首页> 外国专利> still for framstellning of 1n - (alpha - hydroxy - omega - amino - alkanoyl) - 6 721n - methyl - 3 721, 4 721 - dideoxikanamycin b or pharmaceutically acceptable syraadditionssalter derav

still for framstellning of 1n - (alpha - hydroxy - omega - amino - alkanoyl) - 6 721n - methyl - 3 721, 4 721 - dideoxikanamycin b or pharmaceutically acceptable syraadditionssalter derav

机译:仍用于1n-(α-羟基-ω-氨基-烷酰基)-6 721n-甲基-3 721,4 721-双脱氧卡那霉素b或药学上可接受的syraadditionssalter derav

摘要

1-N-(alpha-hydroxy-omega-aminoalkanoyl)-6'-N-methyl-3',4'-dideoxyka namycins B or pharmaceutically acceptable acid addition salts thereof are prepared by selective acylation of the 1-amino group of an amino-protected derivative of the formula IMAGE in which R1 is a monovalent amino protective group and R2 is hydrogen or a monovalent amino protective group, with an alpha -hydroxyomega -amino acid of the formula V or with a functional derivative thereof, in which n is 1, 2 or 3, R3 is an amino protective group and R4 is hydrogen, or R3 and R4 together are a divalent amino protective group, after which the amino protective groups are eliminated from the 1-N-acylated product obtained in this way. The prepared compounds are effective not only against Gram-negative and Gram-positive bacteria with the usual kanamycin sensitivity but also against kanamycin-resistant bacteria. IMAGE
机译:1-N-(α-羟基-ω-氨基链烷酰基)-6'-N-甲基-3',4'-二脱氧卡那霉素B或其药学上可接受的酸加成盐是通过选择性酰化甲壳素的1-氨基而制得的在式的氨基保护的衍生物中,R1是式V的α-羟基ω-氨基酸或其官能衍生物,其中R1是单价氨基保护基,R2是氢或一价氨基保护基。其中n是1、2或3,R3是氨基保护基,R4是氢,或R3和R4一起是二价氨基保护基,然后从得到的1-N-酰化产物中除去氨基保护基。这条路。所制备的化合物不仅对具有卡那霉素敏感性的革兰氏阴性和革兰氏阳性细菌有效,而且对卡那霉素抗性细菌有效。 <图像>

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