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NOVEL 4ß-AMINO PODOPHYLLOTOXIN CONGENERS AS POTENTIAL ANTICANCER AGENTS AND A PROCESS FOR THE PREPARATION THEREOF
专利权人:
发明人:
申请号:
IN953/DEL/2007
公开号:
IN291453B
申请日:
2007.05.03
申请国别(地区):
IN
年份:
2018
代理人:
摘要:

The present invention provides new class of 4beta-[4-(1,3-benzothiazole-2-yl)anilino]podophyllotoxin analogues having the structural formula as follows (4). Where R-H or CH3 R1-H, halogen, CH3 and R2-H, halogen, OCH3. The present invention also provides a process for the preparation of new 4beta-[4-(1, 3-benzothiazole-2-yl)anilino]podophyllotoxin analogues as useful anticancer agents. More particularly, it provides a process for the preparation of 4beta-[4-(1,3-benzothiazole-2-yl)anilino] derivatives of podophyllotoxin. The process for the synthesis of new podophyllotoxin analogues as anticancer agents produces the novel and stereo-selective derivatives of the podophyllotoxin in good yields, where in the key step for the synthesis of these analogues is by direct nucleophilic substitution of C-4beta-iodo intermediates. The 4beta-iodopodophyllotoxin, which has been reacted with substituted or unsubstituted 4-(1,3-benzothiazole-2-yl)aniline in a stereo-selective manner to afford the 4beta-[4-(1,3-benzothiazole-2-yl)anilino] derivatives of podophyllotoxin.

[US2008275248A1]
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