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利用以苯基甘氨酸1为代表的、来源丰富的(-氨基酸通过还原和官能团保护, 修饰为氨基醇手 性砌块3. 5-(l-孟氧基)-3-溴-2(5H)-呋喃酮手性试剂4与3在温和的条件下发生串联的不对称双Michael加成/分子内亲核取代反应, 得到了具有4个新的手性中心的氨基酸手性修饰砌块/螺环/环丙烷类化合物7(52%, 非对映体过量(de)≥ 98 %). 经元素分析, [α]D20, UV, IR, 1 H NMR, 13C NMR, MS以及X射线四圆衍射测定, 确认了它的化学结构、立体化学和绝对构型. 其结果可以为手性砌块的引入、合成含有某些活性官能团的复杂结构化合物以及探讨它们的生物活性提供新的方法和途径.
5- (l-menthoxy) -3-bromo-2 (5H) -trimethylammonium chloride, which is rich in amino acids represented by phenylglycine 1 (amino acids are reduced to amino alcohols by reduction and functional group protection) -furanone Chiral Reagents 4 and 3 A tandem asymmetric double Michael addition / intramolecular substitution reaction was carried out under mild conditions to obtain amino acid chiral modification blocks with 4 new chiral centers Cyclic / cyclopropane compounds 7 (52%, diastereomeric excess ≥ 98%). Elemental analysis of [α] D20, UV, IR, 1 H NMR, 13C NMR, MS and X-ray four circles The results of the determination of its chemical structure, stereochemistry and absolute configuration confirmed that the new methods and approaches could be provided for the introduction of chiral building blocks, the synthesis of complex structural compounds containing some active functional groups and their biological activities .