Abstract

The enantioselective vinylogous Henry reaction of 3,5-dimethyl-4-nitroisoxazole with trifluoromethyl ketones employing a bifunctional squaramide organocatalyst has been developed. A series of isoxazole bearing trifluoromethyl-substituted tertiary alcohols, 2-substituted (R)-1,1,1-trifluoro-3-(3-methyl-4-nitroisoxazol-5-yl)propan-2-ols, were obtained under these mild reaction conditions in good yields and moderate to good enantioselectivities

The enantioselective vinylogous Henry reaction of 3,5-dimethyl-4-nitroisoxazole with trifluoromethyl ketones employing a bifunctional squaramide organocatalyst has been developed. A series of isoxazole bearing trifluoromethyl-substituted tertiary alcohols, 2-substituted (R)-1,1,1-trifluoro-3-(3-methyl-4-nitroisoxazol-5-yl)propan-2-ols, were obtained under these mild reaction conditions in good yields and moderate to good enantioselectivities

中文翻译：

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3,5-二甲基-4-硝基异恶唑与三氟甲基酮的有机催化对映选择性亨利反应

摘要

已经开发了使用双官能方酰胺有机催化剂的3，5-二甲基-4-硝基异恶唑与三氟甲基酮的对映选择性乙烯基类亨利反应。在以下条件下获得一系列带有异恶唑的三氟甲基取代的叔醇，即2-取代的（R）-1,1,1-三氟-3-（3-甲基-4-硝基异恶唑-5-基）丙-2-醇。这些温和的反应条件，收率高，对映选择性中等至良好

已经开发了使用双官能方酰胺有机催化剂的3，5-二甲基-4-硝基异恶唑与三氟甲基酮的对映选择性乙烯基类亨利反应。在以下条件下获得一系列带有异恶唑的三氟甲基取代的叔醇，即2-取代的（R）-1,1,1-三氟-3-（3-甲基-4-硝基异恶唑-5-基）丙-2-醇。这些温和的反应条件，收率高，对映选择性中等至良好