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In some cases, its epimer 4 was also obtained. 22 compounds were synthesized, among them 18 were new.3. Using the intramolecular Pictet-Spengler reaction to form the pentacyclic skeleton of Et-743, the byproducts 25 were obtained under various conditions. The structures of them were determined to be 1, 2-dihydro-isoquinoline compounds, and the mechanism of the reaction was proposed.B. The synthesis of the analogs of Et-743Because of the failure of removing the protective groups in compounds 14, the synthetic strategy was adjusted.

对于苄基保护的羟基化合物13a,顺利得到化合物30,然后与不同的羧酸反应得到18个酯化合物33-50;对于苄氧羰基保护的氨基化合物13b,由于脱除保护基的化合物31在空气中不稳定,所以我们采取不经分离纯化,直接与羧酸反应得到酰胺化合物53-62,然后再分别对其C-21位的羰基进行还原氰基化,得到10个酰胺目标化合物63-72,另外,我们还对羟基转化为氨基的反应进行了探索。3。

A better understanding of the role of PPAR in insulin action system will be critical in developing more efficacious and safe agent s that act on PPAR and benefit patients with type 2 diabetes. The main content is followed: Synthesis and analysis of 1,3-dicarbonyl compounds. Make use of easily available cheap reagent such as 2-naphthol, 6-hydroxyquinoline, 1,2-dibromoethane, 4- hydroxybenzaldehyde, dimethyl malonate, 2-{4- [(2-napthoxy)ethoxyl] benzyl} malonates and 2-{4 [(1,2,3,4-tetrahydro-6 -quinolinoxy)ethoxyl] benzyl } malonates were synthesized through 6-8 steps in virtue of Williamson, Knoevenagel reaction, Pd/C catalyzed hydrogenation with mild conditions and high yield. The total yield of 40-50%.

本论文的主要内容和研究结果如下: 1,3-二羰基类化合物的合成及分析,采用2-萘酚、6-羟基喹啉、1 ,2二溴乙烷、对羟基苯甲醛、丙二酸二甲酯等常见易得试剂,利用Williamson反应、Knoevenagel反应、钯碳加氢等条件温和且收率高的方法,分别合成了2-{4- [(2-萘氧)乙氧基]苄基}丙二酸衍生物和2-{4 [(1,2,3,4-四氢-6-喹啉氧基)乙氧基]苄基}丙二酸衍生物两个系列8个化合物,经6-8步反应,总收率为40-50%,具有一定绿色化学特性。

Acridone 1 reacted with benzyl chlorides 2 in NaH/DMF/KI to give 10-benzyl-9-acridones 3 in high yields. Subsequent reduction of 3 with NaBH4 gave 10-benzy1-9,10-dihydroacridine derivatives 4 with yields of 88%~96%.

吖啶酮1与氯化苄及其衍生物2在氢化钠/N,N-二甲基甲酰胺/碘化钾中反应高产率生成10-苄基吖啶酮类化合物3; 3经硼氢化钠氢化还原生成10-苄基-9,10-二氢吖啶类化合物4,产率88%~96%。

Poly-[N-(2-hydroxyethyl)-L-glutamine] was then obtained by aminolysis of PBLG with 2-aminoethanol.

以L -谷氨酸为单体,经r -羧基的苄基保护,与光气/甲苯液反应制备L-谷氨酸苄酯的羧酸酐,均聚得L -谷氨酸苄酯,然后经由 2 -氨基乙醇胺解得聚 [N -( 2 -羟乙基)-L -谷酰胺 ] 。

Grasp the electron delocolization theory; be capable of judging the relative stability of allylic and benzylic free radicals and carbocations, know the relative stability of dienes and other multiple unsaturated hydrocarbons; grasp the characteristics for the nucleophilic substitution reactions of allyl halides and benzyl halides, and the addition reactions of conjugate dienes.

掌握电子非定域化理论;能够分析判断烯丙基、苄基自由基和正离子的稳定性和二烯及多重不饱和碳氢化合物的稳定性;掌握烯丙基、苄基卤代物的亲核取代反应特性和共轭二烯的加成反应。

Dibenzyl sulfoxide and dibenzyl sulfone were synthesized from dibenzyl sulfide oxidated with H 2O 2 without catalyst.

在无催化剂条件下利用过氧化氢氧化二苄基硫醚合成了二苄基亚砜和二苄基砜。

This work, concentrated on the asymmetric allylation of aldehydes controlled by different chiral auxiliaries prepared from rotational pure tartaric acid, can be divided into three parts.The first part aims to review the developments of chiral drugs and asymmetric synthesis, from which derived the present research topic backgrounds and works.Synthesis and applications of allylation from aldehydes are the second part of the thesis. By optimizing the reaction conditions, such as solvents, temperature, time and chiral auxiliaries like N,N\'-dibenzyl tartamide, N,N\'-p-dimethylphenyl tartamide, N,N\'-o-dimethylphenyl tartamide, N,N\'-o-dichlorophenyl tartamide, N,N\'-a-dinaphyl tartamide, N,N\'-dicyclohexyl tartamide and N,N\'-diphenyl tartamide, ideal experimenttal conditions are obtained according to HPLC monitoring, as well as the auxiliaries\' recoveries experiments. Starting from benzaldehyde and 3-bromopropaldehyde, N,N\'-dibenzyl tartamide is considered the best auxiliary in this reaction.

