含丝氨酸和组氨酸残基手性肽核酸单体的合成

设计合成了含组氨酸残基碱基为胸腺嘧啶的手性肽核酸单体, 咪唑氨基的最终保护基为2,4-二硝基苯基(Dnp). 对文献合成方法进行了适当改进, 制备了两种含丝氨酸和组氨酸残基碱基为腺嘌呤的手性肽核酸单体, 以上化合物均可作为制备手性肽核酸的基本构建单元.     

含咪唑功能基的手性羧酸酯和脂肪醇的合成

含咪唑功能基的手性羧酸酯和脂肪醇的合成;天然氨基酸;手性咪唑羧酸酯;手性咪唑脂肪醇;合成     

肽核酸的合成、修饰和应用

肽核酸是寡核苷酸模拟物, 它的糖-磷酸骨架被N-(2-氨基乙基)甘氨酸骨架所代替. 为了优化肽核酸的性质, 各种结构的肽核酸(PNA)单体被合成出来. 综述了肽核酸的合成、结构修饰及应用.     

咪唑环合成方法的新进展

综述了咪唑环合成方法的新进展，讨论了部分合成方法的特点及反应机理。参考文献４１篇。     

β-羟基酸酯合成方法的研究进展

综述了近几年来合成β-羟基酸酯的方法,特别是手性β-羟基酸酯的不对称合成,并展望了该领域的研究前景。     

咪唑基手性硫醚衍生物的合成与表征

硫及氮、磷、氧等原子能够与大多数过渡金属络合形成多齿的螯合物.手性的硫醚钯络合物常用于不对称碳碳键的形成、不对称的Diels-Alder、Hetero-Diels-Alder环加成、Heck反应以及羰基的加成反应中,很多手性配合物都表现出良好的手性诱导效果.     

含1H-吡唑和咪唑的新型双杂环化合物的合成与生物活性

1-甲基-3-乙基4-取代-5-吡唑甲酰氯与含氮杂环反应,合成了8个新型结构的双杂环化合物。其结构经^1HNMR,IR,MS和元素分析表征。初步生物活性实验结果表明：在500μg．mL^-1,部分化合物对稻黑尾叶蝉的抑制活性达到53．57％。     

肽核酸骨架分子键联卟啉的合成及结构表征

以5,10,15-三苯基-20-(4-羧基苯基)卟啉和5,10,15-三苯基-20-(4-羟基苯基)卟啉为原料, 分别与N-(Boc-氨乙基)甘氨酸乙酯(3)及其衍生物4作用, 得到了两种肽核酸骨架分子键联卟啉化合物6和8. 中间体和目标化合物均由紫外-可见光谱、红外光谱、核磁共振光谱、质谱及元素分析所确证. 目标化合物的荧光光谱测试结果表明, 肽核酸单元分子的链接对卟啉分子的荧光波长和强度影响不大.     

手性咪唑酯类离子液体的合成及其物理性能

以咪唑,溴代烷烃及(-)-薄荷醇为原料合成了12个手性咪唑酯类离子液体,其结构经NMR和IR表征.物理性能研究结果表明,该类离子液体具有较好的热稳定性,且比旋光度存在一定的改变规律.     

Synthesis of New Chrial Building Blocks for Novel Peptide Nucleic Acids

N-Boc protected amino acids of analogues of peptide nucleic acid (PNA),which are a class of conformationally constrained building blocks based on 4-aminoproline backbone with chirality at 2-c and 4-c,have been synthesized.Those monomers can be used for the construction of novel peptide nucleic acid analogues.     

Synthesis of New Chiral Building Blocks for Novel Peptide Nucleic Acids

IntroductionAbouttenyearsago ,PNA ,astructuralmimicofDNAinwhichthesugar phosphatebackboneisreplacedbyN (2 aminoethyl)glycine (aeg)linkageemergedasapotentialanti sensetherapeuticagent.1PNAhassomeadvantages:(1)itisstabletocellularnucleasesandproteases,(2 )ithybridizeswithcomplementaryDNAorRNA (cDNA/RNA)sequenceswithhighaffinity ,(3)ithaslownon specificinteractionwithcellularcontentsand (4 )itiseasilysynthesizedbyadoptionofsolidphasepeptidesynthesischemistry .However,thema jorlimitationo…     

Design and Synthesis of Novel Peptide Nucleic Acid Monomers

All of the four nucleobases in DNA have replaced the 4‐hydroxy group of N‐[2‐(tert‐butoxycarbonylaminomethyl)‐trans‐4‐hydroxy] tetrahydropyrrole acetic acid methyl ester with cis ‐stereochemistry. An efficient route for the synthesis of N‐[2‐(tert‐butoxycarbonylaminomethyl)‐trans‐4‐hydroxy]‐tetrahydropyrrole acetic acid methyl ester has been developed. Starting with this intermediate, the protected monomers were synthesized by the Mitsunobu reaction or via its tosylate.     

Synthesis of Novel Chiral Thioether Ligands Containing Imidazole Rings Based on Natural Amino Acids

Using commercially available natural amino acids (L-Val, L-Leu, L-Phe) as chiral precursors, a series of N-substituted imidazole derivatives containing chiral groups was synthesized from the condensation reaction of amino acids, formaldehyde, glyoxal, and ammonia. Through esterification, reduction, chlorination, and subsequent substitution by thiols, chiral thioethers containing imidazole rings were synthesized, and the synthetic conditions were optimized. All the intermediates and the final products were characterized by NMR, ESI MS, HR MS, and IR.     

From Peptide Nucleic Acids to Supramolecular Structures of Nucleic Acid Derivatives

Nucleic acids play a pivotal role in life processes. The endeavours to shed light on the essential properties of these intriguing building blocks led us to the synthesis of different analogues and the investigation of their properties. First various peptide nucleic acid monomers and oligomers have been synthesized, using an Fmoc/acyl protecting group strategy, and their properties studied. The serendipitous discovery of a side reaction of coupling agents led us to the elaboration of a peptide sequencing method. The capricious behaviour of guanine derivatives spurred the determination of their substitution pattern using ¹³C, ¹⁵N NMR, and mass spectrometric methods. The properties of guanines initiated the logical transition to the study of supramolecular systems composed of purine analogues. Thus, xanthine and uracil derivatives have been obtained and their supramolecular self-assembly properties scrutinized in gas, solid, and liquid states and at solid-liquid interfaces.     

含有络合功能基的非天然氨基酸的设计、合成及在生物活性肽中的应用

设计合成了一类侧链带有络合基团的非天然氨基酸, 即侧链带有N,N-二羧甲基氨甲基、N,N-二酰胺甲基氨甲基和N,N-二羟乙基氨甲基的苯丙氨酸衍生物, 并将这类非天然氨基酸用于促性腺激素释放激素(LHRH)类似物的固相合成. 高效液相色谱分析结果表明, 粗肽的纯度较好, 易于纯化; 用电喷雾质谱测定了多肽的分子量. 这些非天然氨基酸可作为其它肽类药物合成的构建单元.