胺化产物

Then Doripenem came into the market in the July ,2005. We studied the synthesis of Doripemen.Firstly, we synthesized the chemical 2 from the starting material------o-hydroxylphenylacylamine through Reformastky reaction, alkylation, Diekmann reaction, enolization, esterification and etc. Secondly, we synthesized the chemical 3 from L — hydroxylproline through the protection of carboxyl, amidogen and hydroxyl group, reduction by NaBr, SN_2 substitution and Mitsumobu reaction.

我们以水杨酰胺为起始原料，经Reformatsky反应、烷基化、Diekmann环合、烯醇化、酯化等反应合成双环母核2；再从L-羟基脯氨酸出发，经酯化保护羧基、保护氨基、保护羟基、硼氢化还原酯得醇、Sn2取代和Mitsumobu反应等合成巯基侧链3；最后由化合物3经脱保护、水解得硫醇，和化合物2在二异丙基乙基胺的作用下缩合，最后Pd／C催化脱保护，历经16步反应最终得到产物多尼培南。

In another direction, the radical cyclization of thioimide with acylsilane produced simple cyclization product in low yield without expected enol silyl ether compound.

对於硫醯亚胺与矽基酮的自由基反应，则是得到低产率的简单环化产物，而不是预期的烯醇矽醚化合物。

The solvent type significantly affects the catalyst activity and selectivity for cyclohexanone oxime.

结果表明，溶剂的种类对硝基环己烷氢化产物的选择性有很大影响，乙二胺是该反应的合适溶剂。

To avoid the hydrolyzation of the expressed product by the cellular proteases and get more stable humanα-defensin it was attempted to express humanα-defensingenes in cyclic or amidation form.

为了避免表达产物水解，得到更稳定的人α-防御素，以环化形式和酰胺化形式表达人α-防御素基因。

Four different ionic liquids, BF4, BF and PF6 were investigated, arid PF6 showed the best effect when used as the reaction media, giving the highest yield in the shortest reaction time. Promoted by KF in PF6, N-aryl or N-alkyl monosubstituted sulfonamides could react with various activated halides and unactivated primary halides smoothly. Reactions were performed at 85℃ for 2~10 hours, and thirteen N-alkylation products were obtained with 70%~97% yields. Moreover, the ionic liquid recovered could be reused for three times with no appreciable decrease in yield and reaction rate.

结果表明，以PF6为反应介质时显示出了最好的效果，反应的时间最短，收率最高。N-芳基或N-烷基单取代的磺酰胺和各类不同结构的活化的卤代烃和未活化的一级卤代烃在PF6中KF作用下，85℃反应2~10h，以70%~97%的优良收率得到了13个N-烷基化产物，而且离子液体回收使用3次后效果未降低。

And through analyzing the stable configuration of photoactive compounds, the existence of triethylamine salt of diesterified product was thought to be the main factor that affects the solubility.

通过分析，确认二酯化产物三乙胺盐是影响感光剂溶解度的主要原因。

A new organic compound:N,N'-bis(1,10-phenanthroline-2-formacyl)-4,4'-diamino-diphenylmethane was synthesized via oxidation,esterification,substitution,hydrolysis, amidation of 1,10-phenanthroline as the starting material with chemical reagents (hydrogen peroxide,benzoyl chloride,potassium cyanide,sodium hydroxide solution,4,4'-diamino-diphenylmethane).

以邻菲啰啉为起始原料，与双氧水反应合成邻菲啰啉-N-氧化物，接着与苯甲酰氯、氰化钾、NaOH水溶液一一反应合成中间体邻菲啰啉-2-甲酸，再与4，4′-二氨基苯基甲烷进行酰胺化反应合成目标产物。

Nanocrystalline copper tellurides Cu〓Te〓 and Cu〓Te〓 have been successfully prepared in ethylenediamine and ethylenediamine with hydrazine hydrate system under high-intensity ultrasonic irradiation at room temperature respectively. Nanocrystalline silver tellurides Ag〓Te and Ag〓Te〓 have been successfully prepared in ethylenediamine and ethanol system under high-intensity ultrasonic irradiation at room temperature respectively.

在制备碲化铜时，在纯乙二胺体系超声辐射所制备的最终产物为Cu〓Te〓，而在加有水合肼的乙二胺中制得的产物为Cu〓Te〓；在制备碲化银时，在乙二胺体系制备的产物为Ag〓Te，而在乙醇体系制备的产物为Ag〓Te〓。

With the aid of 〓P NMR examination for the process and ESI-MS/MS analysis of the derivatized products from the reaction intermediate, it is found that the corresponding phosphoryl chloride is generated after mixing the hydrogen phosphonate derivative with chlorodiisopropylamine, and they react with amino acid, amino acid methyl ester, dipeptide methyl ester or N-methyl imidazole carboxyl alkyl diamine respectively to form the desired products.

利用〓P NMR对反应过程监测以及对反应中间体衍生化后产物的ESI-MS／MS检测分析发现，氢亚磷酸二酯与氯代二异丙胺反应首先生成了磷酰氯中间产物，它继续与氨基酸、氨基酸甲酯、二肽甲酯、1-甲基咪唑-2-酰基烷基二胺等反应生成了目标产物。

Treatment of pterin (2-amino-4-hydroxy-pteridine) derivatives with N,N-dimethylformamide dimethylacetal [1,(CH 3) 2NCH(OCH 3) 2] usually gave corresponding N 2-(N,N-dimethylaminomethylene)- pterin derivatives in polar solvents.

用N ，N 二甲基甲酰胺缩二甲醇 [(CH3 ) 2 NCH(OCH3 ) 2 ，1]和蝶呤(2 氨基 4 羟基蝶啶)衍生物在极性有机溶剂中反应一般得到脒化产物：N2 (N ，N 二甲基氨基亚甲基)-蝶呤衍生物。

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。