氨基化

Study on the Crystallization Process of Labeled GL-7-ACA Acylase CA130 Complex 7β-bromoacetyl amino cephalosporanic acid (BA-7-ACA), an analog of glutaryl-7-amino cephalosporanic acid (GL-7-ACA), can inhibit and specifically alkylate GL-7-ACA acylase (CA130) from Pseudomonas sp. 130, forming a carbon-carbon bond between BA-7-ACA and the C-2 on indole ring of Trp-β4 residue of CA130.Here we reported that BA-7-ACA labeled CA130 (BA-C130) could self-catalyze the hydrolysis of BA-7-ACA during crystallization process. The hydrolysis was confirmed to be a reaction analogous to the one of GL-7-ACA by comparative MALDI-TOF (matrix-assisted laser desorption/ionization-time of flight) spectrometry analysis.

二、GL-7-AcA酰化酶CA130标记复合物的结晶过程研究溴乙酰氨基头孢烷酸（7β-bromoacetyl amino cephalosporanic acid，BA-7-ACA）作为戊二酰-7-氨基头孢烷酸（GL-7-ACA）的类似物，不仅能够抑制GL-7-ACA酰化酶CA130的活力，而且能通过在BA-7-ACA和CA130的β亚基第四位色氨酸吲哚环二位碳原子之间形成碳-碳共价键而将CA130特异的烷基化。

The resultant was hydrogenised to remove protective group of amino group, then the product was reacted with NaNO2 to give diazonium salt, which was conjugated with salicylic acid, hydroxybenzene, N-salicyloyl glycine acid to get azo derivatives of 4-ASA.

本文首先对4-ASA的氨基和羟基进行了选择性保护，通过氢化还原法选择性脱除氨基的保护基，然后将氢化产物制成重氮盐，通过与水杨酸、苯酚和水杨酰甘氨酸发生反应生成4-ASA的偶氮衍生物，最后在碱性条件下水解得到最终产物。

Both the protection and deprotective group methods for the amino-group on side chain of a new N-pivot lariat crown ether were studied comparatively.

研究了一种新的氮支套素冠醚侧链上氨基的保护和脱保护基方法，结果表明，由过量乙二胺与对甲苯磺酰氯反应得到的单保护乙二胺（N－对甲苯磺酰基乙二胺4a），经N－烷基化环化反应，然后在氢化铝锂存在下脱除保护基，即可制得最佳产率的N－（2－氨基已基）单氮杂－12－冠－4（1）。

Goal compound synthesis namely: Take the vanillic acid as outset raw material, obtains 4- hydroxyl - 3- anisole methyl formate with the methyl alcohol reflux conditions, then after the etherification, the nitration, the return to original state, the ring closure response obtains 6- methoxy - 7- animal pen oxygen radical kui zuo lin - 4- alkone, then passes through the chlorination, the substitution aniline, to escape responses again and so on animal pen oxygen radical, etherification to obtain the goal compound; The goal compound and the diethylamine had the amine substitution reaction to obtain TM1, namely 4- benzene amino - 6- methoxy - 7- [2- hydroxyl - 3-(N, N- two ethyl aminos) third oxygen radical] kui zuo lin; Through zuo has the etherification with the Austria niter to respond obtains TM2, namely 4- benzene amino - 6- methoxy - 7- [2- hydroxyl - 3-(2- methyl - 5- nitryl imidazole) third oxygen radical] kui zuo lin.

目标化合物的合成即：以香草酸为起始原料，与甲醇回流条件下得到4-羟基-3-甲氧基苯甲酸甲酯，然后经过醚化、硝化、还原、环合反应得到6-甲氧基-7-苄氧基喹唑啉-4-酮，然后再经氯化、取代苯胺、脱苄氧基、醚化等反应得到目标化合物；目标化合物与二乙胺发生胺取代反应得到了TM1，即4-苯氨基-6-甲氧基-7-[2-羟基-3-丙氧基]喹唑啉；通过与奥硝唑发生醚化反应得到TM2，即4-苯氨基-6-甲氧基-7-[2-羟基-3-(2-甲基-5-硝基咪唑)丙氧基]喹唑啉。

Results show that, by using thionyl chloride and N,N-dimethyl formamide as chlorinating reagent and dichloromethane as solvent and taking -15℃ as reaction temperature, Z-iomer crystals with pale white color and stable to temperature can be obtained with an overall yield of 70%.