本文介绍了醛的不对称烯丙基化反应,以光学纯酒石酸为原料,研究了不同构型手性配体在醛的烯丙基化反应中的立体选择性,全文共分三部分十个章节:第一部分对当前手性药物和手性技术进行了概述,并由此展开了本文的研究背景和任务;第二部分为有机合成部分,对醛的不对称烯丙基化反应进行了深入探讨,以苯甲醛为原料对反应条件进行优化,在优化的反应条件下对制备的七种可回收手性酰胺配体(N-苄基酒石酸二酰胺、N-对甲苯基酒石酸二酰胺、N-邻甲苯基酒石酸二酰胺、N-邻氯苯基酒石酸二酰胺、N-a-萘基酒石酸二酰胺、N-环己基酒石酸二酰胺和N-苯基酒石酸二酰胺)进行筛选,优化配体回收实验条件,最终确定出N-苄基酒石酸二酰胺在苯甲醛的不对称烯丙基化反应中具有较大优越性,结晶回收的手性配体光学纯度保持不变。

Chapter 2 has analysized the conversly synthetic means of solanesol and designed novelly synthetic routes of solanesol and key intermediate Chapter 3 has summarized the preparation of trans-3-methyl-4-hydroxy (bromo-2-butenyl oxy methyl benzene In chapter 4 ,a novel technology of important intermediate(all trans-8-bromo geranyl acetate),which is suitable for industrial procedure , was found .meanwhile,an another new way has been invented ,of which the key intermediate (all trans-8-hydroxy geranyl acetate) has been produced.

第二部分分析了茄尼醇的逆合成方法,设计了一条适合于合成茄尼醇的合成路线及其重要中间体的合成路线。第三部分研究了重要中间体[Trans-3-甲基-4-羟基-2-丁烯基乙酰基(苄基,2,3-二氢吡喃基)醚]的合成新方法,找到了一条适合于工业化生产的制备反式-3-甲基-4-羟基-2-丁烯基苄基醚的新方法。第四部分研究了重要中间体[-3,7-二甲基-8-羟基-2,6-辛二烯-1-醇乙酸酯、-3,7-二甲基-8-溴-2,6-辛二烯-1-醇乙酸酯]的合成新方法,找到了一条适合于工业化生产的制备它们的新方法;同时研究了一条制备-3,7-二甲基-8-羟基-2,6-辛二烯-1-醇乙酸酯的另一新方法。

Fourteen new pyrethroids containing isoxazole were designed and synthesized from 4-isopropyl-3-substituted phenyl-5-hydroxyl isoxazoles as major material, whose structures were also characterized by IR, 1H NMR and elemental analysis.

以4-异丙基-3-取代苯基-5-羟基异噁唑和3-苯氧基苄基溴为原料,三乙胺为缚酸剂,设计并合成了14个未见报道的4-异丙基-3-取代苯基-5-异噁唑基-(3'-苯氧基)苄基醚。通过红外光谱、核磁共振、元素分析等手段,确证了它们的化学结构。

By synthesizing the hapten LBc starting from the metabolite of bifenthrin (2-methyl-3-phenylbenzyl alcohol), LBs (2-methyl[1,1-biphenyl]-3-ylmethyl 3-carboxyl-2,2-dimethylcyclopropane carboxylate and Lby (2-methyl[1,1-biphenyl]-3-ylcarboxylic acid , Three haptens were praparaed which were used in next step.

利用联苯菊酯的代谢物联苯醇合成了联苯菊酯的半抗原LBc(2-甲基-3-苯基苄基氧基羰基丙酸)、LBs(2-甲基-3-苯基苄基-3-羧基一2,2-二甲基环丙烷羧酸)和LBy(2-甲基-3-苯基苯甲酸)。

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Now, however, all children continue in "comprehensive" schools, and the eleven-plus determines which courses of study the child will follow.

然而现在,所有的孩子都要在综合学校继续学习,所以这次考试只是决定他们将要学习哪些课程。

Cultivatable land , and led to a general recognition that development must not be carried at the cost of agriculture .

城区的迅速扩大在很多情况下侵占了宝贵的可耕地,使人们普遍认识到发展不能以牺牲农业为代价。

Detailed Intrinsic Reaction Coordination calculations were carried out to guarantee the optimized transition-state structures being connected to the related tautomers.

同时,做了详尽的内禀反应坐标计算,以保证所得到的过渡态连接相应的始末异构体。