共查询到20条相似文献,搜索用时 171 毫秒
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本文概述了甲基磺酰氯的合成方法,作者对以硫脲为原料的合成工艺进行了深入的研究,改进后的合成工艺使产品产率提高了10%。 相似文献
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一种高效驱蚊剂的合成高明章(西江大学轻工化学系肇庆526061)关键词驱蚊剂DETA合成中图分类号O625.5为了驱避蚊虫,人们进行了多年的研究,合成了许多驱蚊剂,到1975年止,各国合成和试验过的化合物就有2500种以上[1]。其中N,N-二乙基间... 相似文献
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本文研究了环状膦酸酯的合成方法,通过三种方法合成了十五个具有各种烷基结构的六元和七元环膦酸酯,并对这十五个化合物质谱作了分析和归纳,得出了一些有助于鉴定这类膦酸酯的质谱特征。 相似文献
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抗癌药物紫杉醇的制备、抗癌机理和应用前景 总被引:6,自引:0,他引:6
紫杉醇具有显著的抗癌活性和独特的作用机理,现主要用于治疗晚期乳腺癌和卵巢癌等。紫杉醇分子结构复杂,具有特殊的三环[6+8+6]碳架和桥头双键以及众多的含氧取代基,其全合成引起国内外许多有机化学家的兴趣。本文简述紫杉醇的制备、抗癌机理和不良反应。 相似文献
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Takayuki Doi Shinichiro Fuse Shigeru Miyamoto Kazuoki Nakai Daisuke Sasuga Takashi Takahashi 《化学:亚洲杂志》2006,1(3):370-383
A 36‐step synthesis was carried out in automated synthesizers to provide a synthetic key intermediate of taxol. A key step involved a microwave‐assisted alkylation reaction to construct the ABC ring system from an AC precursor. Subsequent formation of the D ring afforded baccatin III, a well‐known precursor of taxol. 相似文献
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Targeting delivery of paclitaxel into tumor cells via somatostatin receptor endocytosis 总被引:5,自引:0,他引:5
BACKGROUND: The binding of somatostatin (SST) to endogenous G-protein-coupled receptors (SST receptors or SSTRs) is followed by internalization of SST, and, several reports have shown that a high density of SSTRs is present on most hormone-secreting tissue tumors. Facile synthesis of the long-acting SST analog, octreotide, has previously been described. Octreotide might be of practical value in developing tumor tracers and in serving as a carrier of cytotoxic antitumor drugs. RESULTS: Fluorescein-labeled octreotide was internalized into the cytosol of human breast MCF-7 carcinoma cells via binding to SSTRs. Octreotide-conjugated paclitaxel (taxol) was created by coupling taxol-succinate to the amino-terminal end of octreotide. This conjugate retains the biological activity of taxol in inducing formation of tubulin bundles, eventually causing apoptosis of MCF-7 cells. Cytotoxicity of octreotide-conjugated taxol is mainly mediated by SSTR, as shown by the observation that octreotide pretreatment can rescue the induced cell death. In comparison with free taxol, this conjugate shows much less toxicity in Chinese hamster ovary cells. CONCLUSIONS: Octreotide-conjugated taxol exerts the same antitumor effect of free taxol on stabilizing microtubule formation and inducing cell death. This conjugate triggers tumor cell apoptosis mediated by SSTRs and is exclusively toxic to SSTR-expressing cells. Octreotide-conjugated taxol is less toxic to low-SSTR-expressing cells compared with free taxol. Our results strongly indicated that octreotide-conjugated taxol demonstrates cell selectivity and may be used as a targeting agent for cancer therapy. 相似文献
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[reaction: see text] The highly stereoselective construction of the C3 stereogenic center of the taxol C-ring is described. The trans isomer at the C3-C8 position of the taxol C-ring, which is required for the total synthesis, as well as its diastereomeric cis isomer were successfully synthesized with highly diastereoselective S(N)2' reduction of the allylic phosphonium salts. 相似文献
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Formal Total Synthesis of (−)‐Taxol through Pd‐Catalyzed Eight‐Membered Carbocyclic Ring Formation
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Sho Hirai Masayuki Utsugi Mitsuhiro Iwamoto Prof. Dr. Masahisa Nakada 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(1):355-359
A formal total synthesis of (?)‐taxol by a convergent approach utilizing Pd‐catalyzed intramolecular alkenylation is described. Formation of the eight‐membered carbocyclic ring has been a problem in the convergent total synthesis of taxol but it was solved by the Pd‐catalyzed intramolecular alkenylation of a methyl ketone affording the cyclized product in excellent yield (97 %), indicating the high efficiency of the Pd‐catalyzed intramolecular alkenylation. Rearrangement of the epoxy benzyl ether through a 1,5‐hydride shift, generating the C3 stereogenic center and subsequently forming the C1–C2 benzylidene, was discovered and utilized in the preparation of a substrate for the Pd‐catalyzed reaction. 相似文献
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抗癌药物紫杉醇的全合成-Nicolaou法合合成紫杉醇的剖析 总被引:2,自引:0,他引:2
介绍和剖析了用Micolaou法全合成紫杉醇的方法,包括合成的战略和路线,关键反应和保护基的应用等。 相似文献
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Jagat C Borah 《Tetrahedron letters》2004,45(18):3689-3691
The synthesis of the C-13 side-chain of taxol has been achieved using Shibasaki's asymmetric Henry reaction catalyzed by an optically active rare earth lanthanum-(R)-binaphthol complex. 相似文献
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Claire Le ManachAurélie Baron Régis GuillotBoris Vauzeilles Jean-Marie Beau 《Tetrahedron letters》2011,52(13):1462-1465
A library of paclitaxel (taxol) mimics was obtained by a straightforward strategy involving rational design and an efficient synthesis of a simplified taxane core substitute, together with a click-chemistry combinatorial search for phenylisoserine side-chain surrogates. 相似文献
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Paterson I Florence GJ Gerlach K Scott JP 《Angewandte Chemie (International ed. in English)》2000,39(2):377-380
With a similar mechanism of action to taxol, the title compound 1 is a particularly promising candidate for development in cancer chemotherapy. This efficient synthesis, based on stereocontrolled aldol reactions, should help to overcome the scarce natural supply of 1 from the rare sponge source. 相似文献