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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)。

The surface hydroxyl group onto magnetic polyvinyl acetate nanoparticles can be obtained by saponification reaction on their surface.

结果表明,磁性聚苯乙烯颗粒与丁二酸酐发生Freidel-Crafts酰基化反应,可以在颗粒表面引入少量羧基;磁性聚甲基丙烯酸甲酯颗粒分别与乙二醇、二缩三乙二醇、聚乙二醇等发生醇-酯交换反应,可以在颗粒表面接枝不同分子链长度的末端羟基;磁性聚醋酸乙烯酯颗粒经过醇解或皂化反应可以获得表面羟基;磁性聚丙烯酸甲酯颗粒通过乙二胺或1,6己二胺的胺解反应可以得到表面氨基,继而与一氯乙酸反应可以引入亚胺二乙酸基团。

Study on an efficient process for the preparation of trifloxystrobin starting from 2-methylacetophenone bypartial oxidation,esterification,reaction with methoxyamine,bromization and condensation with 3'- acetophenone oxime.

以邻甲基苯乙酮为原料,经过高锰酸钾的碱性氧化,甲醇酯化,再与甲氧基胺盐酸盐肟化后,用N-溴丁二酰亚胺溴化,最后和间三氟甲基苯乙酮肟缩合得到目标产物肟菌酯。

The results showed that the degree of butyryl substitution of CAB increased and the degree of acetyl substitution of CAB decreased as the activation time increased. The degree of substitution of CAB changed slightly after the esterification went along about 2h.

随着活化时间的增加,CAB的丁酯取代度会逐渐增大,乙酯取代度会逐渐减小;酯化反应2h后,CAB取代度变化不大;CAB的丁酯取代度随着反应体系中丁酰基摩尔分数的增加而增大,而乙酯取代度则随着丁酰基摩尔分数的增加而减小。

In order to find biologically active urea compounds,seven new N-[5-(3-pyridyl)-1,3,4-thiadiazol-2-yl]-N'- urea derivatives were synthesized by the reaction of 2-amino-5-(3-pyridyl)-1,3,4-thiadiazole with aroylazides,which were prepared starting from carboxylic acids,ethyl chloroformate and sodium azide by one-pot procedure.

为了寻找高生物活性的脲类化合物,通过2-氨基-5-(3-吡啶基)-1,3,4-噻二唑与酰基叠氮化物反应,设计合成了7个新的N-[5-(3-吡啶基)-1,3,4-噻二唑-2-基]-N'-取代苯基脲,其中芳酰基叠氮化物是以芳酸、氯甲酸乙酯、叠氮化钠为起始原料采用&一锅法&所制得。

The pegylated polylactide-poly glycolide nanoparticle, whose surface was co-modified withmaleimide-polyethylene glycol and methoxy-polyethylene glycol, was made by double-emulsion and solvent evaporation method andcovalently conjugated with thiolated lactoferrin via its maleimide functionalgroup.

第一章首先由复乳/溶媒蒸发法制备马来酰亚胺—聚乙二醇(Maleimide-PEG,MAL-PEG)和甲氧基聚乙二醇表面共修饰的聚乳酸-聚羟基乙酸纳米粒,然后通过其表面MAL-PEG与巯基化Lf共价连接而制备Lf-NP_。

Starting with commercial available tosylmethyl isocyanide and but-2-enoic methyl ester, pyrrolo[2,1-f][1,2,4]triazine derivatives was prepared by twelve-steps process in total yiled of 5.0%~8% via pyrrole and pyrrolo [2,1-f] [1,2,4] triazine ring formation, substitution and amination reactions etc.

本文以简单的对甲基苯磺酰甲基乙腈和反-2-丁烯酸为原料,经过形成吡咯,吡咯并[2,1-f][1,2,4] 三嗪环,取代,酰胺化等等12步反应,合成了结构新颖的吡咯并[2,1-f][1,2,4] 三嗪衍生物,总收率达5%~8%。

The results show that the zirconium sol has good spinnability when n: n= 1:3, reaction time is 6h and aging temperature is 15℃. The ZrO_2precursor fibers are made from hydrous zirconia chelated by acetylacetone. The sintercd fibers arecomposed of metastable tetragonal phase and sized about 15μm in diameter. Moreover, there aremany pores inside the fibers, but no cracks.4. ZrO_2/PVP hybrid fibers were prepared by blending the spinnable zirconium sol and 10 wt%PVP solution.

结果表明,当n(ZrOCl_2·8H_2O):n(H_2O_2)=1:3,反应时间6h,陈化温度15℃时可得纺丝性能良好的锆溶胶,ZrO_2前驱体连续纤维的组成主要为经乙酰丙酮配位的ZrO_2水合物,热处理后的ZrO_2纤维的相结构为亚稳四方相,纤维的直径为15μm左右,纤维中存在大量的纳米级气孔,但无明显裂纹。4。

The hydrophobic core serves as a reservoir for water-insoluble drugs.Hence,these nanoparticles can be used as carriers for hydrophobic drugs.For the synthesis of cholesterol-modified glycol chitosan conjugates,a carboxyl group was initially introduced to cholesterol molecule using succinic anhydride,and then covalently coupled with the primary amino group of glycol chitosan in the presence of 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride and N-hydroxyl succinimide.

本文采用二步反应将胆固醇接枝到乙二醇壳聚糖,首先将胆固醇进行羧基化,将胆固醇与琥珀酸酐反应生成胆固醇半琥珀酸酯,然后用1-乙基-3-(3-二甲基氨丙基)碳二亚胺盐酸盐与N-羟基琥珀酰亚胺作为偶联剂,将胆固醇半琥珀酸酯的羧基与乙二醇壳聚糖主链的氨基进行反应,得到胆固醇疏水改性乙二醇壳聚糖共聚物。

In this research, liposoluble chlorogenic laurate was synthesized by the acylation with lauroy chloride in the existence of alkali catalyst in non-water phase, and yellowish CGL powders with a yield of 81.24% were obtained under the optimal synthesis conditions determined via single-factor tests and orthogonal experiments, that is, carrying out the acylation at 35℃ for 8h with a n:n: n ratio of 1:1:1.5 and with dimethylformamide as the solvating agent and the thinner.

文中对绿原酸进行了改性,即在碱性催化剂催化的条件下使其与月桂酰氯进行非水相的酯化反应,得到了脂溶性的绿原酸月桂酸酯。经过单因素及正交试验,确定了最佳合成条件为:以N,N-二甲基甲酰胺作为溶解、稀释剂,绿原酸/月桂酰氯/三乙胺的摩尔比为1:1:1.5,温度控制在35℃,反应时间8h。

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