胺化

Mission:"equality and mutual benefit, reputation first, unity and cooperation and friendship between the long-term" supply products: ethylenediamine; diethylamide; triethylamine; Diethylenetriamine; three ethylene diamine; three ethylene amines 40; 40 Five ethylene amines; five ethylene amines 6; caprolactam; DMF; allyl amine; N, N dimethylaniline; propylamine; are butylamine; are TOA; 3 Poly Cyanamide; 1,2 c diamine; ethanolamine; diethanolamine, triethanolamine; potassium iodide, potassium hydroxide, potassium permanganate, toluene, xylene, toluene of chlorine ; Acetone, butanone; acetylacetone; ethyl acetate, butyl acetate; Y-butyrolactone; DMC; acetyl of methyl acetate; Sanfu acetyl acid; Sanfu acetyl B Ethyl; methanol, ethanol, isopropanol; propylene glycol; glycerol; propargyl alcohol; 1.3 propylene glycol; xylitol; acetic acid; have acid; mercaptoacetic acid; vary Bitterness; adipic acid; trifluoroacetic acid; oxalic acid, the amino acid; o-amygdalin acid; DL-Acid; anhydrous piperazine; six non-piperazine, furfural, castor oil, ethylene Aldehyde; glutaraldehyde, multi-POM; isopropyl ether; anisole; tetrahydropyrrole; pure pyridine; 1.2 dichloroethane; methylene chloride, chloroform, carbon tetrachloride; hydrazine hydrate; Nonylphenol;-m-cresol; Se phenol; phenol; the tert-butyl phenol; Titanium Dioxide; iron; full Tangfen; Bisphenol A; azo two different nitrile; sodium azide; sodium carbonate ; Sodium chloride; iron oxide; cuprous chloride; thionyl chloride; D4; sodium bicarbonate; ammonia, potassium chloride; anhydrous sodium sulphite; ammonium persulfate; glycol Dingmi; B Glycol ether; calcium chloride; cyclohexanone; cyclohexane, methyl tertiary butyl ether, potassium carbonate, ferric chloride, potassium nitrate; Linsuansanna; zinc oxide; sodium nitrite; antimony oxide; Tartrate; OP-10; TX-10; tablets base; AES; sodium benzoate, sodium citrate; partial sodium silicate, sodium perborate, a sodium carbonate, sodium benzene; Asia sodium chlorate; Wuluo Care products; urea; hydrochloric acid, sulfuric acid, lactic acid; amino acid, hydrogen peroxide, ammonium bicarbonate

公司宗旨："平等互利，信誉至上，团结合作，友谊长久"乙二胺；二乙胺；三乙胺；二乙烯三胺；三乙烯二胺；三乙烯四胺；四乙烯五胺；五乙烯六胺；己内酰胺；二甲基甲酰胺；烯丙基胺；N，N二甲基苯胺；正丙胺；正丁胺；正辛胺；三聚氰胺；1，2丙二胺；一乙醇胺；二乙醇胺；三乙醇胺；碘化钾；氢氧化钾；高锰酸钾；甲苯；二甲苯；对氯甲苯；丙酮；丁酮；乙酰丙酮；醋酸乙酯；醋酸丁酯；Y-丁内酯；碳酸二甲酯；乙酰乙酸甲酯；三伏乙酰乙酸；三伏乙酰乙酸乙酯；甲醇；无水乙醇；异丙醇；丙二醇；丙三醇；丙炔醇；1.3丙二醇；木糖醇；冰醋酸；己醛酸；巯基乙酸；异辛酸；己二酸；三氟乙酸；乙二酸；对氨基苯乙酸；邻氯苦杏仁酸；DL-扁桃酸；无水哌嗪；六无哌嗪；糠醛；蓖麻油；乙二醛；戊二醛；多聚甲醛；异丙醚；苯甲醚；四氢吡咯；纯吡啶；1.2二氯乙烷；二氯甲烷；三氯甲烷；四氯化碳；水合肼；壬基酚；纯间甲酚；硒酚；苯酚；对叔丁基苯酚；钛白粉；铁粉；全糖粉；双酚A；偶氮二异丁腈；叠氮化钠；碳酸钠；氯化钠；三氧化二铁；氯化亚铜；氯化亚砜；D4；碳酸氢钠；氨水；氯化钾；无水亚硫酸钠；过硫酸铵；乙二醇丁醚；乙二醇乙醚；氯化钙；环己酮；环己烷；甲基叔丁基醚；碳酸钾；三氯化铁；硝酸钾；磷酸三钠；氧化锌；亚硝酸钠；氧化锑；酒石酸；OP-10；TX-10；粒碱；AES；苯甲酸钠；柠檬酸钠；偏硅酸钠；过硼酸钠；过碳酸钠；苯磺酸钠；亚氯酸钠；乌洛托品；尿素；盐酸；硫酸；乳酸；氨基磺酸；双氧水；碳酸氢铵

