摘要
环状β氨基酸cispentacin是种抗生素、抗菌素,在医药合成上是种重要的中间体。本论文通过广泛的查阅资料,确定了合成cispentacin的方法为Palmieri研究小组的还原氨化法。该方法起始原料价格低廉易得,所生成的非对映体和顺/反对映体的选择性通过改变还原条件可以得到进一步的改善。这种方法的唯一缺点是得到的产物需要用色谱仪纯化分离。但是研究发现:最后生成的主要的非列应体1(R,S,S)或它的对映体能够从反应混合物中以HBR盐的形式分离出来,并得到很高的产率和光学纯度。另外论文对合成已二酸二乙酯的催化剂进行了选择,确定了该反应的最佳时间、醇酸配比、带水剂的最佳用量、催化剂的最佳用量。用还原氨化法合成了原料(+)α—苯基乙胺。确定合成cispentacin的原料2-oxo-cyclopentanecarboxylate的催化剂为钠,溶剂为甲苯及它们的用量。
Annular β amino acid cispentacin is a kind of antifungal
antibiotic. It ;s an important pharmaceutical intermediate in the synthesization of many Pharmaceuticals. After consulting many literatures , we chose the following way to synthesize cispentacin :diastereoselective reductive amination of 2-oxo-cyclopentanecarboxylate with a -methylbenzylamine.This method reported by Palmieri utilizes inexpensive and readily available starting materials .The only drawback of this method is the necessity of a chromatographic purification to isolate the desired diastereomer .This thesis also reports some research work on the synthesization of di-Et adipate and gets the conclusion of the most reasonable time,the best proportion of acid and alcohol,the most reasonable quality of catalyzer in this.chemical reaction.And also synthesizes the a-methylbenzylamine
and 2-oxo-cyclopentanecarboxylate,,
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