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We screened a set of Lewis base organocatalysts derived from chiral pipecolinic acid and tert-butanesulfinamide for the reduction of-N-Cbz-1- phenylpropenamine, including newly designed ones and some of those previously developed in our lab. However, only moderate stereoselectivities, albeit high yields were obtained.

在本课题组前期研究的基础上,我们筛选并设计了一系列以手性哌啶酸和叔丁基亚磺酰胺为母体的有机小分子路易斯碱催化剂,它们能催化三氯氢硅对-N-苄氧羰基-1-苯基丙烯胺的不对称还原,获得很高的收率和中等的对映选择性,并且具有很好的底物普适性。

With the analysis and discussion of their photoini- liability, it was indicated that their max are all around 330 nm, and all of them have excellent solubility in water and good photoinitiability. Furthermore, the three Photoinitiators with α-tert-amine are obviously superior to the one with just α-sec-amine. Among the four photoinitiators l-(4-aminophenyl)-2-diethylamino-l- propanone dihydrochloride is the best and it has excellent use value.

通过对它们的光引发性能测试和构效关系的分析探讨,表明四种光引发剂的最大吸收波长λ_(max均在330nm左右,具有优异的水溶性和良好的光引发性能,其中具有α-叔胺基团的三种光引发剂明显优于具有α-仲胺基团的光引发剂,尤其以1-(4-氨基苯基)-2-二乙胺基-1-丙酮盐酸盐的光引发性能最好,具有推广应用前景。

Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

本发明涉及含有连接在5元杂环上的稠合至环烷基或者杂环的苯基或者吡啶基环的二环化合物,包括其药学上可接受的盐和前药,它们是G蛋白偶联受体40(GPR40)激动剂并且可以用作治疗性化合物,特别是在2型糖尿病和与这些疾病相关的症状中用作治疗性化合物,这些症状包括肥胖病和脂质疾病,比如混合或者糖尿病型血脂异常症、血脂质过多、高胆甾醇血和高甘油三酯血症。

A new convenient synthesis of a series of 1-aryl-2-propanones using aromatic amines as precursors, via diazo reaction and improved Meerwein arylation reaction under mild conditions, was achieved. In addition, 1-[3,5-bisphenyl]-2-propanone is a new compound among the synthesized compounds. This approach is an efficient synthetic method for the aryl-propanones with the different substituting groups.

以芳香胺为原料,经重氮化和改进的Meerwein芳基取代反应,合成了一系列的1-芳基-2-丙酮,其中1-(3,5-二三氟甲基苯基)2-丙酮是一个新化合物改进后的方法简化了合成步骤,提高了收率,可方便地用于在苯环上具有不同取代基的芳基丙酮的合成。

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