发明名称 |
Synthesis of pancratistatin prodrugs |
摘要 |
A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.
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申请公布号 |
US2004127467(A1) |
申请公布日期 |
2004.07.01 |
申请号 |
US20030475061 |
申请日期 |
2003.10.16 |
申请人 |
PETTIT GEORGE R;ORR BRIAN;DUCKI SYLVIE |
发明人 |
PETTIT GEORGE R;ORR BRIAN;DUCKI SYLVIE |
分类号 |
A61K31/665;C07D213/06;C07D233/54;C07D295/02;C07D295/027;C07D453/04;C07F9/655;(IPC1-7):A61K31/665 |
主分类号 |
A61K31/665 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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