs. of 4'-demethyl epipodophyllotoxin glucosides of formula (I) and pharmaceutically acceptable salts are new, where R1 and R6 together complete a 5-6C cycloalkyl gp.; or R1, R6 = 1-8C alkyl; or R6 = H; and R1 = 1-10C alkyl, 2-10C alkenyl, 5-6C cycloalkyl, 2-furyl, 2-thienyl, 6-10C aryl, 7-14C aralkyl or 8-14C aralkanyl, where the aromatic rings are opt. substd. by halogen, 1-8C alkyl, 1-8C alkoxy, OH, NO2 and/or NH2 gp(s).; Q = -P(:X)(OR7)(OR8) or -P(:X)(Y)(NR2R3); X = O or S; R7, R8 = H, 1-5C alkyl (opt. substd. by A), 3-6C cycloalkyl (opt. substd. by A), 6-10C aryl, A-substd. aryl, alkaryl, 7-14C aralkyl, A-substd. aralkyl or alkyl-substd. aralkyl; A = 1 or more of OH, alkoxy, alkanoyloxy, CN, NH2, mono-or dialkylamino, carboxy, alkylthio, SH, mercaptothio, nitropyridyl disulphide, alkanoylamino, alkanoyl, carbamoyl, NO2 and halogen; Y = Cl, OH or NR4R5; R2-5 = H, 1-5C alkyl (opt. substd. by A); or NR2R3 and/or NR4R5 = 3-6 membered ring. Also new are intermediates (II), of formula (I) where Q = -P(:X)Cl2.
展开▼
机译：含磷量。派生。式（I）的4′-去甲基表鬼臼毒素葡糖苷和药学上可接受的盐是新的，其中R 1和R 6一起完成5-6C环烷基gp。或R 1，R 6 ＝ 1-8C烷基;或R6 = H; R 1 ＝ 1-10C烷基，2-10C烯基，5-6C环烷基，2-呋喃基，2-噻吩基，6-10C芳基，7-14C芳烷基或8-14C芳烷基，其中芳族环是优选的。取代通过卤素，1-8C烷基，1-8C烷氧基，OH，NO 2和/或NH 2 gp。 Q = -P（：X）（OR7）（OR8）或-P（：X）（Y）（NR2R3）; X = O或S; R 7，R 8 ＝ H，1-5C烷基（A取代），3-6C环烷基（A取代），6-10C芳基，A取代。芳基，烷芳基，7-14 C芳烷基，A-取代。芳烷基或烷基取代的。芳烷基; A ＝ 1或1以上的OH，烷氧基，烷酰氧基，CN，NH 2，单或二烷氨基，羧基，烷硫基，SH，巯基硫，硝基吡啶基二硫化物，烷酰氨基，烷酰基，氨基甲酰基，NO 2和卤素; Y = Cl，OH或NR4R5; R2-5 ＝ H，1-5C烷基（被A取代）;或NR2R3和/或NR4R5 = 3-6元环。式（I）的中间体（II）也是新的，其中Q ＝ -P（：X）Cl 2。
展开▼
