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US 8,796,279 B2Granted
4′-demethylepipodophyllotoxin derivative, preparation method and use thereof
AssigneeHubei University of Technology
InventorsYa-Jie Tang, Wei Zhao
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Abstract
A 4′-demethylepipodophyllotoxin derivative of formula (III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4′-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4′-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.
Claims10
A method to synthesize a compound with a structure shown in Formula (III) or its salts:
- wherein:
- (1) 4-hydroxyl in C ring of 4′-demethylepipodophyllotoxin is activated to obtain an activation product;
- and
- (2) tetramethylpyrazine, tetramethylpyrazine hydrochloride or tetramethylpyrazine phosphate is introduced into the 4-position in C ring of 4′-demethylepipodophyllotoxin to obtain the compound with the structure shown in Formula (III) or its salts.
1 more element
Dependencies are inferred from the claim text.