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加成化合物

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Generally speaking, the reaction types involvingα-oxoketene--acetals mainly include the regioselective addition-aromatization with organometallic reagents, conjugate addition-cyclization with nitrogen nucleophilicspecies, nucleophilic reactions ofα-carbon, acting as odorless dithiol equivalentsin thioacetalization, Michael additions and [5+1] annulation, as well as the synthetic applications based on the above reactions.

一般来说,基于α-羰基二硫缩烯酮化学的反应主要为:与金属有机试剂的选择性加成反应,与氮亲核体的共轭加成反应,α-碳原子的亲核性及相关反应,烷硫基作为硫醇的替代试剂的应用,α-羰基二硫缩烯酮在碳环、杂环化合物合成中的应用等。

The reaction of α-hydroxyketone with Michael acceptor nitroalkene.was studied. After many experiments, we then found that in the presence of Zn2 and cinchonine, the α-hydroxyketone could successfully react with nitroalkene. Under our optimized condition, we gained the 95% yield of product with the ratio of syn : anti of 3:1 and 72% ee value for syn-product.

有机碱作用下α-羟基酮对硝基烯烃的加成反应研究研究了α-羟基酮类化合物与Michael受体硝基烯烃类化合物的反应,通过分析和实验发现在Zn2和辛可宁的作用下α-羟基苯乙酮能够与硝基烯烃化合物顺利反应,在优化的条件下以95%产率和3:1的Dr主要得到顺式产物,其中顺式产物的ee值最高为72%。

Target compounds have been synthesized by condensation of the aromatic nucleus and amino heterocylcle with acyl isocyanates or acylisothiocyanates in absolutely anhydrous and aprotic solvent.

为了寻找高活性的农药品种,利用生物等排原理和亚结构连接法,对脲类化合物的母体结构进行了修饰,将芳氧羧酸类及吡唑环引入酰基脲母体结构中,利用酰基异氰酸酯与杂芳环胺类化合物在无水非质子溶剂中发生亲核加成反应,合成了四个系列21种新的酰基脲类目标化合物。

The facts that type I compounds could easily undergo deamination reaction to form α-methylene cyclopentanone derivatives and they could react with glutathione to form an adduct provided sufficient evidence for the hypothesis that the compounds acted as masked α-methylenecyclopen- tanones and reacted with biologically important sulfhydry-containing enzymes, and thus produced anticancer activity.

Ⅰ类化合物在稀溶液中极易进行去胺基化反应形成α-亚甲基环戊酮类化合物。并且Ⅰ类化合物于稀溶液中易与谷胱苷肽进行结合,这些事实为Ⅰ类化合物作为隐蔽的α-亚甲基环戊酮与酶进行加成,从而导致酶失活而具有抗癌活性的设想提供了证据。

In our research on study chemical reaction of active methylene compounds and brom-acetophenone. Because of brom-acetophenone is compound that contain carbonyl and halogen ,which will take place electrophilic substitution and nucleophilic addition. When active methylene compounds are ethyl acetoacetate and β-diketone, controlling reaction condition, we have found that mono-substitution's production and di-substitution's. production is isolated; active methylene compounds are acetoacetanilide and acetoacetanilide derivate, pyrrolidin-2-one derivants were obtained by substitution and close-ring reaction .but there is no report about it.

本文是让活泼亚甲基类化合物与溴代苯乙酮发生化学反应,由于溴代苯乙酮是含有羰基的卤代烃结构,它可以发生亲电取代和亲核加成反应,当活泼亚甲基类化合物为乙酰乙酸乙酯和β-二酮时,控制反应条件可以发生单取代和双取代两种产物;当活泼亚甲基类化合物为乙酰乙酰芳胺类化合物来反应时,溴代苯乙酮中的羰基与氨基会发生分子内的关环反应生成吡咯烷-2-酮衍生物,这在以前的研究中是没有发现的。

A novel carbonyl transposition led by anilines'nucleophilic addition to methyl 2-keto α-D-glucopyranoside was discovered. And the mechanism of the reaction concerned to an enol rearrangment was provided through tracing the change of 〓H-NMR and 〓C-NMR of a hemiacetal intermediate which was obtained in the reaction of o-phenylene diamine with 2-keto glycoside. Both the intermediate and the converting product were identified by 〓H-NMR,〓C-NMR,〓H-〓H COSY and HMQC.

一、发现了2-位氧化α-甲基D-葡萄糖苷的芳胺亲核加成引起羰基转位的新方法,利用核磁共振氢谱及碳谱对邻苯二胺与2-位氧化α-甲基D-葡萄糖苷加成生成的稳定中间体半缩酮化合物在氘代丙酮中的变化进行跟踪,结合对转化产物的氢氢相关谱和HMQC结构确证,提出了该反应中2-位羰基通过烯醇化互变而转至3-位的机理并得到了验证。

The compound obtained in step i., or the acid addition salt thereof, is converted into pyridoxine or an acid addition salt thereof.

将步骤i。获得的化合物或其酸加成盐转化成吡哆素或者转化成吡哆素的酸加成盐。

E. value of productions were detected by high performance liquid chromatography. Results The chiral aminoalcohol ligand compound Ⅰ can promote the asymmetric allylation of acylhydrazones and the yield was 57%; The highest values of e. e. obtained for this reaction was 22%.

结果 手性氨基醇配体化合物Ⅰ能够促进烯丙基三氯硅烷和酰腙的烯丙基化加成反应,在它的辅助作用下,烯丙基化加成产物的产率可达到57%,对映体过量值最高达到22%。

The target compounds were obtained in high yield through Michael conjugative addition of amines to methyl acrylates, cyclocondensation of the obtained diadducts in the presence of sodium methoxide,and decarboxylation of the cyclocondensation products in acid.

以胺类化合物为原料,与丙烯酸甲酯经过两次Michael加成得到N,N 二丙酸甲酯类化合物,该化合物在甲醇钠存在下进行环合,在酸性条件下脱羧,高收率得到4 哌啶酮类化合物,从而证明了这是一条合成N 取代 4 哌啶酮类化合物的普遍方法。

A series of new isoxazolines were prepared by 1,3-dipolar cycloaddition between different mono-substituted styrenes and new 1,3-dipolar compounds which were synthesized by the reaction of N-methylhydroxylamine sulfate with aromatic carbonyl compounds.

以N-甲羟胺硫酸盐和芳香族羰基化合物为主要原料合成了一系列不同的1,3-偶极化合物,并合成了四种不同的单取代苯乙烯。以该系列1,3-偶极化合物和单取代苯乙烯为主要中间体,采用1,3-偶极环加成反应合成了一系列异恶唑啉类新化合物。

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