Methods utilizing aryl thioimines in synthesis of erythromycin derivatives
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United States of America Patent
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Sep 24, 2002
Grant Date -
Aug 22, 2002
app pub date -
Dec 21, 2000
filing date -
Dec 21, 2000
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Abstract
An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
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