at corresponding meanings of radicals or pharmaceutically acceptable salts with inorganic or organic acids. Method of synthesis involves benzylation of azithromycin, O-methylation of C-6, C-11, C-4 hydroxy-groups at 2,, O, 3-N-bis(benzylhydroxycarbonyl)-N-demethylerythromycin followed by separation by column chromatography on silica gel and some additional stages. Ia R1=R2=CO2CH2C6H5, R3= CH3, R4=R5=H Ib R1=R2=CO2CH2C6H5, R3= R4=CH3R5=H Ic R1=R2=CO2CH2C6H5, R3= R5=H , R4=CH3 Id R1=R2=CO2CH2C6H5, R3= R4= R5= CH3 Ie R1=R2= R4= R5=H, R3=CH3 If R1=R2=R5=H, R3=R4= CH3 Ig R1=R2=R3= R5=H, R4=CH3 Ih R1=R2= H, R3= R4=R5=CH3 Ii R1=R4=R5=H, R2=R3= CH3 Ij R1=R5=H, R2=R3=R4=CH3 Ik R1=R3=H, R2= R4=CH3 Ie R1=H, R2= R3=R4=R5=CH3. EFFECT: improved method of synthesis. 15 cl"/> O-METHYL DERIVATIVES OF AZITHROMYCIN A SHOWING ANTIBACTERIAL ACTIVITY, AZITHROMYCINS AS INTERMEDIATE COMPOUNDS FOR SYNTHESIS OF O-METHYL DERIVATIVES OF AZITHROMYCIN A AND A METHOD OF SYNTHESIS OF O-METHYL DERIVATIVES OF AZITHROMYCIN A
首页> 外国专利> O-METHYL DERIVATIVES OF AZITHROMYCIN A SHOWING ANTIBACTERIAL ACTIVITY, AZITHROMYCINS AS INTERMEDIATE COMPOUNDS FOR SYNTHESIS OF O-METHYL DERIVATIVES OF AZITHROMYCIN A AND A METHOD OF SYNTHESIS OF O-METHYL DERIVATIVES OF AZITHROMYCIN A

O-METHYL DERIVATIVES OF AZITHROMYCIN A SHOWING ANTIBACTERIAL ACTIVITY, AZITHROMYCINS AS INTERMEDIATE COMPOUNDS FOR SYNTHESIS OF O-METHYL DERIVATIVES OF AZITHROMYCIN A AND A METHOD OF SYNTHESIS OF O-METHYL DERIVATIVES OF AZITHROMYCIN A

机译:偶氮霉素的O-甲基衍生物具有抗细菌活性,作为合成偶氮霉素A的O-甲基衍生物的中间体化合物的偶氮霉素及其合成方法

摘要

FIELD: organic chemistry. SUBSTANCE: products: azithromycin derivatives of the formula (I) at corresponding meanings of radicals or pharmaceutically acceptable salts with inorganic or organic acids. Method of synthesis involves benzylation of azithromycin, O-methylation of C-6, C-11, C-4 hydroxy-groups at 2,, O, 3-N-bis(benzylhydroxycarbonyl)-N-demethylerythromycin followed by separation by column chromatography on silica gel and some additional stages. Ia R1=R2=CO2CH2C6H5, R3= CH3, R4=R5=H Ib R1=R2=CO2CH2C6H5, R3= R4=CH3R5=H Ic R1=R2=CO2CH2C6H5, R3= R5=H , R4=CH3 Id R1=R2=CO2CH2C6H5, R3= R4= R5= CH3 Ie R1=R2= R4= R5=H, R3=CH3 If R1=R2=R5=H, R3=R4= CH3 Ig R1=R2=R3= R5=H, R4=CH3 Ih R1=R2= H, R3= R4=R5=CH3 Ii R1=R4=R5=H, R2=R3= CH3 Ij R1=R5=H, R2=R3=R4=CH3 Ik R1=R3=H, R2= R4=CH3 Ie R1=H, R2= R3=R4=R5=CH3. EFFECT: improved method of synthesis. 15 cl
机译:领域:有机化学。物质:产品:式(I)的阿奇霉素衍生物,其含义为自由基或药学上的相应含义与无机或有机酸形成的可接受的盐。合成方法包括阿奇霉素的苄基化,2,O,3-N-双(苄基羟基羰基)-N-去甲基红霉素的C-6,C-11,C-4羟基的O-甲基化,然后通过柱色谱分离在硅胶上和其他一些步骤。 Ia R 1 = R 2 = CO 2 CH 2 C 6 H < Sub> 5 ,R 3 = CH 3 ,R 4 = R 5 = H Ib R 1 = R 2 = CO 2 CH 2 C 6 H 5 ,R 3 = R 4 = CH 3 R 5 = H Ic R < Sup> 1 = R 2 = CO 2 CH 2 C 6 H 5 ,R 3 = R 5 = H,R 4 = CH 3 Id R 1 = R 2 = CO 2 CH 2 C 6 H 5 < / Sub>,R 3 = R 4 = R 5 = CH 3 即R 1 < / Sup> = R 2 = R 4 = R 5 = H,R 3 = CH 3 如果R 1 = R 2 = R 5 = H,则R 3 = R < Sup> 4 = CH 3 Ig R 1 = R 2 = R 3 = R < Sup> 5 = H,R 4 = CH 3 Ih R 1 = R 2 = H,R 3 = R 4 = R 5 = CH 3 Ii R 1 = R 4 = R 5 = H,R 2 = R 3 = CH 3 Ij R 1 = R 5 = H,R 2 = R 3 = R 4 = CH 3 Ik R 1 = R 3 = H,R 2 = R 4 = CH 3 即R 1 = H,R 2 = R 3 = R 4 = R 5 = CH 3 。效果:改进的合成方法。 15厘升

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