发明名称 NOVEL 5-O-DEOSAMINYL 6-O-METHYL ERYTHRONOLIDE A DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF FOR PREPARING BIOLOGICALLY ACTIVE MATERIALS
摘要 1. A compound of formula (I): in which R is residue of carboxylic acid having upto 18 carbon atoms. 2. A compound of formula (I) according to claim 1, in which R is acetyle. 3. A method for preparing compounds of formula (I) according to claim 1 or 2, wherein a compound of formula (II): in which R has a value as defined hereinbefore is subjected to the action of sulfonic acid and then to a base selected from diazabicycloundecene, diazabicyclononene, 2,6-lutidine, 2,4,6-collidine or tetramethylguandine to obtain a compound of formula (III): which is subjected to the action of carbonyldiimidazole, then to NH2NH2 hydrazine to obtain a corresponding compound of formula (I). 4. A compound of formula (III) according to claim 3 as intermediate products to obtain compounds of formula (I). 5. A compound of formula (III) according to claim 4, wherein R is acetyle. 6. A method for preparing compounds of formula (VIII): wherein R'1 is a hydrogen atom or a hydrocarbon radical having upto 23 carbon atoms, saturated or unsaturated, which can be interrupted by one or several heteroatoms and can carry one or several functional groups, wherein a compound of formula (I): in which R is residue of carboxylic acid having ipto 18 carbon atoms is subjected to the action of an agent cleaving protected hydroxy groups to obtain a compound of formula (IV): which is subjected to the action of aldehyde of formula (V): in which R'1 has a value as defined hereinbefore to obtain a compound of formula (VI): which is subjected to the action of diimide in the presence of dimethylsulfoxide for hydroxyle oxidation in position 3, then to the action of an agent cleaving hydroxyle in position 2' to obtain a compound of formula (VII): which is subjected to the action of a reducer to obtain a corresponding compound of formula (VIII), in which R'1 is a radical.
申请公布号 EA000765(B1) 申请公布日期 2000.04.24
申请号 EA19980000280 申请日期 1996.10.08
申请人 HOECHST MARION ROUSSEL 发明人 BONNET, ALAIN;CHAPPERT, BERNADETTE;LAGOUARDAT, JACQUES
分类号 A61K31/70;C07H17/00;C07H17/08 主分类号 A61K31/70
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