N-二异丙氧磷酰化氨基酸的合成

以亚磷酸二异丙酯为磷酰化试剂、次氯酸钠为氯代试剂首次对20种常见的α-氨基酸进行了磷酰化.通过添加适量四丁基溴化铵为相转移催化剂,使用过量的亚磷酸二异丙酯以补偿其在强碱环境中的水解,从而提高了反应产率.所得产物经核磁共振谱、红外光谱和质谱鉴定结构并分析总结了该类化合物的谱图特征规律.     

N-甲基吗啉的合成

N 甲基吗啉是一种杂环叔胺 ,具有醚和胺基的性质 ,广泛应用于杀虫剂、杀菌剂、植物生长调节剂等农药化合物的合成 ,也用于表面活性剂、润滑油冷却剂、金属防锈剂、纤维处理剂等精细化工产品的合成。N 甲基吗啉有 6种合成方法[1～ 3] ,其中以吗啉为原料的合成路线 ,原料来源方便 ,反应条件缓和 ,环境污染较小 ,对生产设备要求较低 ,易于工业化生产。前文[4] 曾报道以吗啉、多聚甲醛和次亚磷酸钠为原料合成N 甲基吗啉 ,文献 [5 ]以吗啉为原料 ,氢氧化钠水溶液为溶剂 ,一氯甲烷为烷基化试剂 ,合成了N 甲基吗啉 ,收率为 43 7%。本文根据正交实…     

硝基苯衍生物一锅法合成N-单烷基苯胺化合物

N-单烷基苯胺化合物是染料、医药的重要中间体.以取代硝基苯和醛为原料,钯碳为催化剂,甲酸铵为氢供体,经硝基还原、醛胺缩合、碳氮双键还原反应,在室温下一锅法合成N-单烷基化苯胺化合物,收率和转化率均超过80%.重点对反应配比、甲酸铵用量等工艺参数进行了考察,最佳反应参数为:n(硝基化合物)︰n(甲酸铵)=1︰4;w(硝基化合物)︰w(钯碳)=1︰0.10.并对苯环上取代基对反应的影响进行了探讨,结果显示,由于苯环上供电子基团有利于醛胺缩合物中间体的形成,故反应活性较高.该工艺具有反应温和、安全、操作简单等优点.     

高选择性N-单甲基化芳香胺的合成

本文报道了一种高效专一性合成N-单甲基芳胺的方法。芳胺先与醋酐反应生成乙酰胺,再与碘甲烷在氢化钠作用下反应生成相应的N-甲基乙酰芳胺。在乙二醇中用酸水解高产率得到相应的N-单甲基芳胺。并将该方法用于药物中间体的合成。     

一种含N-乙酰氨基葡萄糖三糖熊果酸皂苷的合成

本文采用汇聚式糖苷化策略以48.0%的总产率合成了一种含N-乙酰氨基葡萄糖三糖熊果酸皂苷ursolic acid 3-yl -L-arabinopyranosyl-(1→2)-α-L- arabinopyranosyl-(1→6)-2-acetamido-2-deoxy-β-D-glucopyranoside 1，其结构通过¹H NMR，¹³CNMR，二维核磁谱和质谱得到了确证。     

N-二茂铁甲基乙酰胺的合成及其晶体结构

标题化合物(C13H15FeNO)由二茂铁甲酰肟与乙酸乙酯经一锅煮方法制得,其结构通过元素分析,1HNMR,13CNMR,IR和单晶X-射线衍射法确定,化合物具有一维无限链状结构。其晶体属正交晶系,Pbca空间群,M r:257.11,a=9.6101(19),b=9.2313(18),c=25.869(5),v=2295.0(8)3,z=8,D c=1.488Mg.m-3,u=0.71073,F(000)=1072,最终偏离因子为R=0.0517,wR=0.0877。     

4—（N—烷基）胺甲基苯丙氨酸的合成

在生物活性肽研究中,通过在肽主链中引入特定结构的氨基酸,得到其活性类似物,可以使人们进一步认识肽结构与生物活性之间的关系,发展高活性、低副作用的肽类药物。蛋白氨基酸的结构都是一定的,不能满足研究工作的需要,所以需要设计合成特定结构的非蛋     

氨基酸合成方法研究 IV: 相转移催化下N-氰甲基亚氨酸酯的烷基化反应

研究了在固液相转移催化条件下, N-氰甲基苯甲亚氨酸酯的烷基化反应, 得到烷基化产物C-烷基化的亚氨酸酯, 烷基化产品不需进一步纯化就可水解得到α-氨基酸, 利用这一方法合成了十个α-氨基酸.     

