Method for synthesizing epidaunorubicin serving as epirubicin intermediate
The invention belongs to the field of organic synthesis and specifically discloses a method for synthesizing epidaunorubicin serving as an epirubicin intermediate. According to the method, (2R,6S)-6-methoxy-2-methyl-6H-pyran-3-one is adopted as a starting raw material, the raw material is subjected...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention belongs to the field of organic synthesis and specifically discloses a method for synthesizing epidaunorubicin serving as an epirubicin intermediate. According to the method, (2R,6S)-6-methoxy-2-methyl-6H-pyran-3-one is adopted as a starting raw material, the raw material is subjected to double bond reduction, halogenation, ammoniation and chiral separation, then an amino group is protected by a trifluoroacetyl group and subjected to chlorination to obtain an intermediate VI, and the intermediate VI is coupled with daunorubicinone, reduced by sodium borohydride and subjected to trifluoroacetyl group removal to obtain the epidaunorubicin serving as the epirubicin intermediate. The whole synthetic route has the advantages that the steps are short, reaction conditions are mild,the yield is high, and aftertreatment is convenient; the method has a good industrialization prospect.
本发明属于有机合成领域,具体公开了一种表柔比星中间体表柔红霉素的合成方法。本发明以(2R,6S)-6-甲氧基-2-甲基-6H-吡喃-3-酮为起始原料,经还原双键、卤代、氨化、手性拆分、再经三氟乙酰基保护氨基、氯代后得中间体VI,中间体VI与柔红 |
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