共查询到19条相似文献,搜索用时 218 毫秒
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制备3-O-去红霉糖红霉素衍生物的新途径 总被引:1,自引:0,他引:1
目的 开发一种合成酮基内酯和酰基内酯常用中间体3-O-去红霉糖衍生物的新方法。方法 红霉素9(E)-(O-烷基)-肟衍生物与对甲基苯磺酸一水合物在DMF中于室温下反应选择性水解红霉素得到相应的3-O-去红霉糖衍生物。结果 高收率得到3-O-去红霉糖衍生物并利用MS、^13C-NMR、^1H—NMB和IR确定了其结构。结论 该方法是制备3-O-去红霉糖红霉素衍生物的简捷、有效的新途径。 相似文献
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摘 要 目的: 采用超声-微波辐射法合成新的5-氯苯并三氮唑衍生物,并对其结构进行表征。方法: 以5 氯苯并三氮唑为起始原料,与氯乙腈合成中间体,再分别与6-氯烟醛和5-甲醛-2-甲氧基吡啶合成相应的目标产物。结果:合成得到6个新的5 氯苯并三氮唑衍生物,通过测定熔点、IR、LC-MS和1H-NMR确认其结构。结论: 用超声 微波辐射法合成得到6个5-氯苯并三氮唑衍生物。 相似文献
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微波及离子液体条件下香豆素类化合物的合成研究 总被引:1,自引:0,他引:1
目的:探索操作简便、环境友好的香豆素衍生物的合成方法:方法:以乙酰乙酸乙酯和苯酚类化合物为原料,通过Pechmann反应,在4种不同的反应条件(浓硫酸催化、Lewis酸三氯化铋催化、微波Lewis酸三氯化铋催化、微波离子液体催化)下催化合成多种香豆素衍生物,并对4种方法进行对比。结果:微波离子液体条件下的Pechmann反应与传统方法相比革除了有机溶剂的使用,缩短了反应时间且产率较高。结论:微波及离子液体条件下合成香豆素类化合物是一种条件简单、环境友好的合成方法。 相似文献
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克拉霉素(clarithromycin,CLM),化学名为克红霉索、甲红霉索、6—甲红霉素、6—甲氧基红霉素。商品名:克拉先、利迈仙。是半合成的红霉素衍生物(1),是由美国ABBTT公司研制成功。1991年11月美国FDA批准上市。已在美国、日本、英国、意大利、西班牙等20多个国家上市。利迈先是我 相似文献
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2H-1-苯并吡喃衍生物的合成及其体外抗癌活性的初步评价 总被引:1,自引:1,他引:0
目的设计并合成2H-1-苯并吡喃衍生物化合库并对其体外抗癌活性进行评价。方法以2'-羟基查耳酮为原料通过微波促进合成得到黄酮衍生物中间体,此中间体与POCl,反应得到4-氯-2H-色原烯-3-醛,通过微波辅助液相平行合成的方法,此醛与ROCONHNH2反应得到2H-1-苯并吡喃衍生物化合库。利用HL-60细胞系评价该化合物库的体外抗癌活性。结果与结论合成了含有32个化合物的2H-1-苯并吡喃衍生物库,体外活性评价表明。部分化合物对HL-60细胞的增殖有一定的抑制作用,其中。化合物9e在浓度为30μmol·L^-1的抑制率为70.8%。 相似文献
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Design,synthesis and biological evaluation of novel quinoline [4,3-b]chromene derivatives as AChE inhibitors through an efficient one-pot,four-component microwave-mediated reaction
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An efficient synthesis of chromeno[4,3-b]quinoline derivatives via one-pot, four-component reaction of 4-hydroxycoumarin, formaldehyde, cyclohexanedione, ammonium ceric nitrate under microwave irradiation was accomplished. The structures of these compounds were unambiguously confirmed by single crystal X-ray diffraction. Furthermore, the anti-AChE activities of these compounds in vitro were investigated at concentrations of 20 μM and 50 μM by using a standard Ellman’s method. The relationship of inhibitory activities and structures of these chromeno [4,3-b]quinolines was also systematically studied. Of all the compounds investigated, 4ag emerged as the most potent AChE inhibitor with IC50 values of 5.63 µM, and it might be used as potent lead for the development anti-AChE agents. Moreover, molecular modelling was conducted to understand the optimal interaction of AChE with these types of compounds. 相似文献
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目的探索环境友好、操作简便的monastrol合成方法。方法以间羟基苯甲醛、乙酰乙酸乙酯和硫脲为起始原料,在无溶剂微波加热条件下,用绿色室温离子液体1-丁基-3-甲基咪唑-L-樟脑磺酸盐催化Biginelli反应合成monastrol。结果 1-丁基-3-甲基咪唑-L-樟脑磺酸盐在无溶剂微波加热条件下可催化Biginelli反应合成monastrol,操作简单、耗时缩短、环境友好。结论以新型绿色室温离子液体1-丁基-3-甲基咪唑-L-樟脑磺酸盐为催化剂,经微波促进无溶剂Biginelli反应合成monastrol是一种操作简便、反应温和的绿色合成方法。 相似文献
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目的合成设计哌啶酮类法尼基转移酶抑制药,并对其抗肿瘤活性进行初步评价。方法以取代苯甲醛为起始原料,经Perkin反应和Michael加成,最后在微波辐射条件下环合得到目标化合物,并用MTT法测试它们抑制人Hela细胞和ANC-1细胞的IC50值。结果采用微波辐射技术合成哌啶酮类化合物,反应时间为20~45 min,产率为36.0%~67.1%。经1H-NMR、ESI-MS及IR对化合物的结构确证,总共合成11个新化合物。初步抗肿瘤活性测试结果显示11个目标化合物均有抑瘤活性,其中8个化合物IC50值低于氟尿嘧啶。结论哌啶酮类法尼基转移酶抑制药的合成路线可靠,具有显著抗肿瘤活性。 相似文献
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T. N. Mohammed Musthafa Zeba N. Siddiqui Fohad M. Husain Iqbal Ahmad 《Medicinal chemistry research》2011,20(9):1473-1481
