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In this dissertation, Ir-catalyzed asymmetric hydrogenation of quinoline derivatives, pyridine derivatives and exocyclic enamines have been studied.

本论文研究了铱催化的喹啉和吡啶衍生物以及环外烯胺的不对称氢化。

While the basicity of the N-atom is stronger, more active second generation catalyst is indispensable and the temperature needs to be reached 150℃, and mixture of pyrrolidine and pyrrole was gained.

研究结果表明微波辐射条件下氮原子的碱性强弱对于二烯丙基胺发生关环复分解反应具有很大的影响:当底物的碱性比较强时,必须使用活性更高的第二代Grubbs催化剂,且温度需升至150℃反应才能顺利发生,得到光学纯吡咯啉和吡咯的混合物。

Benzyloxy benzoyldimethylsulfoxide was prepared by the reaction of ethyl 4-benzyloxybenzoate and dimethyl sulfoxide in the presence of sodium hydride, followed by Pummerer reaction with concentrated hydrochloric acid to afford eo-hydroxy-co-thio-methyl-(4/-benzyloxy) acetophenone, which reacted with urea, thiosemicarbazide, semicarbazide hydrochloride and o-phenylenediamine to give imidazolidine-2,4-dione, l,2,4-triazine-3- one and quinoxaline derivatives, respectively.

本文用4-苄氧基苯甲酸乙酯和二甲亚砜为原料,在氢化钠存在下反应,合成了(4′-苄氧基)-苯甲酰基-二甲亚砜。研究了该亚砜在浓盐酸的存在下发生的Pummerer重排反应,用重排产物ω-羟基-ω-甲硫基-(4′-苄氧基)-苯乙酮分别与尿素、氨基脲、氨基硫脲和邻苯二胺反应合成了2,4-咪唑啉-二酮、1,2,4-三嗪-3-酮、喹喔啉等含氮杂环化合物。

The auxiliary can be recovered in high yield (81%) only by filtering and recrystallization. Besides, some other aldehydes have been chosen to test the enantioselectivity of N,N\'-dibenzyl tartamide, in comparison with two other allylaborates reagents developed previously by Roush and Brown, respectively. The results show that %e.e. of homoallylic alcohol is superior to that of the former, and approaches the Brown reagent.

产物经S_N2反应得瑞格列萘中间体-甲基烯丙基-2-氯苯基-叠氮甲烷(17);同时,将筛选出的新型手性配体N-苄基酒石酸二酰胺用于其他几种醛(正丁醛,异戊醛和环己醛)的不对称烯丙基化反应,并与广泛应用的Roush配体(22)和Brown配体(27)相比较,发现其立体选择性优于Roush配体,并接近Brown配体,但明显具有可回收利用的优势。

OBJECTIVE: To observe the effect of low molecular weight saccharide in rhizoma polygonati on the immune function of normal mice and immunosuppression ones caused by cyclophosphamide.

目的:观察黄精中小分子糖对正常小鼠及对环磷酰胺所致免疫功能低下小鼠免疫功能的影响。

The results show that water salability and water dispersion stability are excellent when the mass fraction of GMA is 15%, the ambition ring-open is 50% and neutralization is 80%.

结果表明:甲基丙烯酸缩水甘油酯含量为15%,胺化开环址为50%,中和度为80%时,树脂的水溶性及水分散体系稳定性均良好。

The regioselectivity of primary aminyl radical cyclization was first investigated in this dissertation. The total synthesis of 14-Aza camptothecin was then achieved on the basis of our investigation in the construction of pyrimidin-4-one skeleton via [4+2] strategy.

中文摘要本论文首先探讨了伯胺氮自由基环合反应的区域选择性,然后应用[4 + 2]策略对吡咯并嘧啶-4-酮的合成方法进行了研究,并在此基础上完成了14-氮杂喜树碱的合成工作。

The synthesis of the pentacyclic skeleton of Et-743 and the construction of the five chiral centers thereof.1. The core pentacyclic skeleton of phthalascidin was constructed with L-dopa as the starting material via thirteen steps. First, two basic synthons, the C-1 functionalized tetrahydroisoquinoline compounds 8 and N-protected Z-dopa derivative 9, were prepared from L-dopa. They were coupled via amide bond to form the dipeptide compounds 10, which were the first key intermediates. Then the primary hydroxyl groups were transformed into the corresponding amino aldehydes 11 via Swern oxidation. Followed by the intramolecular Pictet-Spengler cyclization, the pentacyclic compounds 12 were synthesized.

五环骨架的构建及五个正确手性中心的确立:1.1我们以L-多巴为起始原料,经过多步官能团保护和转化合成了基本结构单元8然后和苯丙氨酸衍生物9,通过缩合反应生成酰胺中间体10,经Swern氧化得到醛化合物11,然后再次利用分子内改良的Pictet-Spengler反应一步构建c,d两环,得到五环骨架化合物12,最后,实现了21-位羰基向氰基的转化,得到了C-1位官能化的化合物14,化合物14不但具有和Et-743一致的五环骨架,而且分子中五个手性中心立体构型也与其完全相同:其中,3,位和13,位的手性中心由原料L-多巴带入,而1,位,11,位和21,位手性中心则通过不对称诱导而确立。

This research uses dicyandiamide as firming agent in epoxy powder coating and sodium fluoride as additive in epoxy.

采用磷酸双氰胺盐作环氧粉末涂料的固化剂、氟化钠作添加剂。

Methods S180 and H22 mice were divided into solanine (37.50、18.75, and 9.37mg/kg) groups, negative control group and cytoxan (30mg/kg) group, whom were given drugs by sc.

将S180和H22荷瘤小鼠分为龙葵碱37.50、18.75、9.37mg/kg组、阴性对照组和环磷酰胺(30mg/kg)组,各组sc给药。

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As she looked at Warrington's manly face, and dark, melancholy eyes, she had settled in her mind that he must have been the victim of an unhappy attachment.

每逢看到沃林顿那刚毅的脸,那乌黑、忧郁的眼睛,她便会相信,他一定作过不幸的爱情的受害者。

Maybe they'll disappear into a pothole.

也许他们将在壶穴里消失

But because of its youthful corporate culture—most people are hustled out of the door in their mid-40s—it had no one to send.

但是因为该公司年轻的企业文化——大多数员工在40来岁的时候都被请出公司——一时间没有好的人选。