高等佑胄与机 第2讲(合成).ppt

胺甲基化(Mannich)反应 具有活泼氢的化合物与甲醛、胺之间能缩合反应, 生成氨甲基衍生物。能发生Mannich反应的化合物有：醛、酮、酸、酯、腈、硝基烷、炔、及酚等. Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. Mannich 反应的活性点 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. * * 第二讲、有机胺的合成 医药绝大部分是有机胺化合物, 例如： 大部分染料是偶氮化合物, 其中间体是芳胺. Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. ? 卤代烷的氨解 ? 卤代芳烃的氨解 ? 磺酸脂的氨解 ? 醇的氨解 ? 酚的氨解 ? Gabrie 合成法制备伯胺 一、氨解反应 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 利用卤代烃的氨解制备胺 叔RX 易发生消除副反应 亲核性: R3N R2NH RNH2 NH3 利用沸点差进行分离， 适用于大规模工业生产。 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 实验室可利用大投料比来制备一级胺，但纯度不高。 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 卤代烷的氨解用于合成?-氨基酸, 生成的铵盐阻止了进一步N-烷基化反应. 伯卤代烃与六亚甲基四胺反应生成季铵卤, 而后在乙醇浓盐酸中加热分解成伯胺, 卤代烃最好是碘代烷,若用溴代烷或氯代烷时, 需加碘离子. 这种方法用于合成??-氨基酸和??-氨基酮等. Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 位阻胺与卤代反应, 可得到仲胺, 不会发生进一步的N-烷化副反应. 仲胺负离可与卤代烃顺利反应, 制备叔胺. Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 多卤代烃的氨解用于制备N-杂环化合物 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 卤代芳烃的氨解反应较困难 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 磺酸酯的氨解 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 醇的氨解反应 Evaluation only. Created with Aspose.Slides for .NET 3.5 Client Profile 5.2.0.0. Copyright 2004-2011 Aspose Pty Ltd. 酚的氨解反应 Evaluation only. Created with Aspose