发明名称 |
Process of preparing etoposide phosphate and etoposide |
摘要 |
Etoposide phosphate is prepared by coupling dibenzyl 4'-demethyl-4-epipodophyllotoxin-4'-phosphate with 2,3-di-O-benzyl-4,6-O-ethylidene- alpha , beta -D-glucopyranose in a solvent and subsequently removing the protecting groups. The tetra-benzyl protected etoposide phosphate is recrystallized from methanol or directly crystallized from acetonitrile by adding methanol to yield substantially the pure C-1''- beta form. The benzyl protecting groups are simultaneously removed by hydrogenation to produce etoposide phosphate in high yields. In a further embodiment, etoposide phosphate is treated with a phosphatase enzyme to yield etoposide.
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申请公布号 |
US5459248(A) |
申请公布日期 |
1995.10.17 |
申请号 |
US19930145517 |
申请日期 |
1993.11.04 |
申请人 |
BRISTOL-MYERS SQUIBB COMPANY |
发明人 |
SILVERBERG, LEE J.;VEMISHETTI, PURUSHOTHAM;DILLON, JR., JOHN L.;USHER, JOHN J. |
分类号 |
C12N9/16;A61K31/70;A61K31/7042;A61K31/7048;A61P35/00;C07F9/6561;C07H15/18;C07H15/24;C07H17/04;C12P19/60;(IPC1-7):A61K31/70 |
主分类号 |
C12N9/16 |
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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