公开(公告)号：EP0015339A1

公开(公告)日：1980-09-17

申请号：EP79302272.4

申请日：1979-10-19

申请人： ELI LILLY AND COMPANY

发明人： Shyan-Ell Su, Kenneth ,  Templeton, Robert Joseph ,  Wikel, James Howard

IPC分类号： C07D235/30

CPC分类号： C07D235/30

摘要： To separate the syn and anti oximes of the formula
wherein R 1 is C 1 -C 5 alkyl; and R 2 is phenyl, or phenyl substituted by C 1 -C 4 alkyl, C 1 -C 4 alkoxy, chloro, bromo, iodo, nitro or trifluoromethyl, e.g. 1-isopropylsulfonyl-2-amino-6-(a-hydroximinobenzyl)-benzimidazole, a mixture of these oximes is dissolved in a water miscible organic solvent selected from methyl ethyl ketone, methanol, ethanol, isopropanol, acetonitrile, dimethylacetamide, dimethyl sulfoxide and, preferably, acetone, a sufficient quantity of water is added to initiate crystallization, and the precipitated anti oxime isomer which displays good antiviral activity is separated, e.g. in greater than about 95% purity.

摘要翻译： 为了分离下式的顺式和反式肟... 其中R 1是C 1 -C 5烷基; 或R 2为苯基，或被C 1 -C 4烷基，C 1 -C 4烷氧基，氯，溴，碘，硝基或三氟甲基取代的苯基。 1-异丙基磺酰基-2-氨基-6-（α-羟基肟基苄基） - 苯并咪唑，将这些肟的混合物溶于选自甲基乙基酮，甲醇，乙醇，异丙醇，乙腈，二甲基乙酰胺，二甲基亚砜的水混溶性有机溶剂和 ，优选丙酮，加入足量的水以引发结晶，并且分离出显示良好抗病毒活性的沉淀的抗肟异构体，例如 大于约95％的纯度。