发明名称 PROCESSES FOR ASYMMETRIC CONVERSION OF 3-FLUORO-L-ALANINE AND 2-DEUTER/-3-FLUORO-L-ALANINE TO THEIR D-ISOMERS
摘要 2-Deutero-3-fluoro-L-alanine is converted into its D-isomer in an asymmetrical manner. In this process, the L-isomer is reacted with sodium nitrite to give the corresponding L-2-deutero-2-halo-3-fluoro-propionic acid in solution in an aqueous hydrohalic acid. This L-2-deutero-2-halo-3-fluoropropionic acid is then reacted either with ammonia or with sodium azide with replacement of the 2-halogen substituent by a 2-azido group and subsequent catalytic hydrogenation to give 2-deutero-3-fluoro-D-alanine. 2-Deutero-3-fluoro-L-alanine can be converted into pharmaceutically acceptable salts. The resulting compound can be used for inhibition of the growth of Gram-positive and Gram-negative pathogenic bacteria.
申请公布号 ZA7601045(B) 申请公布日期 1977.09.28
申请号 ZA19760001045 申请日期 1976.02.23
申请人 MERCK & CO INC 发明人 REINHOLD D
分类号 C07C227/08;C07C53/21;C07C59/19;C07C67/00;C07C227/00;C07C227/06;C07C229/20 主分类号 C07C227/08
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