1-.alpha.-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivatives and process for the preparation thereof
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United States of America Patent
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Dec 28, 2010
Grant Date -
Oct 11, 2007
app pub date -
Jun 21, 2005
filing date -
Jul 29, 2004
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Expired
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Abstract
1-.alpha.-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-.alpha.-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.
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