内酰亚胺

Lactam was gained by the Staudinger reaction of imine and olefineketone in the presence of N-heterocyclic carbene catalyst.

以N-杂环卡宾催化剂1催化亚胺与烯酮之间的Staudinger反应，得到相应的β-内酰胺。

The cis novel bisoxazoline ligands L1-L4 have been synthesized through the treatment of new cis dihydroxy diamide with p-toluenesulfonyl chloride in the presence of catalytic quantity of 4--pyridine, and the cis dihydroxy diamide could be achieved from the condensation of the amino alcohols and cis cyclopropane dicarbonyl chloride prepared via oxidation and halogenation from cis-2,2-dimethyl-3-formylcyclopropanecarboxylate with DCC.

我们以蒈醛酸内酯为起始原料，经过氧化反应、酰氯化反应得到顺式环丙烷二酰氯，然后在二环己基碳二亚胺的催化下与相应的氨基醇反应合成了顺式二羟基酰胺，再用对甲苯磺酰氯将羟基活化，最后在二甲氨基吡啶的催化下关环合成顺式双噁唑啉配体L1～L4。

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。

The loss or diminishment of OprD2 was the main reason for the imipenem resistance of P.aeruginosa in our hospital, but its effect on meropenem resistance deserved further study.

在对亚胺培南耐药的菌株中，合并有其他β-内酰胺类抗生素耐药的菌株达到62.34%(48/77)。32株Pa外膜蛋白电泳结果显示OprD2相对含量在耐药组为0～3.5%(其中有一株为8.70%)，敏感组为6.20%～10.20%。

Results: The proportion of Gram-negative bacilli rose obviously, so did the opportunistic pathogen's and Yeasts detected rate. Most drug sensitive tests showed the drug-fast rate turned to be high. Escherichia coli, Salmonella and Citrobacter resistant and so on to fluoroquinolones was 57%~97%. These bacteria to imipenem showed excellent activity. Meticillin-resistant-staphylococcus resistant to ciprofloxacin, norfloxacin, clindamycin, tetracycline, erythromycin, cefazolin and ampicillin were 40.9%, 42.4%, 63.6%, 72.2%, 85.9%, 100.0% and 100.0%, respectively Streptococcus and Enterococcus resistant to major β-lactams-penicillin, aminoglycosides, macrolides, tetracyclines and sulfonamides were between 36.0% to 100.0%.

结果：革兰阴性杆菌比例显著升高，条件致病菌和酵母样真菌检出机会显著增多；药敏结果显示多数临床细菌对常用抗生素的耐药趋势在不断上升；大肠埃希菌、沙门菌和枸橼酸杆菌等革兰阴性杆菌对喹诺酮类药物的耐药率达57%~97%，亚胺培南则对阴性杆菌有较高的敏感覆盖率；耐甲氧西林葡萄球菌对环丙沙星、诺氟沙星、氯洁霉素、四环素、红霉素、头孢唑啉和氨苄西林的耐药率分别为40.9%、42.4%、63.6%、70.2%、85.9%、100.0%和100.0%；链球菌和肠球菌对多数β内酰胺类青霉素、氨基糖苷类、大环内酯类、四环素类以及磺胺类药物均呈高度耐药，耐药率在36%~100%。

To Dec. 2003 years in Yuxi city People's Hospital. RESULTS: The proportion of G－ bacilli were much. The opportunistic pathogen's and Yeasts detected rate rose obviously. Most drug sensitive tests showed the drug-fast rate turned to be high. Escherichia coli, Salmonella and Klebsiella and so on to fluoroquinolones was 50～97.7%. These bacteria to imipenem showed excellent activity. MRS resistant to ciprofloxacin, norfloxacin, clindamycin, tetracycline, erythromycin, gentamycin, trimeth/sulfa and cefazolin were above 50%. Streptococcus resistant to major β-lactams-penicillin, aminoglycosides, macrolides, tetracyclines and sulfonomides were highness.

