Synthesis of Quinolone Analogues: 7-[(2S,4R)-2-Aminomethyl-4- hydroxypyrrolidin-1-yl] Quinolones

New quinolone derivatives of 7-[(2S, 4R)-2-aminomethyl-4-hydroxypyrrolidin-1-yl] quinolone-3-carboxylic acids were synthesized by condensation of 7-halo substituted quinolone- 3-carboxylic acids with (2S, 4R)-2-aminomethyl-4-hydroxypyrrolidine. These compounds were characterized by FAB-MS and 1H NMR.

The synthesis and activity in vitro of a series of 8-difluoromethoxy quinolones: Analogues of gemifloxacin

7-[4-（Aminomethyl）-3-（methoxyimino）pyrrolidin- 1-yl]- 1-cyclopropyl-6-fluoro-8-difluoromethoxy- 1,4-dihydro-4-oxoquino- line-3-carboxylic acid and its analogues have been prepared and evaluated for antibacterial activity in vitro.

Synthesis of Quinolone Analogues: 7-[2-Aminomethylaziridin-l-yl]-quinolones

New quinolone derivatives of 7-[2-aminomethylaziridin-l-yl]quinolone-3-carboxylic acids were synthesized. The structures of these compounds were characterized by IH NMR and HRESI-MS.

Design,synthesis and antitumor activity of 3-substituted quinolone derivatives (Ⅰ)

A series of quinolone derivatives containing benzimidazole, benzoxazole or benzothiazole ring were synthesized. The cytotoxicity of 12 new compounds was evaluated in KB, Be17402, A2780 and HT-29 cell lines. Most of synthesized compounds showed moderate inhibitory activity against cancer cells. The inhibitory activities of 6k, against KB and A2780 tumor ceils are comparable to that of topotecan, one of topoisomerase I inhibitors.

Synthesis and bioactivity of novel strobilurin derivatives containing the pyrrolidine-2,4-dione moiety

（E）-Methyl-2-（2-（bromomethyl）phenyl）-3-methoxyacrylate was reacted with substituted 1-acetylpyr-rolidine-2,4-diones and 3-（1-（hydroxylamino）ethylidene）pyrrolidine-2,4-diones respectively to synthesize two series of/%methoxyacrylate derivatives containing the pyrrolidine-2,4-dione moiety. The structures of the targeted compounds were confirmed by IR, 1H NMR, 13C NMR, MS and elemental analysis. The fungicidal activity against Rhizoctonia solani, Botrytis cinerea and Fusarium graminearum was evaluated. The bioassay results demonstrated that these compounds showed visible fungicidal activity.

Solid Phase Synthesis of 4(1H)Quinolones from Resin-Bound Cyclic Malonic Ester

The solid phase synthesis of 4 (1H) quinolones has been reported.

Synthesis of 6,8-dichloroquinolones utilizing new method and evaluation of their antibacterial activities

Several 6,8-dichloroquinolone analogues were synthesized from the key intermediate compound of 2,3,4,5-tetrachlorobenzene carbonyl chloride, which was obtained from the starting material of tetrachlorophthalic anhydride. Their in vitro antibacterial activities were evaluated. As a result of this study, compounds 21e and 21d were twofold more potent than ciprofloxacin （CPFX） and norfloxacin （NFLX） against Staphylococcus aureus-9, and with the same potent as CPFX and NFLX while against Escherichia coli-2, but were less potent than references in against Pseudomonas aeruginosa-17.

Synthesis and bioactivity of novel 3-(1-hydroxyethylidene)-5-substituted-pyrrolidine-2,4-dione derivatives

3-(1-hydroxyethylidene ) 的十新奇 5 代用品衍生物 pyrrolidine-2,4-dione 被综合。混合物被红外， 1H NMR， MS 和元素的分析证实。生物鉴定分别地显示这些混合物显示出显著 herbicidal 活动，并且混合物 6f 和 6j 对 Echinochloa crusgalli 的梗展出了优秀禁止的活动，与 94.4 和 72.7 mg/L 的 EC50 价值。

A Facile Synthesis of 4-Alkyl-2-Quinolones

The derivatives of 4-alkyl-2-quinolones possess a variety of biological activities. The general synthetic method of 4-alkyl-2-quinolones is the reaction of aryl amines with β-ketoesters to form β-ketoamides, which are then heated in concentrated sulfuric acid to complete the ring closure. Although a number of its 4-methyl and aryl derivatives have been obtained, other 4-alkyl-2-quinolones are rarely mentioned for lack of a convenient method to prepare the appropriate β-ketoesters used in condensation.

The Synthesis and Activity in vitro of a Series of 5-Amino-8-methoxyquinolones

A series of 1-cyclopropyl-5-amino-6-fluoro-8-methoxyquinoline-3-carboxylic acidshave been prepared and evaluated for antibacterial activity in vitro.

Synthesis of novel fullereneα-amino acid conjugates

Aspartic acid and glutamic acid with protected α-amino and α-carboxyl groups had been used to react with the activated hydroxyl group of N-substituted 3,4-fullero pyrrolidine. The products were deprotected, affording two monofuUerene α-amino acids, monofullerene aspartic acid （mFas） and monofullerene glutamic acid （mFgu）. Then a bifullerene glutamic acid conjugate （bFguC） was synthesized by reaction of mFgu containing protected amino group with N-substituted 3,4-fullero pyrrolidine.

