CAJ | 학술논문

本文以（S）-二乙基（1-重氮-2-（1，3-二氧化异吲哚酮-2-基）丙基）膦酸酯（化合物a）为原料，以5%Pd/C为催化剂，在冰乙酸、异丙醇存在下加氢还原，成功制得了（S）-二乙基（2-（1，3-二氧化异吲哚酮-2-基）丙基）膦酸酯（化合物b），即手性β-氨基膦酸酯，并探讨了催化剂5%Pd/C加入量，冰乙酸用量以及反应时间对试验的影响，得出了制备化合物b的较佳条件.即：化合物a∶催化剂5%Pd/C∶冰乙酸的物质的量比为1∶0.2∶0.6，反应时间为2 h；同时化合物b通过1HNMR、13CNMR、31PNMR、MS的测定，进行结构表征，结构正确；最后计算出化合物b的ee值为94.5%.
본문이（S）-이을기（1-중담-2-（1，3-이양화이신타동-2-기）병기）련산지（화합물a）위원료，이5%Pd/C위최화제，재빙을산、이병순존재하가경환원，성공제득료（S）-이을기（2-（1，3-이양화이신타동-2-기）병기）련산지（화합물b），즉수성β-안기련산지，병탐토료최화제5%Pd/C가입량，빙을산용량이급반응시간대시험적영향，득출료제비화합물b적교가조건.즉：화합물a∶최화제5%Pd/C∶빙을산적물질적량비위1∶0.2∶0.6，반응시간위2 h；동시화합물b통과1HNMR、13CNMR、31PNMR、MS적측정，진행결구표정，결구정학；최후계산출화합물b적ee치위94.5%.
This paper using (S)-diethyl (1-diazo-2-(1,3-dioxoisoindolin-2-yl)propyl)phosphonate as starting material which catalysted by 5%Pd-C, prepared(S)-diethyl(2-(1,3-dioxoisoindolin-2-yl)propyl)phosphonate in the presence of glacial acetic acid and i-PrOH. The effect of catalyst amount, the glacial acetic acid amount and the reaction time were discussed. The results indicate that the optimum conditions were the ratio of compound a, 5%Pd-C and glacial acetic acid was 1∶0.2∶0.6 and reacted 2 h. The obtalned compound b was identified by 1HNMR,13CNMR,31PNMR and MS and the enantiomeric excess was 94.5%.