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US 5,208,349 AGranted
Process for preparing milbemycin derivatives and certain novel compounds employed therein
AssigneeSankyo Company, Limited
InventorsKazuo Sato, Takao Kinoto, Shigeru Mio, Toshiaki Yanai
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Abstract
13-Hydroxy-5-ketomilbemycin derivatives are prepared by oxidizing a 5-ketomilbemycin with selenium dioxide in the presence of a lower aliphatic carboxylic acid. A range of new 13-acyloxy-5-ketomilbemycins and a method of preparing them are also disclosed.
Claims13
A process for preparing a compound of formula (I):
- ##STR5## in which R.sup.1 represents a methyl, ethyl, isopropyl or sec-butyl group, by treating a compound of formula (III):
- ##STR6## wherein R.sup.1 is as defined above, with selenium dioxide in the presence of a carboxylic acid of formula (IV):
- R.sup.2 --COOH (IV)
- wherein R.sup.2 represents a hydrogen atom to produce said compound of formula (I) together with a compound of formula (II):
- ##STR7## wherein R.sup.1 and R.sup.2 are as defined above and optionally, hydrolizing said compound of formula (II) to form said compound of formula (I).
2 more elements
A process for preparing a compound of formula (I):
- ##STR8## in which R.sup.1 represents a methyl, ethyl or isopropyl group by treating a compound of formula (III):
- ##STR9## wherein R.sup.1 is as defined above, with selenium dioxide in the presence of a carboxylic acid of formula (IV):
- R.sup.2 --COOH (IV)
- wherein R.sup.2 represents a hydrogen atom, to produce said compound of formula (I) together with a compound of formula (II):
- ##STR10## wherein R.sup.1 and R.sup.2 are as defined above and, optionally, hydrolizing said compound of formula (II) to form said compound of formula (I).
2 more elements
Dependencies are inferred from the claim text.