N-苯基-α-氨基酸的微波合成及表征

以溴苯，α-氨基酸为原料，碘化亚铜为催化剂，DMF为溶剂，在碱性介质中微波辐射合成了目标化合物，并以颉氨酸与溴苯的偶联为模型反应进行条件优化，产物结构经IR，1H NMR表征。     

Excess enthalpies and apparent molar volumes of some N-methyl substituted amino acids in aqueous solutions

The excess enthalpies and limiting partial molar volumes at 25°C for aqueous solutions of N-methyl glycine, N-methyl alanine, and N-methyl serine are reported and compared with the same properties for the parent amino acids. For each N-methyl derivative the enthalpic contribution to the pairwise interaction is less favorable than that for the parent amino acid. The contribution of the N-methyl substituent to V ₂ ⁰ is similar for each amino acid, and is about 2 cm³-mol^–1 greater than for a methyl substituent on the -carbon. These observations have been rationalized in terms of the likely solute-solvent interactions. In addition a rigid particle model is used with the volume data to examine solute-solvent interactions.     

CuAlOx catalyst for the batch-flow tandem synthesis of amino acid-derived furfurylamines

Various amino acid-based furfurylamine derivatives were synthesized by two-stage procedure, which includes the condensation of 5-hydroxymethylfurfural (or furfural) with amino acid salts in methanol followed by hydrogenation of obtained imines in a flow reactor over CuAlO_x catalyst.     

A compilation of amino acid analyses of proteins

The amino acid analyses of 183 proteins, as residues per 1000 residues, are given. In addition the carbohydrate content and the content of any noncommon amino acids are also given. The sources of all proteins are presented.     

氨基酸自动分析仪快速分析方法的研究

本文研究了适用于日立L8900氨基酸自动分析仪(L8800同样适用)的国产化缓冲溶液和茚三酮反应液配方,研究出了适用于日立L8900氨基酸自动分析仪的快速分析程序方法。结果表明:本文所研究的国产化试剂能够完全达到原装进口试剂的效果,并且相比原装试剂拥有更好的适应性,便于在国内推广使用。快速分析程序方法相比原装程序方法分析时间缩短至43 min,减少20%,具有分析时间短、检测成本更短,工作效率更高的优点,同时也减少了有机试剂的排放,降低了对实验人员和环境的伤害。     

Nucleophilic cosubstitution of poly(dichlorophosphazene) with alkyl ether and amino acid ester

The nucleophilic substitution reaction of poly(dichlorophosphazene) with sodium 2‐methoxyethoxide and glycine ethyl ester has been studied in detail. Polymers prepared with different methods have been characterized by ¹H NMR, and the results reveal that the addition sequence of the two nucleophilic reagents is an important factor in determining the structure of the resultant polymer. If alkyl ether is added first, the subsequently introduced amino acid ester not only reacts with residual P? Cl but also attacks the alkyl ether side units present by replacing either the whole group or just ? OCH₃. As a result, a new kind of side group (? OCH₂CH₂NHCH₂COOC₂H₅) can be detected in the macromolecule. To obtain polymers with desired compositions {poly[(methoxyethoxy)_x(ethylglycino)_yphosphazene]}, the amino acid ester should be introduced initially to react with poly(dichlorophosphazene), and it should be followed by the alkyl ether. © 2005 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 43: 2417–2425, 2005     

A compilation of amino acid analyses of proteins

The amino acid analyses of 186 proteins are given as residues per 1000 residues. Additional information as carbohydrate composition, content of uncomon amino acids, and sources of all proteins are also presented.     

A genetically encoded metallocene containing amino acid

Redox active amino acids, cofactors, and metal ions are involved in a large number of catalytic, electron transfer, and regulatory processes in biology. Consequently, the ability to engineer redox active centers at defined sites in proteins would facilitate both the study and manipulation of a wide range of biological processes. Recently, we demonstrated that the redox active amino acid 3,4-dihydroxyphenylalanine could be efficiently and selectively incorporated into proteins in Escherichia coli using a nonsense codon and a corresponding orthogonal tRNA/aminoacyl-tRNA synthetase pair. We now report that ferrocene derivative 1 can be genetically encoded in Saccharomyces cerevisiae (S. cerevisiae) in good yield in response to the amber codon, TAG.     

氨基酸酯-烷基醚混合取代聚膦腈的合成与表征

聚膦腈高聚物,因其良好的生物相容性而用作生物医用材料。若在其侧链引入对热(如烷氧基醚)或对pH值敏感和可生物降解的基团(如氨基酸酯),则可得到具有环境敏感性和可生物降解性能的高聚物,这些高聚物可望作为药物载体,用于药物的控制释放。     

Synthesis and antitumour activity of arctigenin amino acid ester derivatives against H22 hepatocellular carcinoma

Arctigenin (ARG) is famous in its abundant pharmacological activity. However, many researches in it entered the bottleneck period because of its poor water solubility. The derivatives of ARG have been synthesised with five amino acids which have t-Butyloxy carbonyl (BOC) as a protective group. We examined the effects of removing BOC. The results showed that the amino acid derivatives without protective group have better water solubility and nitrite-clearing ability than ARG. Based on these results, ARG6′ and ARG9′ were selected at a dosage of 40 mg/kg to evaluate their antitumour activity. The percentage inhibition rate of ARG6′ and ARG9′ were 55.87 and 51.40, respectively, which was twice as much as ARG. Furthermore, they could increase liver and kidney indexes and produce less damage in these organs. In brief, this study provides a basis for new drug development.