结果：G－杆菌比例居多，条件致病菌和酵母样真菌检出机会显著增高；药敏结果显示多数临床细菌对常用抗生素的耐药趋势在不断上升；大肠埃希菌、沙门菌和克雷伯菌等G－杆菌对喹诺酮类药物的耐药率在50％～97.7％，亚胺培南则对阴性杆菌有较高的敏感覆盖率；耐甲氧西林葡萄球菌对环丙沙星、诺氟沙星、氯洁霉素、四环素、红霉素、庆大霉素、复方新诺明和头孢唑啉的耐药率均在50％以上，链球菌对多数β内酰胺类青霉素、氨基糖苷类、大环内酯类、四环素类以及磺胺类药物呈高度耐药。

It should be noted that the reaction with alkylimines failed to give the,β-lactam under current standard reaction conditions.

值得注意的是，在相同条件下，烷基亚胺参与的该反应都没能得到相应的β-内酰胺。

Drug sensitive test and three-dimensional test220 strains of Pa were isolated from hospitalized patients between 2003 and 2007. K-B method was used to tested the susceptibility of 10 different antibiotics. IRPa was screened by testing the minimal inhibitory concentration of imipemem by using agar diluiion method.The susceptibility of these IRPa to the antibiotics was analysised. Three-dimensional test was used to identify the different kinds of beta lactamases from 220 strains of Pa.2.Carbarpenems hydrolytic enzyme genes and oprD2 gene were detectedamong the selected IRPa strains, PCR method was performed to detect carbapenemase genes which included GES、KPC、SPM、VIM、IMP、GIM gene and the oprD2 gene;Multiplex PCR were used to detect OXA genes and plasmid-mediated AmpC beta lactamase genes; The expression of the chromosomal AmpC beta lactamases and oprD2 genes in IRPa strains were analyzed by Real-time PCR.3.Identification and characterization of integronsIntegrase gene was detected by PCR, and the classification of integrons was performed by using restriction fragment length polymorphism.PCR was performed to detect the qacE△1-sull gene,and the gene cassetes which are located at variable region of integrons in the strains were detected to be positive.

方法1、药敏实验和三维实验收集2003～2007年临床分离的220株Pa，对这些菌株采用K-B法测定10种临床常用抗生素的药敏情况，同时采用琼脂稀释法检测亚胺培南的最低抑菌浓度(Minimal inhibitory concentration，MIC)，筛选出对亚胺培南耐药的铜绿假单胞菌，并分析其对其它抗生素的药物敏感率；采用三维实验的方法分析220株Pa产β内酰胺酶的类型。2、碳青霉烯类水解酶和oprD2蛋白的检测针对鉴定的IRPa菌株，采用普通PCR方法检测具有碳青霉烯水解作用的β内酰胺酶耐药基因(GES、KPC、SPM、VIM、IMP、GIM基因)和oprD2基因，采用多重PCR的方法检测OXA型基因和质粒携带的AmpC酶基因，用荧光定量RT-PCR方法检测oprD2蛋白基因表达情况；同时对产AmpC酶的Pa(25株，含IMP耐药和敏感株)用RT-PCR方法检测AmpC酶基因的表达量情况。3。

In the last part we first synthesized the propargylic amines though several methods and then developed a new methodology for the synthesis of -α-chloroalkylidene-β-lactams via the catalysis of PdCl〓 with CuCl〓 and BQ with moderate to good yields and good generality.

论文的第三部分工作是我们首先通过几种方法合成了炔丙基胺化合物，接着对PdCl〓催化的炔丙基胺的羰基插入环化反应进行了研究，以中等收率得到-α-氯代亚烷基-β-内酰胺化合物，反应的普适性良好。

A plausible process of this reaction is as following: Aldehyde was in equilibrium with the enol form, aldehyde reacted with aniline catalyzed by 2,2,2-trichloroacetic acid to afford imine, the generated imine immediately reacted with enol to form intermediate via intramolecular cyclization.

我们发现一分子芳基叠氮和一分子三苯基磷反应生成一分子磷亚胺，后者与由两分子取代的苯氧乙酰氯原位生成的烯酮反应生成4-亚烷基-β-烷基-内酰胺，其串联过程涉及烯酮亚胺的形成及其与烯酮的[2+2]的环加成反应。

But we don't care about Battlegrounds.

但我们并不在乎沙场中的显露。

Ah! don't mention it, the butcher's shop is a horror.

啊！不用提了。提到肉，真是糟透了。