化合物

The condensation of 3 carbethoxy isoquinol 4 one with carbamidine, amidine, carbamide and sulfocarbamide gave isoquinolo pyrimidine derivatives, respectively and isoquinolo quinoline derivatives were synthesized by the reaction of o aminobenzaldehyde or o aminopiperonal with isoquinol 4 one.

报道了利用 3 乙氧甲酰基异喹啉 4 酮分别与胍、脒、脲及硫脲类化合物缩合反应合成异喹啉并嘧啶衍生物，邻氨基苯甲醛、邻氨基胡椒醛分别与异喹啉 4 酮反应合成异喹啉并喹啉化合物。6个新化合物的结构通过元素分析、红外光谱、核磁共振氢谱和质谱予以证

The structures of these two molecules are almost the same with slight differences in bond lengths and bond angles. And compounds 1-3 are the first examples of this type containing amido and ethoxide groups.

而且到目前为止，Sn4O4的梯子状结构中同时含有氨基和乙氧基的化合物还未见报道，化合物1，2和3为首次合成此类化合物。

In part one, the reactions of some active fluorine-containing compounds such as 2, 2-dihydropolyfluoroalkanoic acids and ethyl 2-hydropolyfluoroalkenoates were studied and various fluorine-containing heterocyclic compounds were synthesized. Using 2, 2-dihydropolyfluoroalkanoic acids as the starting material, 4-fluoroalkyl quinolin-2-ols, 2- [ -1-hydropolyfluoro-1-alkenyl] -4H-3, 1-benzoxazin-4-ones, 1-aryl -4, 9-dihydro-3-fluoro-alkyl-1H-pyrazo [3, 4-b] quinolin-4-ones, 5-fluoroalkyl-12H-quin olino [2, 1-b] quinazolin-12-ones, 4-fluoroalkyl-1, 3-dihydro-1, 5-benzodiazepin-2-ones and 4-fluoroalkyl-2H-pyrido [1, 2-a] pyrimidin-2-ones were synthesized through its condensation reaction with anilines, anthranilic acid, N'-aryl-o-aminobenzamides, o-nitro aniline, o-amino pyridine and their derivatives and the subsequent transformations. 5-Fluoroalkyl isoxazolidines, 3-fluoro-3-fluoroalkylisoxazolidino [4, 3-c] quinolin-4-ones, 3-fluoroalkylisoxazolino [4, 3-c] quinolin-4-ones and 2-aryl-3per fluoroacylindoles were synthesized by inter-and intramolecular 1, 3-dipolar cycloaddition of fluorine-containing olefins and nitrones.

第二部分，我们研究了α，α-二氟苄基卤类化合物的亚磺化脱卤反应、产物的转化及全氟烷基亚磺酸盐与芳环化合物的全氟烷基化反应，发现全氟苄基碘或溴及α，α一二氟苄基溴在保险粉等亚磺化脱卤试剂引发下可生成相应的亚磺酸盐；全氟苄基亚磺酸盐与氯气或溴反应可生成全氟苄基磺酰氯或磺酰溴；在烯烃存在下，全氟苄基碘则与烯烃发生加成反应，生成相应的1：1加成产物；在三价醋酸锰的作用下，部分芳香化合物如茴香醚，二甲氧基苯，吡啶，喹啉等可以和过量的全氟烷基亚磺酸盐发生双全氟烷基化反应，反应表现出一定的区域选择性，产率良好。

Compound I was isolated from roots of Arnebia euchroma for the first time.

其中化合物Ⅰ是从新疆软紫草中首次得到，根据已检索的信息可知此化合物为新化合物。

Given the success of 9-aminocamptothecin and meanwhile to investigate the impact of substituents with electron-donating groups on the activity of these compounds, amino group was incorporated into the 7-position of benzimidazole, benzoxazole or benzothiazole.

将第Ⅲ类化合物中的喹诺酮环用其电子等排体色酮环代替，得到第Ⅲ类化物，以考察喹诺酮的氮原子被氧原子取代后对活性的影响，该类化合物包括9个化合物，其中含4个色酮开环产物。

The result indicates that the hydrogen bond formed by Arg24 in PTP-1B and benzotriazole molecules is of great importance for the selectivity of the compounds.

计算结果表明PTP-1B中的Arg24与化合物的氢键相互作用是提高选择性的重要因素，并且在R2位引入氢键供体且体积较大的强供电子基团，将有利于化合物抑制活性的提高，而在R2位取代基的末端引入氢键受体且体积较大的强吸电子基团，将有利于化合物选择性的提高。

In summary, 15 new N--2-(4, 6-dimethoxypyrimidin-2-yl-oxy)benzylamine derivatives with high herbicidal activity are obtained.

4氧桥双取代嘧啶苄胺类化合物也是一类具有高除草活性的化合物，在75 g ai／hm~2低剂量下，化合物主要表现出芽后除草活性。

The good herbicidal activity can not be observed at low dosage of 75 g ai/hm~2 for N-(mono-ester substituted phenyl)-2-(4, 6-dimethoxy-pyrimidin-2-yloxy)benzylamine derivatives in post-emergent and pre-emergent application.

主要研究结果如下：(1)氧桥单取代卤素嘧啶苄胺类化合物是一类具有高除草活性的化合物，在75 g ai／hm~2低剂量下，一些化合物表现出良好的芽后和芽前除草活性。

It is Concluded that the mode of action of pyrimidine benzylamine differs from the other typically commercial ALS inhibitors, such as sulfonylurea and pyrimidine salicylic acid herbicides. Its herbicidal activity is activated by the metabolic processes in the plants.

离体条件下，化合物104-4 IC_(50)＞100 mg／L，而除草剂双草醚IC_(50)值为10~(-5)～10~(-4)mg／L，说明化合物104-4对离体ALS没有抑制作用；活体条件下，化合物104-4对ALS有一定的抑制作用，且随着处理时间的延长，酶活力降低，对ALS的抑制作用增加。

The results of bioassay suggest that 2-methylthio-6-methyl-4-substituted pyrimidine and 4, 6-dimethoxy-2-substituted pyrimidine derivatives show herbicidal activity. In these target compounds, 4, 6-dimethoxy-2-substituted pyrimidine benzylamine and 4, 6-dimethoxy-2-Substituted pyrimidine benzylidene amine exhibit good herbicidal activity, and the herbicidal will be affected by the substituents in the benzene ring.

对分子库中的目标分子进行了生物活性筛选研究，发现其中的2-甲硫基-6-甲基-4-取代嘧啶衍生物和4，6-二甲氧基-2-取代嘧啶类化合物显示出除草活性，其中4，6-二甲氧基-2-取代嘧啶苄胺类化合物和4，6-二甲氧基-2-取代嘧啶亚苄胺类化合物具有较好的除草活性，而且其活性和苯环上的取代基有关。

The split between the two groups can hardly be papered over.

这两个团体间的分歧难以掩饰。

This approach not only encourages a greater number of responses, but minimizes the likelihood of stale groupthink.

这种做法不仅鼓励了更多的反应，而且减少跟风的可能性。