Synthesis and Crystal Structure of Ethyl 3-(4-Chlorophenyl)-3,4-dihydro-6-methyl-4-oxo-2-(pyrrolidin-1-yl)furo[2,3-d]pyrimidine-5-carboxylate

The crystal structure of the title compound ethyl 3-（4-chlorophenyl）-3,4-dihydro-6- methyl-4-oxo-2-（pyrrolidin-1-yl）furo[2,3-d]pyrimidine-5-carboxylate （C20H20ClN3O4, Mr= 401.84） has been prepared and determined by single-crystal X-ray diffraction. The crystal is of monoclinic, space group P21/n with a = 20.6215（9）, b = 8.5311（4）, c = 21.6886（9） A^°, β = 91.607（1）°, V = 3814.0（3）A^°^3, Z = 8, Dc = 1.400 g/cm^3, F（000） = 1680, μ = 0.233 mm^-1, R = 0.0718 and wR = 0.1545 for 6717 observed reflections with I 〉 2σ（I）. X-ray diffraction analysis reveals two crystallographically independent molecules in the asymmetric unit.

Stereoselective synthesis of vic-halohydrins and an unusual Knoevenagel product from an organocatalyzed aldol reaction:A non-enamine mode

Stereoselective synthesis by an aldol reaction between chloroacetone and aldehyde was studied using a synthesized chiral organocatalyst and triethylamine. The reaction gave α-chloro-β-hydroxy ketones in excellent yield with high anti selectivity and enantioselectivity. The chiral organocatalyst was also used in the Knoevenagel reaction, which gave α-cyano-β-hydroxy ketones at a low temperature and the usual Knoevenagel product at a high temperature. Both products were obtained in good to moderate yield with good anti selectivity in the case of α-cyano-β-hydroxy ketone derivatives.

基于“烯丙基迁移”反应的创新性实验设计研究

结合科研成果及有机化学实验的教学经验,对有机化学实验中的“烯丙基迁移”实验进行研究。实验教学的实施过程中以设计合成的N-烯丙基-2-苯基-4-喹诺酮为底物原料,其在金属钯的催化下,烯丙基发生迁移反应,得到3-烯丙基-2-苯基-4-喹诺酮化合物。本实验结合新颖的科研内容,引入具有不同官能团的化合物进行案例对比,并进行反应机理的验证。不仅有利于学生更好的掌握烯丙基迁移的理论知识,且有利于激发学生对科学研究的兴趣,提高学生的综合素养能力。

3-(4-溴苯基)吡咯烷-2,5-二酮的合成

以4-溴苯乙腈和1,1-二(甲硫基)-2-硝基乙烯为原料,二甲基亚砜为溶剂,经过4步反应,获得3-(4-溴苯基)吡咯烷-2,5-二酮。反应时间为24、2、48、3.5 h时,收率分别为75.2%、76.8%、77.8%、78.5%,纯度分别为95.6%、96.6%、97.5%、97.8%(HPLC)。对终产物和标准样对比测定熔点、~1H NMR进行表征。

电化学合成在有机化学实验教学改革中的应用与实践——以2-苯基-4-喹诺酮的合成为例

有机化学实验是学生牢固掌握有机化学基本操作技术的关键训练环节。鉴于近年来电化学合成技术的在有机合成中的广泛应用,笔者将电化学有机合成的最新研究成果引入到有机实验教学中,以2-苯基-4-喹诺酮的合成为例,展示了电化学技术在有机合成中的应用。本实验无需额外添加氧化剂利用电化学氧化C(sp^(3))-H/C(sp^(3))-H键的氧化偶联,实现2-苯基-4-喹诺酮的绿色合成。本实验将薄层色谱、柱层析、核磁共振波谱融入与教学,有助于提高学生综合分析问题和解决问题的能力。

3-取代吡咯烷-2,4-二酮衍生物的合成

吡咯烷-2,4-二酮类衍生物存在于很多的天然产物中,具有很好的生物活性,引起了科学家的关注。本文以丙二酸单乙酯酰氯和不同的氨基酸乙酯盐酸盐为原料,通过狄克曼酯缩合反应和脱羧反应,得到了吡咯烷-2,4-二酮类化合物。最后与不同的芳香醛反应,合成了新型的3-取代吡咯烷-2,4-二酮类衍生物。

吡咯及二氢吡咯类化合物的合成研究进展

吡咯衍生物单体是一类重要的五元氮杂环化合物,用途非常广泛.根据母环氧化状态的不同,吡咯衍生物单体可分为吡咯、二氢吡咯以及四氢吡咯等三类化合物.综述了它们的合成方法及其合成研究进展情况.

氧氟沙星及其光学异构体的合成

以２，３，４，５－四氟苯甲酰乙酸乙酯为原料，与原甲酸三乙酯缩合后，和不同构型的２－氨基丙醇反应，再经环合，水解，与Ｎ－甲基哌嗪缩合分别制得氧氟沙星及其右旋体，总收率分别为４３．２％和３８．９％。