万古霉素N4氨基的还原烷基化条件优化

目的 优化万古霉素N4氨基还原烷基化的反应条件。方法 以万古霉素为原料,筛选还原烷基化反应的溶剂、还原剂、醛用量和反应温度,用HPLC方法测定原料和产物含量。结果 确立了以甲醇/二甲基亚砜=1:1为溶剂、硼烷叔丁胺为还原剂、1.3倍醛用量、缩合温度65℃、还原温度为室温的最优反应条件。结论 利用本文优化后的条件可以有效合成万古霉素N4氨基还原烷基化产物,研究结果为其他糖肽类抗生素的半合成衍生化提供技术基础。     

利奈唑胺的合成

对利奈唑胺合成工艺进行优化。以吗啉和3,4-二氟硝基苯为原料,经取代、还原反应得到中间体5;（R）-环氧氯丙烷7、邻苯二甲酰亚胺钾盐6发生取代反应合成中间体9;最后中间体5和9经取代、环化、水解合成目标产物利奈唑胺,总收率36.5%（以3,4-二氟硝基苯计）。     

咪达那新合成工艺的改进

目的：对咪达那新的合成工艺进行改进。方法：以二苯乙腈为起始原料,经缩合1、缩合2及水解得到目标产物。结果：经三步合成了目标产物,总收率为68%,目标化合物结构经1HNMR和MS确证。结论：本合成方法原料易得,反应条件温和,适合工业化生产。     

卡莫司他衍生物的合成

目的 合成一种具有游离伯胺的卡莫司他衍生物.方法 以对羟基苯乙酸为原料,经4步反应得到目标化合物.结果与结论 成功制备了目标产物,所得产物的化学结构经1HNMR、MS确认.     

新型抗EV71病毒3C蛋白酶抑制药的设计、合成及其活性

摘 要 目的： 寻找抗EV71病毒新化合物。方法: 采用分子模拟技术,以EV71病毒3C蛋白酶活性口袋为靶,设计二肽、三肽,四肽,五肽和六肽等多个系列寡肽化合物,合成对接评分较高的寡肽化合物并进行抗EV71病毒活性筛选。结果: 五肽对接评分高于其他系列寡肽,显示五肽化合物与EV71 病毒3C蛋白酶有更强的键合力。研究中合成了两个评分较高的五肽化合物25和化合物16,体外抗EV71病毒活性实验显示化合物25活性较强（EC₅₀=1.36 μmol·L^-1,CC₅₀=211.94 μmol·L^-1, SI=155.84）,而化合物16则无明显活性。结论:五肽化合物25可作为抗EV71病毒新骨架开展进一步研究。     

A Competent and Commercially Viable Process for the Synthesis of the Anti-Hypertensive Drug Olmesartan Medoxomil

Drug product purity and potency are of most significance in the regulatory market as we notice many recalled batches worldwide, particularly in the US and Japan. Olmesartan Medoxomil is an anti-hypertensive drug. The present invention relates to a process for the preparation of Olmesartan Medoxomil with 99.9% purity in an overall 62% yield. The synthesis includes three isolations and one purification with easy plant operations. This process describes the formation and control of each individual impurity in all stages. This process for Olmesartan Medoxomil and its intermediates is competent for industrial production in very short reaction time intervals with an appreciable yield and high purity.     

Synthesis and Characterization of Impurities in the Production Process of Lopinavir

Lopinavir is an antiretroviral drug used for the inhibition of HIV protease. Four related substances of lopinavir were observed during the manufacturing process of lopinavir in the laboratory and they were identified. The present work describes the origin, synthesis, characterization, and control of these related substances.     

氟马西尼的有关物质B的合成(英文)

我们以7-甲氧基-4-甲基-3H-1,4-苯并二氮杂卓-2,5-(1H,4H)–二酮为原料,经脱甲基、苄基保护、环合和脱苄基反应合成了氟马西尼有关物质B。氟马西尼有关物质B结构经氢谱、碳谱和高分辨质谱确证,总收率为29.3%。该发现有助于合成工艺的优化和氟马西尼的质量控制。     

PF‐8380 and Closely Related Analogs: Synthesis and Structure–Activity Relationship towards Autotaxin Inhibition and Glioma Cell Viability

A series of PF‐8380 analogs, a recently developed autotaxin inhibitor, was explored. Inhibition of autotaxin by these analogs, as well as by all PF‐8380 synthetic intermediates, shows the importance of meta‐dichlorobenzyl and benzo[d]oxazol‐2(3H)‐one fragments. However, analogs 8 and 9 , bearing only the benzo[d]oxazol‐2(3H)‐one moiety, are more cytotoxic on the LN229 glioblastoma cell line than PF‐8380 and temozolomide (TMZ).