| 摘要 |
<p>PURPOSE: A preparation method of 6-O-methylerythromycin A is provided to manufacture 6-O-methylerythromycin A of the formual (1) effectively and simply. Also, an intermediate of the foemula (8) which is used therefor is provided. CONSTITUTION: A preparation method of 6-O-methylerythromycin A of formula (1) comprises the following steps: (i)producing a compound of formula (3) by oxidizing erythromycin A 9-oxime of formula (2) or dimethylamino group at 3'-location of acid added salt thereof; (ii)producing a compound of formula (5) whose 9-oxime hydroxy group is protected by reacting the compound of formula (3) in step(i) and a compound of formula (4); (iii)producing a compound of formula (6) by methylating the compound of formula (5) in step (ii); (iv)producing a compound of formula (7) by hydrolyzing an oxime protecting group of the compound of formula (6) in step (iii) in the presence of acid; (v)performing reductional hydrolysis and reduction reaction of 9-oxime group of the compound of formula (7) in step (iv) and oxide group at 3'-location independently, in the formulae, R¬1 is -CH2R¬4 or -OR5 group(R¬4 is C1-C5 alkyl group, R5 is C1-C6 alkyl group), R¬2 is H, C1-C6 alkyl, phenyl or aralkyl group or forms C3-C4 alkylene group which can be substituted with C1-C3 alkyl group, with R¬4, R¬3 is C1-C6 alkyl, C4-C7 cycloalkyl, phenyl or aralkyl, forms C2-C3 alkylene group with R¬4, R6 is -OR5 group or forms =CHR¬4 group with R¬1.</p> |
