吳學亮Wu, Hsyueh-Liang黃志浩Huang, Chih-Hao2019-09-04不公開2019-09-042016http://etds.lib.ntnu.edu.tw/cgi-bin/gs32/gsweb.cgi?o=dstdcdr&s=id=%22G060342041S%22.&%22.id.&http://rportal.lib.ntnu.edu.tw:80/handle/20.500.12235/100051本論文研究主題為利用本實驗室所開發的掌性雙環[2.2.1]雙烯配體與一價銠金屬形成之催化劑催化芳香基硼酸與γ-位胺基及膦酸酯取代之α , β-不飽和酯類進行不對稱1,4-加成反應。使用三莫耳百分率的銠金屬試劑(3 mol% of Rh)及L1e或L1f配體催化加成反應進行，生成的產物其產率有26–>99%，鏡像超越值為90–>99.5% ee。這個合成方法可利用來合成balcofen及phaclofen藥物分子。This thesis describes an efficient synthesis of highly enantioenriched 4-amino-3-aryl-butanoates and 4-phosphoryl-3-aryl-butanoates via an enantioselective 1,4-addition of an array of aryboronic acids to γ-amino-α , β-unsaturated esters and γ-phosphoryl-α , β-unsaturated esters. In the presence of 3 mol% of the Rh(I)/ chiral diene L1e or L1f as catalyst, the conjugate addition adducts were isolated in 26–>99% yield and 90–>99.5% ee. The synthetic usefulness of the developed method was demonstrated in the syntheses of baclofen and phalcofen.銠金屬催化試劑掌性雙烯配基αβ-不飽和羧酸酯RhodiumChiral diene ligandαβ-Unsaturated esters