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NOVEL OPTICALLY PURE CAMPTOTHECIN ANALOGS, A NEW OPTICALLY PURE SYNTHESIS INTERMEDIATE AND PROCESS FOR PREPARING THE SAME
NOVEL OPTICALLY PURE CAMPTOTHECIN ANALOGS, A NEW OPTICALLY PURE SYNTHESIS INTERMEDIATE AND PROCESS FOR PREPARING THE SAME
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机译:新型光学纯喜树碱类似物,一种新型光学纯合成中间体,用于制备相同的
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摘要
Two optically pure beta-hydroxy lactone camptothecin analogs (+)-5-ethyl-9,10-difluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-b)quinoline-3,15-dione (I) and (+)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-(4-methylpiperidinomethyl)-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-c)quinoline-2,15-dione (II), as well as one of its salts, (+)-1-(9-chloro-5-ethyl-5-hydroxy-10-methyl-3,15-dioxo-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-b)quinoline-12-yl methyl)-4-methyl-hexahydropyridinium chloride (III) and intermediates (M) are new. Optically pure beta-hydroxy lactone camptothecin analogs of formulae (I) and (II), as well as salts of (II) of formulae (III) are new. Independent claims are also included for industrial intermediates of formula (M) and their preparation. R = 1-10C alkyl, especially ethyl.
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机译:两个光学纯的β-羟基内酯喜树碱类似物(+)-5-乙基-9,10-二氟-5-羟基-4,5,13,15-四氢-1H,3H-氧代庚烷(3',4':6 ,7)吲哚并ino(1,2-b)quinoline-3,15-dione(I)and(+)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-(4-methylpiperidinomethyl)- 4,5,13,15-四氢-1H,3H-oxepino(3',4':6,7)吲哚并(1-2,c)喹啉-2,15-二酮(II)以及其盐,(+)-1-(9-氯-5-乙基-5-羟基-10-甲基-3,15-二氧代-4,5,13,15-四氢-1H,3H-氧杂环丁烷(3' ,4':6,7)吲哚并(1,2-b)喹啉-12-甲基)-4-甲基-六氢吡啶鎓氯化物(III)和中间体(M)是新的。式(I)和(II)的光学纯的β-羟基内酯喜树碱类似物以及式(III)的(II)的盐是新的。式(M)的工业中间体及其制备也包括独立权利要求。 R = 1-10C烷基,尤其是乙基。
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