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芳基胺

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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。

Chapter two: Using 5-(4-aminophenyl)-10,15,20-triphenylporphyrin as thestarting compound, the classical diazotization of aniline and the resulting reaction ofdiazo salts were applied to porphyrin for the first time, and a series of asymmetriclysubstituted meso-tetraarylporphyrins including 5-(4-chlorophenyl)-10,15,20-triphenylporphyrin, 5-(4-iodinphenyl)-10,15,20-triphenylporphyrin, 5-(4-cyanophenyl)-10,15,20-triphenylporphyrin, 5-(4-bisphenyl)-10,15,20-triphenylporphyrin and 5-(4-hydroxylphenyl)-10,15,20-triphenylporphyrin were synthesized.

第二章:在已合成的5-(4-氨基苯基)-10,15,20-三苯基卟啉基础上,首次将芳胺的重氮化及重氮盐反应应用于卟啉,合成了5-(4-氯苯基)-10,15,20-三苯基卟啉、5-(4-碘基苯基)-10,15,20-三苯基卟啉、5-(4-氰基苯基)-10,15,20-三苯基卟啉、5-(4-联苯基)-10,15,20-三苯基卟啉和5-(4-羟基苯基)-10,15,20-三苯基卟啉等一系列不对称取代的meso-四芳基卟啉。

Eight novel N,N′-naphthalene acyl substituted aromatic acylamino thiocarbamide s(Ⅱ1~Ⅱ8) were synthesized from aryl acylhydrazine and α-naphthalene acyl isothiocyanate, which was obtained by the reaction of potassium thiocyanate with α-naphthalene acyl chloride obtained from 2-naphthylacetic acid and thionyl chloride in anhydrous benzene.

通过α-萘乙酸和SOCl2在无水苯中反应制得α-萘乙酰氯,与硫氰酸钾反应生成α-萘乙酰基异硫氰酸酯,再与芳基酰肼进行加成反应,合成8种新型N,N′-萘乙酰基取代芳乙酰胺基硫脲类化合物(Ⅱ1~Ⅱ8)。

Eight novel N,N′-naphthalene acyl substituted aromatic acylamino thiocarbamides(Ⅱ1~Ⅱ8) were synthesized from aryl acylhydrazine and α-naphthalene acyl isothiocyanate, which was obtained by the reaction of potassium thiocyanate with α-naphthalene acyl chloride obtained from 2-naphthylacetic acid and thionyl chloride in anhydrous benzene.

通过α-萘乙酸和SOCl2在无水苯中反应制得α-萘乙酰氯,与硫氰酸钾反应生成α-萘乙酰基异硫氰酸酯,再与芳基酰肼进行加成反应,合成8种新型N,N′-萘乙酰基取代芳乙酰胺基硫脲类化合物(Ⅱ1~Ⅱ8)。

The major contents in this thesis are described as follows:(1) Seven new thiol fluorescence reagents containing 2-phenylbenzoxazole (or 2-phenylbenzothiazole) derivatives or benzanthrone as fluorphore and iodinacetylamine or maleimide as reaction groups have been synthesized.

本论文的研究工作主要分为以下几个方面:(1)以碘乙酰胺或马来酰亚胺为反应基团和以2-芳基苯并噁唑类化合物或苯并蒽酮为荧光团,首次合成了七种新的碘乙酰胺类和马来酰亚胺类巯基荧光试剂。

Chapter 2 presents our studies on aromatic amide-derived phosphine applied to room temperature Suzuki cross-coupling of unactivated aryl chlorides with aryl boronic acids.

第二章主要研究了芳基酰胺衍生的膦配体在不活泼的氯代芳烃同芳基硼酸在室温下的Suzuki偶联反应中的应用。

Studing on samarium diiodide promoted asymmetric intramolecular reducing coupling reactions, we have made the resolution of the racemic biaryl dials by using enantiomeric N-tert-butanesulfinamine as the resolving reagent successfully and thus obtained a series of axially chiral biaryl dials with high enantiomeric excess.

中文摘要在二碘化钐促进的分子内不对称还原偶联反应中,我们不仅对联芳基二醛底物的合成路线进行了优化,还发现N-叔丁基亚磺酰胺辅基可以作为手性试剂,成功地对联芳基骨架二醛化合物进行拆分,得到高对映体过量的轴手性二醛类化合物。

Benzoyl chloride was treated with potassium selenocyanate in dichioromethane by using polyethylene glycal-400 as the solid-liquid phase transfer catalyst to yield the corresponding benzoyl isoselenocyanate. This intermediate did not need to be isolated and directly reacted with arylamines, affording the N-benzoyl-N'-arylselenoureas 2a~2p. These compounds were characterized by IR, 1H NMR spectra and elemental analysis and the single crystal structure of 2k has been confirmed by X-ray crystallographic analysis.

以PEG-400为固液相转移催化剂,通过苯甲酰氯与硒氰酸钾反应合成了中间体苯甲酰基异硒氰酸酯,该中间体不需分离,直接与芳胺反应,得到N-苯甲酰基-N'-芳基硒脲(2a~2p),这些化合物用1H NMR,IR及元素分析进行了表徵,并用X射线单晶衍射确定了化合物2k的单晶结构。

Based on the experimental results, it could be consequentially concluded that N-methoxycarbonylation of aromatic amines was followed by the exclusive N-methylation of methyl N-aryl carbamates during the reaction process.

苯环上有钝化基团的一级芳胺反应活性比较好,获得N-甲基-N-芳基氨基甲酸甲酯的产率较高,反应时间也较短;而苯环上活化基团的存在,则会降低一级芳胺的反应活性。

Firstly, phenyliodine diacetate was immobilized to the 2% cross-linked polystyrene or the liner polystyrene resin. The more iodine the resin had, the lower conversion to phenyliodine diacetate. We made our endeavor to extend the range of useful application of polystyrene supported phenyliodine diacetate in organic synthesis:(1) the reagent was used as an effective reagent of carbonyl regeneration from oximes and semicarbazones of ketones.(2) the reagent was also applied to the synthesis of 1, 3, 4-oxadiazoles, 1, 3-disubstituted-2-pyrazoline, 2-arylbenzoxazole from aldehyde N-acylhydrazones, aldehyde hydoazones and phenolic Schiff's bases respectively.

首先,我们以2%交联的聚苯乙烯和线性的聚苯乙烯树脂为载体,制备了聚合物负载的二醋酸碘苯,通过研究发现:(1)聚苯乙烯二醋酸碘苯是酮肟、缩氨脲有效的去保护试剂,不仅芳香酮,脂肪酮和α,β不饱和酮的肟、缩氨脲也能顺利转化为相应的酮,实现酮基的再生;(2)我们还利用此试剂,分别与醛的N-酰基苯、N-酰基苯腙及邻羟基芳亚胺反应,在温和的条件下发生成环反应,以良好的产率生成1,3,4-噁二唑、吡唑啉和二取代苯并噁唑等杂环化合物;(3)聚苯乙烯二醋酸碘苯还可有效地将邻羟基芳酮的酰腙经氧化、重排成1,2-二酰基苯。

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然而,正如其名字所指出的那样,CD盘不能写,也不能用任何方式改变其内容。

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