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Seco compounds from the class of tylosins

机译:泰乐菌素类山高化合物

摘要

Seco compounds from a class of tylosins represented by the formula I whereinPPR stands for H or CH.sub.3,P PR. sup.1 stands for H, CH. sub.3, C.sub.1 -C.sub.3 acyl or aryl sulfonyl, PPR.sup.2 stands for H and R.sup.3 stands for NH.sub.2 or OH, or R.sup.2 and R.sup.3 together stand for O or NOH,P PR.sup.4 stands for H or C.sub.1 -C. sub.3 acyl,PPand the line - - - stands for a double or a single bond, PP and to a process for their preparation are provided.PP Oximation of 4'-demicarosyl-8a-aza-8a- homorelymycin causes breaking of the lactam to obtain a seco compound. The seco compound can be subjected to reductive N-alkylation or to conversion of the hydroxyimino group into a keto group and then optionally to N- or N,O-acylation, a catalytical hydrogenation of the double bond or a reduction of the ketone or a reduction of the hydroxyimino group into an amino group.
机译:来自式I代表的一类泰乐菌素的山高化合物,其中P P代表H或CH 3,P代表R。 sup.1代表H,CH。 sub.3,C.sub.1 -C.sub.3酰基或芳基磺酰基,

R.sup.2代表H,R.sup.3代表NH.sub.2或OH, R 2或R 3一起代表O或NOH,R 4代表H或C 1-C。 sub.3酰基,

和线---表示双键或单键,表示

及其制备方法。

4'-二去甲糖基-8a-氮杂-8a-高黏菌素引起内酰胺断裂,获得山高化合物。可以将山高化合物进行还原性N-烷基化或将羟基亚氨基转化为酮基,然后视需要进行N-或N,O-酰化,双键的催化加氢或酮或环的还原。羟基亚氨基还原成氨基。

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