A series of novel chromone derivatives have been synthesized employing 3-formylchromones and 5-acetyl-1,3-dimethylbarbituric acid as starting materials both under conventional heating method and microwave irradiation technique in good yields. The synthesized compounds were screened in vitro antibacterial activity against the representative panel of two Gram-positive bacteria and two Gram-negative bacteria. The synthesized compounds were also tested for their inhibitory action against three strains of fungus. The various compounds show potent inhibitory action against test organisms. 相似文献
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Synthesis and structure-activity relationships of new 9-N-alkyl derivatives of 9(S)-erythromycylamine 总被引:4,自引:0,他引:4
H A Kirst J A Wind J P Leeds K E Willard M Debono R Bonjouklian J M Greene K A Sullivan J W Paschal J B Deeter 《Journal of medicinal chemistry》1990,33(11):3086-3094
A series of new 9-N-alkyl derivatives of 9(S)-erythromycylamine has been synthesized by reductive alkylation of erythromycylamine with aliphatic aldehydes and sodium cyanoborohydride. Alternative syntheses employing hydrogenation methods have also been developed. These new 9-N-alkyl derivatives possess excellent antimicrobial activity in vitro and in vivo, especially when administered orally to treat experimental infections in mice. From structure-activity studies, 9-N-(1-propyl)erythromycylamine (LY281389) was selected as the most efficacious derivative. These methods have also been extended to the synthesis of some 9-N,N-dialkyl derivatives of erythromycylamine. 相似文献
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A green chemistry approach for organic synthesis is described here, which involves microwave exposure of reactants in presence or absence of solvents. A novel and simple method has been developed for the synthesis of some benzotriazole derivatives under microwave irradiation. In addition, these compounds were synthesised also by conventional heating procedures for comparison. All the compounds synthesised were characterised by melting point, TLC, IR and 1H NMR spectroscopy. Comparison between conventional and microwave-assisted synthesis was done by comparing total reaction time and percentage yield. The results suggest that microwave-assisted syntheses lead to higher yields within very short reaction times. On antifungal evaluation by cup plate method, all compounds showed antifungal activity. One compound showed activity similar to and two compounds showed better activity than standard antifungal drug flucanazole. 相似文献
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Bharat Parashar Abhilasha Jain Sudhir Bharadwaj V. K. Sharma 《Medicinal chemistry research》2012,21(8):1692-1699
Microwave synthesis technique opens new avenues for the synthesis of many compounds. A novel and simple method has been developed for the synthesis of 1-(2,4-dinitrophenyl) pyrazolidine-3,5-dione and 1-(2,4-dinitrophenyl)-3,5-dimethyl-1H-pyrazole derivatives under microwave irradiation. These compounds exhibit mild to moderate antimircrobial activity against different strains of bacteria (e.g. E. coli, P . aeruginosa, S. aureus and B subtilis) and fungi (e.g. C.?albicans and A. niger). All these synthesised compounds have been characterised by employing various techniques like TLC, Elemental analysis, IR, NMR and MS spectra. In addition to this, the yields of these compounds have been compared with the same compounds, obtained by conventional heating procedures. And the results show that by microwave irradiation method, the product yield is either high or may be same but it takes a very short period of time for reaction. Moreover, this technique provides ecofriendly or green chemical pathway for the synthesis of these compounds. Thus, the microwave irradiation method is more useful than the conventional method because of the shorter reaction time, better yield, conservation of energy and ecofriendly nature. 相似文献