发明名称 |
Process for the preparation of 9-amino camtothecin |
摘要 |
9-Amino-20(S)-camptothecin (I) is prepared by reducing 12-nitro-20(S)-camptothecin (II); converting the resulting 12-amino-20(S)-camptothecin (III) into a compound of formula (IV)whereinX is a group which can be reductively removed; reacting the compound of formula (IV) with a nitrating agent, to obtain thereby the corresponding 9-nitro-20(S)-camptothecin compound of formula (V) substituted at the 12-position by the group X; reducing in a single step the compound of formula (V), so obtaining the 9-amino-20(S)-camptothecin of formula (I); or reducing the compound of formula (V), so obtaining the corresponding 9-amino-20(S)-camptothecin compound of formula (VI) substituted at the 12-position by the group X and reductively removing the X group from the compound of formula (VI), so obtaining 9-amino-20(S)-camptothecin. |
申请公布号 |
ZA9405878(B) |
申请公布日期 |
1995.03.10 |
申请号 |
ZA19940005878 |
申请日期 |
1994.08.05 |
申请人 |
FARMITALIA CARLO ERBA S.R.L. |
发明人 |
ANGELO BEDESCHI;WALTER CABRI;ILARIA CANDIANI;FRANCO ZARINI |
分类号 |
C07D491/147;A61K31/47;A61K31/4745;A61P35/00;C07D471/16;C07D491/22 |
主分类号 |
C07D491/147 |
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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