以2-（2-氨基噻唑－4-基）－2-甲氧亚氨基乙酸为原料，经盐酸化、氯代等反应合成了Z-2-（2-氨基噻唑－4-基）－2-甲氧亚氨基乙酰氯盐酸盐；氯代时以用亚硫酰氯和N，N-二甲基甲酰胺的混合物代替五氯化磷作氯化剂，并考察了温度和溶剂对氯代产物中Z-异构体和E-异构体收率的影响。

It was prepared from \%o\% nitroaniline and \%m\% aminophenol by diazotisation, coupling reaction and reduction, yield was 89%.

以邻硝基苯胺和间氨基酚为原料，经重氮化、偶合、还原制备了 2 (2 羟茎 4 氨基苯基)氢化苯并三唑，产率为 89%。

The copolycondensation type polyamic acid was synthesized by using 3,3', 4,4'-Benzophenonetetracarboxylic dianhydride as the dianhydride monomer, 4,4'-Diamino diphenylmethane and 4,4'-Oxydianiline as the diamine monomer under microwave irradiation in Dimethylformamide.

在微波辐射条件下，采用3，3'，4，4'-二苯酮四羧酸二酐、4，4'-二氨基二苯甲烷和4，4'-二氨基二苯醚为单体，N，N'-二甲基甲酰胺为溶剂，低温合成一种共缩聚聚酰亚胺的前驱体聚酰胺酸，化学亚胺化脱水环化生成BTDA型共缩聚聚酰亚胺。

Xinquan HuTwo new chiral backbones R-- and S--2-amino-2"-hydroxy-4,4",6,6"-tetra methyl-1,1"-biphenyl were synthesized via nitration, diazotation/iodination, Ulhnann coupling, selective reduction, diazotation/hydrolysis, hydrogenation and resolution from 2,4-dimethyl-aniline in seven steps.

以2，4-二甲基苯胺为起始原料，经过硝化反应、重氮化碘代反应、Ullmann缩合反应、选择性双硝基单还原反应、重氮化水解反应、催化氢化反应和拆分，首次合成了--2-氨基-2'-羟基-4，4'，6，6'-四甲基-1，1'-联苯和--2-氨基-2'-羟基-4，4'，6，6'-四甲基-1，1'-联苯两个对映体。

The yield reached 67.0% The medicinal and pesticidal activities of a part of the compounds have been measured .

在进行氨基酰化时，论文克服了该类嘧啶环上4位氨基在常规条件下不与芳香类和带有强吸电子基如三氯乙酰基酰化试剂发生反应的困难，通过采用在强碱性条件下进行酰化，得以成功。

Four hemicyanine derivatives,-N-(4-sulfobutyl)-4-[2-(4-N,N-dimethylamino-phenyl) etheny1] pyridinium (P1),-N-(4-sulfobutyl)-4-[2-(4-N,N-dimethylaminophenyl)-1,3-buteny1] pyridinium (P2),-N-(4-sulfobutyl)-4-2-(4-N,N-dimethylaminophenyl) ethenyll quinolinium (Q1) and-N-(4-sulfobutyl)-4-

合成了具有不同共轭链长度的吡啶盐类及喹啉盐类半菁染料-N-（4-磺酸丁基）-4-[2-4-N，N-二甲基氨基苯基）乙烯基]吡啶鎓盐(P1、-N-（4-磺酸丁基）-4-[2-4-N，N-二甲基氨基苯基）丁二烯基]吡啶鎓盐(P2、-N-（4-磺酸丁基）-4-[2-(4-N，N-二甲基氨基苯基)乙烯基]哇琳鎓盐(Q1)以及-N-（4-磺酸丁基）-4-[2-4-N，N-二甲基氨基苯基丁二烯基]喹啉鎓盐(Q2)。研究了它们的光物理性质，并将它们用作TiO2纳米晶电极的光敏化剂引入光电化学电池。

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。