They are, 4 21-amidohydrocortisone Ba1～Ba4, 10 21-amidoprednisolone Bb1～Bb10, 4 21-amidomethylprednisolone Bc1～Bc4, 4 21-amidodexamethasone Bd1～Bd4, 1 21-amidobetamethasone Be1, 1 21-amidoRS Bf1, 1 21-amidocortisone Bg1, 1 21-amidoprednisone Bh1. The amido groups were acetamido, nicotinamido, hemesuccinamido, benzoylamido, methanesufonamido, or arylsufonylamido.

包括：4个21-酰胺基氢化可的松（Ba1～Ba4），10个21-酰胺基氢化泼尼松（Bb1～Bb10），4个21-酰胺基甲泼尼龙（Bc1～Bc4），4个21-酰胺基地塞米松（Bd1～Bd4），1个21-酰胺基倍它美松（Be1），1个21-酰胺基RS（Bf1），1个21-酰胺基可的松（Bg1），1个21-酰胺基强的松（Bh1）。21-酰胺基分别为乙酰胺基、烟酰胺基、单琥珀酰胺基、苯甲酰胺基、甲烷磺酰胺基或取代苯磺酰胺基等。

Mission:"equality and mutual benefit, reputation first, unity and cooperation and friendship between the long-term" supply products: ethylenediamine; diethylamide; triethylamine; Diethylenetriamine; three ethylene diamine; three ethylene amines 40; 40 Five ethylene amines; five ethylene amines 6; caprolactam; DMF; allyl amine; N, N dimethylaniline; propylamine; are butylamine; are TOA; 3 Poly Cyanamide; 1,2 c diamine; ethanolamine; diethanolamine, triethanolamine; potassium iodide, potassium hydroxide, potassium permanganate, toluene, xylene, toluene of chlorine ; Acetone, butanone; acetylacetone; ethyl acetate, butyl acetate; Y-butyrolactone; DMC; acetyl of methyl acetate; Sanfu acetyl acid; Sanfu acetyl B Ethyl; methanol, ethanol, isopropanol; propylene glycol; glycerol; propargyl alcohol; 1.3 propylene glycol; xylitol; acetic acid; have acid; mercaptoacetic acid; vary Bitterness; adipic acid; trifluoroacetic acid; oxalic acid, the amino acid; o-amygdalin acid; DL-Acid; anhydrous piperazine; six non-piperazine, furfural, castor oil, ethylene Aldehyde; glutaraldehyde, multi-POM; isopropyl ether; anisole; tetrahydropyrrole; pure pyridine; 1.2 dichloroethane; methylene chloride, chloroform, carbon tetrachloride; hydrazine hydrate; Nonylphenol;-m-cresol; Se phenol; phenol; the tert-butyl phenol; Titanium Dioxide; iron; full Tangfen; Bisphenol A; azo two different nitrile; sodium azide; sodium carbonate ; Sodium chloride; iron oxide; cuprous chloride; thionyl chloride; D4; sodium bicarbonate; ammonia, potassium chloride; anhydrous sodium sulphite; ammonium persulfate; glycol Dingmi; B Glycol ether; calcium chloride; cyclohexanone; cyclohexane, methyl tertiary butyl ether, potassium carbonate, ferric chloride, potassium nitrate; Linsuansanna; zinc oxide; sodium nitrite; antimony oxide; Tartrate; OP-10; TX-10; tablets base; AES; sodium benzoate, sodium citrate; partial sodium silicate, sodium perborate, a sodium carbonate, sodium benzene; Asia sodium chlorate; Wuluo Care products; urea; hydrochloric acid, sulfuric acid, lactic acid; amino acid, hydrogen peroxide, ammonium bicarbonate

