发明名称 PROCESS OF MAKING AN ALPHA-ANOMER ENRICHED 2-DEOXY-2,2-DIFLOURO-D-RIBOFURANOSYL SULFONATE AND USE THEREOF FOR MAKING A BETA NUCLEOSIDE
摘要 <p>A process of preparing an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate, which is useful as an intermediate in the preparation of a beta nucleoside, such as gemcitabine, an anti-tumor agent. A beta-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate is heated and converted to an alpha-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate in the absence of an effective amount of a sulfonate salt to facilitate the conversion. In addition, an anomeric mixture of an alpha-anomer and a beta-anomer of 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate can be dissolved in a mixture of water and a solvent and heated to produce a lactol, which may be further converted to an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate.</p>
申请公布号 EP1891087(A1) 申请公布日期 2008.02.27
申请号 EP20060771094 申请日期 2006.05.24
申请人 SCINOPHARM TAIWAN, LTD.;SCHLOEMER, GEORGE 发明人 WANG, LUNG-HU;LIU, ALLEN;SCHLOEMER, GEORGE
分类号 C07H19/073 主分类号 C07H19/073
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