首页> 外国专利> FOERFARANDE Før FRAMSTAELLNING OF 1-N-substituted derivate audio 4,6-DI (AMINOGLYKOSYL) -1,3-DIAMINOCYKLITOLERNA Gentamicin B Gentamicin C1 Gentamicin C1A sisomicin verdamicin Antibiotic JI-20B, Antibiotic G-52 MUTAMICIN 2 OCH MUTAMICIN 6

FOERFARANDE Før FRAMSTAELLNING OF 1-N-substituted derivate audio 4,6-DI (AMINOGLYKOSYL) -1,3-DIAMINOCYKLITOLERNA Gentamicin B Gentamicin C1 Gentamicin C1A sisomicin verdamicin Antibiotic JI-20B, Antibiotic G-52 MUTAMICIN 2 OCH MUTAMICIN 6

机译：制备1-N-取代的衍生物音频4,6-DI（酰胺基糖基）-1,3-二氨基环丁酸之前的步骤庆大霉素B庆大霉素C1庆大霉素C1A西索霉素维达霉素抗生素JI-20B，抗生素G-52突变霉素2

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1473733 Pseudo trisaccharides SCHERICO Ltd 1 Aug 1974 [6 Aug 1973 19 March 1974 (2)] 33968/74 Heading C2C The invention comprises 1-N substituted derivatives of the 4,5-di-(aminoglycosyl)-1,3- diaminocyclitols gentamicin A, gentamicin B, gentamicin B 1 , gentamicin C 1 , gentamicin C 1a , gentamicin C 2 , gentamicin C 2a , gentamicin C 2b , gentamicin X 2 , sisomicin, vendamicin, tobramycin, Antibiotic G-418, Antibiotic 66-40B, Antibiotic 66-40D, Antibiotic J1-20A, Antibiotic J1-20B, Antibiotic G-52, mutamicin 1, mutamicin 2, mutamicin 4, mutamicin 5 and mutamicin 6, where the substituent is -CH 2 X with X being hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, aminoalkyl, N-alkylaminoalkyl, aminohydroxyalkyl, N-alkylaminohydroxyalkyl, phenyl, benzyl or tolyl, said aliphatic radicals having up to seven carbon atoms and, if substituted by amino and hydroxy, bearing the substituents on different C atoms and pharmaceutically acceptable acid addition salts thereof. The compounds of the invention may be prepared by treating one of the above named 4,6-di-(aminoglycosyl)-1,3- diaminocyclitols which may have aminoprotecting groups at any position other than position 1, with an aldehyde of formula XSP1/SP-CHO, with XSP1/SP being a group as defined for X above wherein any amino or hydroxy group present may be protected in the presence of a hydride donor and reducing agent and, if required, removing all protecting groups present in the molecule the last process step being followed by isolating the derivative as such or as a pharmaceutically acceptable acid addition salt.

机译：1473733伪三糖SCHERICO Ltd 1974年8月1日[1973年8月6日（1974）（2）] 33968/74标题C2C本发明包含4，5-二-（氨基糖基）-1,3-二氨基环糖醇庆大霉素的1-N取代衍生物。 A，庆大霉素B，庆大霉素B 1，庆大霉素C 1，庆大霉素C 1a，庆大霉素C 2，庆大霉素C 2a，庆大霉素C 2b，庆大霉素X 2，西索米星，芬达霉素，妥布霉素，抗生素G-418，抗生素66-40B，抗生素66-40D，抗生素J1-20A，抗生素J1-20B，抗生素G-52，mutamicin 1，mutamicin 2，mutamicin 4，mutamicin 5和mutamicin 6，其中取代基为-CH 2 X，X为氢，烷基，烯基环烷基，环烷基烷基，羟基烷基，氨基烷基，N-烷基氨基烷基，氨基羟基烷基，N-烷基氨基羟基烷基，苯基，苄基或甲苯基，所述脂族基具有至多七个碳原子，并且如果被氨基和羟基取代，则在不同的C原子上带有取代基及其药学上可接受的酸加成盐。本发明的化合物可以通过用式X ＜的醛处理上述4，6-二-（氨基糖基）-1，3-二氨基环醇中的一种来制备，所述4，6-二-（氨基糖基）-1，3-二氨基环醇可以在除位置1以外的任何位置具有氨基保护基。 SP> 1 -CHO，其中X 1 是上面X所定义的基团，其中存在的任何氨基或羟基可在氢化物供体和还原剂的存在下得到保护，如果需要的话，除去分子中存在的所有保护基，最后一个工艺步骤是分离衍生物本身或药学上可接受的酸加成盐。

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公开/公告号FI62100B

专利类型
公开/公告日1982-07-30

原文格式PDF
申请/专利权人 OY KOLSTER AB;
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申请/专利号FI19740002304
发明设计人 WEINSTEIN MARVIN JOSEPH;DANIELS PETER JOHN LOVELL;WAGMAN GERALD HOWARD;TESTA RAYMOND;MALLAMS ALAN KEITH;WRIGHT JOHN JESSEN;NAGABHUSHAN TATTANAHALLI LAKSHMINARAYAN;
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申请日1974-08-01
分类号C07H15/22;
国家 FI
入库时间 2022-08-22 13:47:49

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