公司宗旨：&平等互利，信誉至上，团结合作，友谊长久&乙二胺；二乙胺；三乙胺；二乙烯三胺；三乙烯二胺；三乙烯四胺；四乙烯五胺；五乙烯六胺；己内酰胺；二甲基甲酰胺；烯丙基胺；N，N二甲基苯胺；正丙胺；正丁胺；正辛胺；三聚氰胺；1，2丙二胺；一乙醇胺；二乙醇胺；三乙醇胺；碘化钾；氢氧化钾；高锰酸钾；甲苯；二甲苯；对氯甲苯；丙酮；丁酮；乙酰丙酮；醋酸乙酯；醋酸丁酯；Y-丁内酯；碳酸二甲酯；乙酰乙酸甲酯；三伏乙酰乙酸；三伏乙酰乙酸乙酯；甲醇；无水乙醇；异丙醇；丙二醇；丙三醇；丙炔醇；1.3丙二醇；木糖醇；冰醋酸；己醛酸；巯基乙酸；异辛酸；己二酸；三氟乙酸；乙二酸；对氨基苯乙酸；邻氯苦杏仁酸；DL-扁桃酸；无水哌嗪；六无哌嗪；糠醛；蓖麻油；乙二醛；戊二醛；多聚甲醛；异丙醚；苯甲醚；四氢吡咯；纯吡啶；1.2二氯乙烷；二氯甲烷；三氯甲烷；四氯化碳；水合肼；壬基酚；纯间甲酚；硒酚；苯酚；对叔丁基苯酚；钛白粉；铁粉；全糖粉；双酚A；偶氮二异丁腈；叠氮化钠；碳酸钠；氯化钠；三氧化二铁；氯化亚铜；氯化亚砜；D4；碳酸氢钠；氨水；氯化钾；无水亚硫酸钠；过硫酸铵；乙二醇丁醚；乙二醇乙醚；氯化钙；环己酮；环己烷；甲基叔丁基醚；碳酸钾；三氯化铁；硝酸钾；磷酸三钠；氧化锌；亚硝酸钠；氧化锑；酒石酸；OP-10；TX-10；粒碱；AES；苯甲酸钠；柠檬酸钠；偏硅酸钠；过硼酸钠；过碳酸钠；苯磺酸钠；亚氯酸钠；乌洛托品；尿素；盐酸；硫酸；乳酸；氨基磺酸；双氧水；碳酸氢铵

This work, concentrated on the asymmetric allylation of aldehydes controlled by different chiral auxiliaries prepared from rotational pure tartaric acid, can be divided into three parts.The first part aims to review the developments of chiral drugs and asymmetric synthesis, from which derived the present research topic backgrounds and works.Synthesis and applications of allylation from aldehydes are the second part of the thesis. By optimizing the reaction conditions, such as solvents, temperature, time and chiral auxiliaries like N,N\'-dibenzyl tartamide, N,N\'-p-dimethylphenyl tartamide, N,N\'-o-dimethylphenyl tartamide, N,N\'-o-dichlorophenyl tartamide, N,N\'-a-dinaphyl tartamide, N,N\'-dicyclohexyl tartamide and N,N\'-diphenyl tartamide, ideal experimenttal conditions are obtained according to HPLC monitoring, as well as the auxiliaries\' recoveries experiments. Starting from benzaldehyde and 3-bromopropaldehyde, N,N\'-dibenzyl tartamide is considered the best auxiliary in this reaction.

