A Stereospecific Synthesis and Unambiguous Assignment of the Absolute Configuration of(-)-erythro-Me

来源 :全国药物化学学术会议暨第四届中英药物化学学术会议 | 被引量 : 0次 | 上传用户:A121972311
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  A number of research groups have attempted to determine the absolute configuration of(+)-mefloquine hydrochloride since 1974.Very surprisingly,its absolute configuration is controversial for nearly 40 years:having the assignment of(+)-(11R,12S)six times and of(-)-(11R,12S)three times! We have synthesized stereospecifically(-)-erythro-mefloquine hydrochloride from commercial available(S)-(-)-1-Boc-2-piperidinecarboxylic acid in four steps without affecting the chiral center and unambiguously determined its absolute configuration as(11R,12S).
其他文献
mTOR(mammalian target of rapamycin),a serine/threonine kinase,plays a central role in cell growth,proliferation,metabolism and survival[1].Dysregulation of mTOR signal pathway is closely related with
Since the discovery of ERβ in 1996,much attention has been paid to studying its difference from ERα.In the following years,ERβ was comfirmed to associate with many diseases,such as cancer,cardiovascul
The epidermal growth factor receptor(EGFR,erbB1,HER1)has been well-validated as a molecular target in anticancer drug discovery.As part of our effort toward developing an effective therapeutic agent f
HSP90 既是细胞应激反应的生物标志物,也是细胞的内源性保护蛋白,发挥着分子伴侣的作用.HSP90 调控的客户蛋白有很多,包括EGFR、Met、Raf-1、IKK、p53 等,都与肿瘤的发生和发展关系密切.HSP90 可以通过其受体多环节多途径影响癌细胞生长和(或)存活,在肿瘤治疗领域展示出良好前景.基于分子片段的药物发现方法已经在药物研究中显示出巨大的潜力.片段分子具有相对分子质量小,结构多样
目的 研究新型二萜类化合物OP46 体外抑制细胞增殖并诱导人食管癌细胞EC9706 发生凋亡及与LKB1-AMPK-ROS 通路之间的关系.方法 分别使用OP46,OP46 联合NAC(ROS 清除剂),OP46 联合二甲双胍(AMPK 激活剂)处理细胞后,倒置光学显微镜进行细胞形态学观察,流式细胞术分析其对细胞凋亡的影响及细胞内 ROS 水平[1],荧光酶标仪检测细胞内还原型与氧化型谷胱甘肽的含
Iminosugars or azasugars,which exhibit effective inhibition against carbohydrate-processing enzymes,have attracted great interest for their potential clinical applications as anti-HIV,anti-diabetic,an
吡咯[1,2-f][1,2,4]三嗪类结构化合物在药物化学领域中表现出抗肿瘤、抗炎症活性,比如EGFR 酪氨酸激酶抑制剂BMS690514 、BMS599626 及IGFR1R 抑制剂 BMS754807 等都含有此类结构,因此对其合成研究正受到广泛地关注。含异喹啉类结构的化合物在天然产物及上市药物中也经常出现。我们课题组在前期研究工作的基础上,设计一类铜催化的偶联环化反应合成吡咯[1,2-f][
Podophyllotoxin(PPT)has cathartic,antiviral and antimitotic activity.1,2 As part of our ongoing efforts towards the development of new podophyllotoxin-based compounds with potent activities3,we synthe
会议
Lycogarubin C 是由Steglich 和 Akazawa 在1994 年分别独立的从粘细菌Lycogala epidendrum 中分离得到的海洋天然产物.Lycogarubin C 有一定的抗肿瘤活性,以其他取代的芳基代替Lycogarubin C 中的吲哚环,设计合成了一系列的Lycogarubin C 类似物.它们的合成以亚氨基二乙酸为起始原料,经过成酯、保护、环合、磺酰化、su
他汀类降血脂药物是一种3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂,可阻断HMG-CoA 转变为胆固醇前体甲羟戊酸,并反馈性激活肝脏低密度脂蛋白受体(LDLR),使肝脏胆固醇合成受阻,引起细胞内胆固醇减少,从而显著降低血清总胆固醇(TC)及低密度脂蛋白胆固醇浓度[1].现有的他汀类药物(如:洛伐他丁、辛伐他汀、氟伐他汀、阿托伐他汀、罗素伐他汀等)分子结构中都包含有(3R,5R)-二