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Compositions and methods for preparing 13-deoxyanthracyclines
专利权人:
ファーマシューティカルズ,;ジェム ファーマシューティカルズ, エルエルシー;エルエルシー;ジェム
发明人:
ウォルシュ, ジェラルド, エム.,オルソン, リチャード, ディー.,ウォルシュ, ジェラルド, エム.,オルソン, リチャード, ディー.
申请号:
JP2007540146
公开号:
JP5307399B2
申请日:
2005.11.08
申请国别(地区):
JP
年份:
2013
代理人:
摘要:
13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthrcyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines to 13-deoxyanthrcyclines wherein the reduction reaction is maintained at temperatures of about 55° C. to 64° C. without stirring or agitation. The reaction is completed with the addition of aqueous bicarbonate which forms the 13-deoxyanthracycline and precipitates. The precipitates are filtered and the precipitate and filtrate are extracted separately with organic solvents. The crude 13-deoxy anthracycline can be converted to 5-imino-13-deoxy anthracycline by reaction with methanolic ammonia. The reaction can also be performed with an acidic pyridinium salt instead of a strong acid so that neutralization of the reaction or extraction of the product is not necessary, thereby facilitating purification.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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