本文介绍了醛的不对称烯丙基化反应，以光学纯酒石酸为原料，研究了不同构型手性配体在醛的烯丙基化反应中的立体选择性，全文共分三部分十个章节：第一部分对当前手性药物和手性技术进行了概述，并由此展开了本文的研究背景和任务；第二部分为有机合成部分，对醛的不对称烯丙基化反应进行了深入探讨，以苯甲醛为原料对反应条件进行优化，在优化的反应条件下对制备的七种可回收手性酰胺配体(N-苄基酒石酸二酰胺、N-对甲苯基酒石酸二酰胺、N-邻甲苯基酒石酸二酰胺、N-邻氯苯基酒石酸二酰胺、N-a-萘基酒石酸二酰胺、N-环己基酒石酸二酰胺和N-苯基酒石酸二酰胺)进行筛选，优化配体回收实验条件，最终确定出N-苄基酒石酸二酰胺在苯甲醛的不对称烯丙基化反应中具有较大优越性，结晶回收的手性配体光学纯度保持不变。

Seven of them have not been reported.Their structures were confirmed by IR,~1HNMR,MS,and element analysis. 4.Meanwhile,the green methylation procedure of imides was developed by using dimethyl carbonate as methylation reagent.A series of imides,for example,phthalimide,3,4-dibromo-maleimide and succincide were used for substrates.The effects of DABCO(1,4-diazabicyclo [2.2.2]octane)and DBU(1,8-diazabicyclo[5.4.0]undec-7-ene)as a catalyst in this kind of reactions were investigated.2-Bromo-3-(1-methylindolyl-3-yl)-1-methyl-1H-pyrrole-2,5-dione was prepared by using dimethyl carbonate,which further expanded the use of dimethyl carbonate,as a green agent in organic synthesis.

在以硫酸二甲酯为甲基化试剂对3，4-二溴马来酰亚胺进行N-甲基化反应合成3，4-二溴-N-甲基马来酰亚胺的同时，以碳酸二甲酯为甲基化试剂，对3，4-二溴马来酰亚胺、邻苯二甲酰亚胺、琥珀酰亚胺等酰亚胺类化合物的N-甲基化反应进行了研究；考察了1，4-二氮杂双环[2.2.2]辛烷，1，8-二氮杂双环[5.4.0]十一碳-7-烯、碳酸钾和四丁基溴化铵等作为催化剂对碳酸二甲酯N-甲基化反应的反应时间和收率等的影响，并应用碳酸二甲酯为甲基化试剂，合成了N-甲基-3-溴-4-(1-甲基-吲哚-3)-马来酰亚胺。

The graft polymerization of acrylonitrile on Crosslinked polyvinyl alcohol microspheres CPVA microspheres was performed by using cerium ammonium sulfate as initiator, and grafted microspheres CPVA-g-PAN were prepared. Subsequently, the grafted PAN was converted into poly via amidoximation reaction with hydroxylamine hydrochloride as reagent, resulting in the functional microspheres CPVA-g-PAO. The chemical structure and physicochemistry characters were adequately characterized with infrared spectrum, scanning electron microscope and determining Zeta potential. The effects of main factors on the amidoximation transform reaction of the grafted PAN were researched with emphasis, and the adsorption property of the functional microspheres CPVA-g-PAO for some biomolecules was examined preliminarily with uric acid as a model biomolecule.

