N-acetyl amino acid ESTER derivatives of betulin and preparation method thereof
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United States of America Patent
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Jan 31, 2017
Grant Date -
Dec 24, 2015
app pub date -
Jan 16, 2015
filing date -
Jun 20, 2014
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Abstract
The present invention disclosed N-acetyl amino acid ester derivatives of betulin and the preparation method thereof, the method comprising the steps that in the presence of an alkaline substance, a catalyst and a racemization-inhibitor, the carboxyl group of N-acetyl amino acid is activated by a coupling agent; and then the activated N-acetyl amino acid is reacted with betulin via esterification reaction to obtain the N-acetyl amino acid ester derivative of betulin. The present invention provided a simple synthesis method to synthesize the N-acetyl amino acid ester derivatives of betulin by using betulin as a precursor compound and modifying the molecular structure of betulin. Such structural modification of betulin significantly enhances the anti-tumor activity of the betulin derivatives and therefore has important values.
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