Northeast Forestry University

Tao Yu

Xiufeng Yan

Sheng Zhang

Weiming Ding

Lijia Jing

Weimin Ding

Jian Zheng

Qiuying Pang

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.

N-acetyl amino acid ESTER derivatives of betulin and preparation method thereof

Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, Calkyl, Chaloalkyl, aryl substituted Calkyl, phosphate substituted Calkyl, amino-substituted Calkyl, carboxyl substituted Calkyl, hydroxyl substituted Calkyl, and amide-substituted Calkyl; Ris selected from hydrogen and t-butoxycarbonyl substituted amino. Also provided in the present invention are the preparation method of the derivate and the use thereof in anti-tumor drug preparation.

Derivate, preparation method and use of 10-methoxycamptothecin

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Heilongjiang, China

Tao Yu