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US 4,394,312 AGranted
Process for preparing rifamycin derivatives
AssigneeKorea Advanced Institute of Science and Technology
InventorsMoon H. Han, Baik L. Seong
Life of this patent
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Abstract
3-Dialkylaminomethyl derivatives of rifamycin S is provided by reacting rifamycin S with an iminium salt in an organic solvent. This compound is converted to 3-dialkylaminomethyl derivatives by virtue of ascorbic acid.
Claims4
A process for preparing 3-dialkylaminomethyl rifamycin S derivatives having the formula:
- ##STR8## wherein R.sup.1 and R.sup.2 are oxo (.dbd.O);
- and R.sup.3 and R.sup.4 are methyl, ethyl, propyl, isopropyl, butyl or pentyl, or are connected by methylene bridge where ##STR9## represents piperidine or 3-methylpyrrolidine which process comprises contacting rifamycin S with 1 to 1.5 equimolar amount of an appropriate iminium salt in an organic solvent at a temperature ranging from room temperature to the boiling point of the solvent for a time sufficient to complete the reaction.
Dependencies are inferred from the claim text.