氨基化合物

Tetrahydroisowuinolin derivatives and phthalide derivatives were designed and synthesized on the basis of a PDE4 inhibitor pharmacophore model set up through computer simulation. Some tetrahydroisowuinolin derivatives synthesized were evaluated on their activity against PDE4 for study on the structure-activity relationship.(7-cyclopentyloxy)-6-methoxy-3,4-dihydroisoquinolin-2(1H)-yl(4-hydroxy-3-methoxyphenyl)methanone (155) and Methyl 7--6-methoxy-2-(4-methoxy- benzoyl)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (170) showed good activity against PDE4, which were chosen as the lead compounds to design and synthesize another analogs in order to develop selective PDE4 inhibitors with better activity.

分别设计合成了以四氢异喹啉和氨基苯酞为骨架的两类小分子杂环化合物，并对部分四氢异喹啉衍生物测试了其相关的生物活性，初步确定了其构效关系，发现了两个对PDE4有较好抑制活性的先导化合物(7-cyclopentyloxy)-6-methoxy-3，4-dihydroisoquinolin-2(1H)-yl(4-hydroxy-3-methoxyphenyl)methanone (155)和Methyl 7--6-methoxy-2-(4-methoxy- benzoyl)-1-phenyl-1，2，3，4-tetrahydroisoquinoline-3-carboxylate (170)。

In order to find new pyrazole leading compounds, 14 1--4-(pyrazol- 5-ylcarbony)semicarbazide devivatives were synthesized from 4-chloro-3-ethyl-1-methyl-5-pyrazole car-bonydrazide and substituted phenylisocyanate.

为了寻求新的吡唑先导化合物，用4-氯-1-甲基-3-乙基-5-吡唑甲酰肼与取代苯基异氰酸酯反应得到了14个新的1-吡唑酰基-4-芳基氨基脲类化合物。

A new photochromic organic compound of thiosemicarbazone, 4-( p -bromo-α-methylaminothiocarbonyl hydrazonobenzal)-2,5-dihydro-3-methyl-5-oxo-1-phenyl pyrazole, was synthesized and characterized by elemental analyses, IR, 1H NMR spectra, and X-ray single-crystal diffraction analysis.

文章合成了一个新的有机化合物1-苯基-3-甲基-4-对溴苯亚甲基-吡唑啉酮-5 缩甲基氨基硫脲(1)，并分别用元素分析、红外光谱、氢核磁共振及X-射线单晶衍射对化合物的结构进行了确证和表征。

The thermal property studies indicate that the mass loss of compound B was 54.39% at 242.2~750℃, and when the temperature was 1000℃, there was 25.11% char residue left, which showed that the title compound has a good thermal stability and char forming capability. Using acetonitrile as the solvent instead of trichloromethane or 1, 2-dichloethane gave higher yield. During the synthesis, the yield was very low when triethylamine was used as acid acceptor alone, and when a little amount of 4-dimethylaminopyridine was added at the same time, the yield could be 81%.

结果表明，所合成的化合物B的结构与预期的结构一致；热性能研究表明，化合物B在242.2~750℃质量损失为54.39%，1000℃时仍有25.11%的炭残渣，显示出优异的热稳定性和成炭性；在相同反应条件下，用乙腈作为溶剂的反应产率比使用氯仿和二氯乙烷为溶剂的高，并且在合成过程中，单独使用三乙胺作为缚酸剂时产率很低，而当同时加入少量4-二甲氨基吡啶时，产率可达81%。

Based on literature procedures, a dithiol tridentate ligand containing amino groupand its iron carbonyl complex (4) are synthesised and characterised. An attempt isalso made to protonate this complex.

在文献方法的基础上也合成了含有氨基的二硫醇三齿配体及其铁羰基化合物[Fe_2(SCH_2)_2C(CH_2NH_2)_5](4)的合成与表征，尝试了合成该化合物的质子化产物。

As CAAX-mimetics, 1, 3-dihydro-5-phenyl-2-H-1, 4-benzodiazepin-2-one was modified by linking carboxyl groups with various carbon through N-1 and C-3, 3-(imidazol-4-yl) propion amido group with different substituents was connected at C-7; In the synthesis of bisubstrate analogues, thiocarbamido compounds was alkylated by alkyl iodide and then hydrolyzed to give alkylthiol benzoate compounds.

1，4-苯并二氮杂草-2-酮类化合物的合成过程中分别对其1、3、4和7位进行了基团变化，在1和3位连接不同长度含羧基或酯基的侧链，在7位连接不同取代的咪唑丙酰氨基。在苯甲酸硫醇酯化合物合成过程中，建立了一种硫原子连有不同长度碳链的苯甲酸硫醇酯的合成方法。

The yield was 47.3%. A series of21 azo-1,3,4-thiadiazole compounds were synthesized by diazotizing of2-amino-5-alkyl-1,3,4-thiadiazole with nitrosylsulfuric acid, then couplingwith phenol, substituted phenol or naphthol. The yields were 19.6～58.8%.16 of them were new compounds.

制得的2-氨基-5-烃基-1，3，4-噻二唑用亚硝酰硫酸进行重氮化，再与苯酚、取代苯酚或萘酚发生偶合反应合成了21个偶氮-1，3，4-噻二唑类化合物，其中16个为新化合物，收率为19.6～58.8％。

This method had been applied to determination of the optical purity of the product from asymmetric ring opening of meso- epoxides.

方法已用于非手性环氧化合物不对称开环反应产物β-氨基醇及β-羟基硫醚类化合物的光学纯度鉴定。

The recent research progress of oxidation carbonylation of amines/β-amino alcohols, alkoxycarbonylation of epoxides, carbonylative Suzuki coupling, carbonylative Sonogashira, and double carbonylation of aryl iodides has been presented, focusing on the carbonylation reactions studied by us in the past few years, with 81 references.

综述了胺／氨基醇类化合物氧化羰化、环氧化合物氢酯基化、碘代芳烃的羰化Suzuki偶联、羰化Sonogashira以及双羰基化等重要羰基化反应的研究状况，特别是结合本课题组近年来在该领域中的工作，并对羰基化反应的发展及应用前景进行了展望。

The good results can be obtained with the newalgorithm; the local minimal can be avoided in some degree. In this paper, neural networks also were applied to quantitativestructure-property relationships analysis:1Studies on the toxicity of aniline, nitrobenzene and phenol derivatives and their structures.2 Studies on HEPT compounds for their anti-aids.3 Studies on nitrogen mustards and 2-formylpyridine thiosemicarbazone compounds for their anti-cancer.4 Studies on phenol and aniline derivatives for their gas chromatographic retention values.5 Studies on discrimination of tea by Self-organizing feature map network.

本论文还利用上述方法进行了一些定量结构活性相关性研究，主要内容： 1环境中有毒有害有机物的定量结构活性相关性研究。2抗艾滋病类药物定量结构活性相关性研究。3抗肿瘤类药物(氮芥子气类化合物和2-甲酸吡啶缩氨基硫脲类化合物)定量结构活性相关性研究。4苯酚和苯胺类衍生物色谱比移值预测。5将神经网络用于茶叶的分类。

This one mode pays close attention to network credence foundation of the businessman very much.

这一模式非常关注商人的网络信用基础。

Cell morphology of bacterial ghost of Pasteurella multocida was observed by scanning electron microscopy and inactivation ratio was estimated by CFU analysi.

扫描电镜观察多杀性巴氏杆菌细菌幽灵和菌落形成单位评价遗传灭活率。