N-acetyl amino acid ESTER derivatives of betulin and preparation method thereof
US9556221B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jan 16, 2015 |
| Grant date | Jan 31, 2017 |
| Priority date | — |
| Expiry date | Feb 22, 2035 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.