以硫酸铈铵为引发剂，实施了丙烯腈在交联聚乙烯醇微球表面的接枝聚合，制备了接枝微球CPVA-g-PAN，然后以盐酸羟胺为试剂，通过偕胺肟化转变，将接枝的PAN转变为聚偕胺肟，制得了接枝有聚偕胺肟的功能微球CPVA-g-PAO，采用红外光谱法、扫描电子显微镜及Zeta电位测定等法，对功能微球CPVA-g-PAO的化学结构及物理化学特性进行了表征，重点考察了各主要因素对接枝PAN的偕胺肟化转变反应的影响，也以脲酸为模型分子，初探了功能微球CPVA-g-PAO对生物分子的吸附性能。

Restoration of ODC expression in the HL60-ODC cells resulted in rescue of rottlerin-induced apoptosis of HL60 cells. Simultaneously, phosphothreonine-ODC of rottlerin-treated HL60-ODC cells was highly elevated comparing with HL60-pcDNA3 cells. Taken together, we suggested that rottlerin, a PKCd inhibitor, might decrease phosphothreonine-ODC to reduce both protein stability and enzyme activity of ornithine decarbooxylase and finally resulted in cell apoptosis.

为了侦测鸟胺酸去羧化是否能够负调节rottlerin所引发的细胞凋亡，我们将具有鸟胺酸去羧化cDNA载体稳定转染至HL60细胞内，此细胞称为HL60-ODC细胞，另转染载体的细胞称为HL60-pcDNA3细胞；实验发现HL60-ODC细胞中的鸟胺酸去羧化蛋白为HL60-pcDNA3细胞与HL60细胞表现之2.5倍，同时HL60-ODC细胞提升鸟胺酸去羧化蛋白表现，能够减少rottlerin造成之细胞凋亡现象，并且此蛋白在HL60-ODC细胞中酥胺酸磷酸化较HL60-pcDNA3细胞表现高。

Our data are showed that apoptosis parameters including DNA fragmentation, nuclear morphological change and sub-G1 fraction, appeared after 24 h by 5 μM rottlerin treatment. Furthermore, rottlerin caused a decrease in 72% of ODC protein expression and an increase in threonine, rather than serine and tyrosine dephosphorylation on ODC enzyme compared with the control after incubation for 10 h. To determine whether ODC could down-regulate rottlerin-induced apoptosis, HL60 cells were stably transfected with ODC cDNA. HL60-ODC cells exhibited a 2.5-fold increase in ODC protein compared with vector only (HL60-pcDNA3) or HL60 cells.

在我们筛选天然化合物实验中，发现rottlerin抑制鸟胺酸去羧化活性最具成效，之前的研究人员已知蛋白激Cd调节鸟胺酸去羧化的活性，因此在人类白血病HL60细胞处理rottlerin的实验中发现加入rottlerin二十四小时后，细胞进行计划性死亡，并可侦测到DNA片段、细胞核浓缩及sub-G1提增；而细胞处理药物十小时后与控制组细胞比较，观察到鸟胺酸去羧化的蛋白表现与活性下降50﹪以上；除此以外，测定鸟胺酸去羧化去磷酸化的情况，发现於酥胺酸位置有显著差异，而丝胺酸和酪胺酸位置并无差异。

In order to investigate whether the lysine 188 residue in the XRCC4 is chemically modified by the enzyme SIRT2 or not, I apply site-directed mutagenesis to alter this lysine to either arginine or glutamine, which mimicking the non-acetylating or fully acetylating of lysine residue.

为探讨具酵素功能之SIRT2是否对於XRCC4 188位置之离胺酸进行化学修饰作用，利用定位突变方式分别将该离胺酸置换成麸醯胺或精胺酸，试图模仿XRCC4离胺酸188乙醯化与去乙醯化，是否造成其对SIRT2之亲和力之改变。

Finally,ITC added with amino resin to prepare PSTU resin.The temperature、ratio and reaction time of aminition and esterification reactions were investigated.

分别考察了胺化、二异硫氰酸酯加成反应的反应温度、反应配比及反应时间等条件对树脂合成的影响，确定优化工艺条件。

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。