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甲基亚磺酸锌二水合物(2)与环氧乙烷经开环、氯代、取代及水解反应制得2-(氨基)乙基甲基砜盐酸盐(1),总收率50%。2或甲基亚磺酸钠与N-(2-溴乙基)邻苯二甲酰亚胺经取代和水解反应也可制得1,总收率68%或79%。 相似文献
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以邻氰基氯苄为原料,与苯甲醛或2-噻吩甲醛经Wittig-Horner反应、水解及氢化反应制得2-(2-苯乙基)苯甲酸或2-(2-噻吩基)乙基苯甲酸,总收率分别约64%和60%。 相似文献
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目的:改进1-[2-(N-甲基)氨基-2-(2,4-二氯苯基)乙基]-1H-1,2,4-三唑的合成方法,降低成本,提高收率,方法:以2-氯-1-(2,4-二氯苯基)乙酮为原料,经三唑烷基化与甲胺反应生成酮亚胺后还原(A法),或与N-甲基甲酰胺进行Leukart反应(B法),结果:A和B两种方法制得目标化合物的收率分别为57.6%和63.2%。结论:A和B两种方法原料易得,反应简便,降低了成本,提高了收率。 相似文献
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目的建立手性固定相HPLC法检查左舒必利起始原料(S)-N-乙基-2-氨甲基吡咯烷中右旋异构体。方法采用Chiralpak IA(250 mm×4.6 mm,5μm)为色谱柱,以正己烷-乙醇-乙醇胺(97.5:2.5:0.1)为流动相,流速1.0 m L·min-1,检测波长225 nm。结果实现了N-乙基-2-氨甲基吡咯烷左旋体与右旋体的基线分离,右旋体在4.82~48.19μg·m L-1内与峰面积线性关系良好。结论本方法适用于(S)-N-乙基-2-氨甲基吡咯烷的内在质量控制。 相似文献
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目的:改进罗格列酮的关键中间体4-[2-(N-甲基,N-(2-吡啶基)氨基)-乙氧基]苯甲醛的合成方法。方法:以2-[N-甲基,N-(2-吡啶基)氨基]乙醇为原料,分别与对氟苯甲醛发生威廉森成醚反应(以乙腈作溶剂,KOH作去酸剂)及与对羟基苯甲醛发生脱水缩合反应,合成目标化合物。结果:得到目标化合物,其结构经1HNMR和MS验证。结论:两种改进的合成方法操作简便,适于工业化生产。 相似文献
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新型氨基糖苷类抗生素合成的最新进展 总被引:1,自引:0,他引:1
氨基糖苷类抗生素是治疗感染性疾病的一类重要药物.但是,随着细菌对氨基糖苷类耐药性不断增加,大大限制了其临床疗效,从而激起了人们对细菌耐药机制的研究和开发新的氨基糖苷类抗生素的兴趣.本文主要对近年来新氨基糖苷类衍生物的设计及合成的研究进展进行综述. 相似文献
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Yan Cheng Jiang Fu Long Chen Lu-Lu Li 《Journal of Asian natural products research》2019,21(3):207-216
Two new diterpenoid glycosides, fructusnoids D (1) and E (2), and two new monoterpenoid glycosides (3, 4), together with three known diterpenoid glycosides (5-7) and three known monoterpenoid glycosides (8-10), were isolated from the fruits of Xanthium chinense. Their structures were elucidated by spectrometric analyses.
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Hong Huang Chun-Song Yang Li-Nan Zeng 《Journal of Asian natural products research》2013,15(3):289-298
We present in this paper the efficient synthesis of three macrocyclic lactone units which are core structures of natural resin glycosides by the use of a Keck macrolactonization approach. 相似文献
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Qiang Fu Mao-Ling Tan Hai-Mei Yuan Jiang Chen 《Journal of Asian natural products research》2017,19(1):22-27
The EtOH extract of the roots of Paeonia veitchii afforded two new monoterpene glycosides paeonidanin I (1) and paeonidanin J (2), and a new dimeric monoterpene glycoside paeonidanin K (3). Their structures were elucidated on the basis of spectroscopic means and hydrolysis products. 相似文献
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We present in this paper the efficient four-component one-pot synthesis of a fully protected hexaarabinogalactan 2 with di-branched structure by using d-thiogalactopyranoside 3,6-diol 3 as the central glycosylating agent. After global deprotection, 2 was converted into the 3-aminopropyl linker-containing free oligosaccharide 1 that is structurally related to ALR-5IIa-1-1, an arabino-3,6-galactan with intestinal immune system modulating activity. 相似文献
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Sui-Ku Liu Sheng Que Wei Cheng Qing-Ying Zhang Min Ye 《Journal of Asian natural products research》2013,15(12):1243-1248
Two new glycosides, syringic acid-4-O-β-l-arabinopyranoside (1) and kaempferol-3-O-α-l-rhamnopyranosyl-7-O-β-d-glucuronopyranoside (2), were isolated from whole plants of Carduus acanthoides (Asteraceae), and their structures were elucidated on the basis of spectroscopic analysis. 相似文献
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A new series of potential epidermal growth factor receptor inhibitors possessing bisquinazoline and saccharide moieties were designed and synthesized. The biological results demonstrated that the synthetic derivatives significantly inhibited epidermal growth factor receptor enzymatic activity in vitro. Of them, compound 14b showed the highest inhibitory rate toward epidermal growth factor receptor protein tyrosine kinase (81.36%) at a concentration of 1 μM. Further molecular simulation predicted that 14b offered its saccharide moieties hydrogen bonding to ATP-binding pocket. 相似文献
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A comparison of the O-glycosylation of resin-bound assembled peptides with the incorporation of glycosylated amino acids using established chemistry is presented. Fmoc/tert-butyl-based protecting groups were used for the peptidic moieties in conjunction with acetyl sugar protection. Koenigs-Knorr glycosylations were carried out using protected bromomannose derivatives, the acceptor being threonine or serine, either in solution or within a resin-bound peptide. The characterisation of microgram quantities of glycopeptides by the use of glycosidases in combination with mass spectrometry is also described. 相似文献
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Shi-Qiao Liu Li-Ping Kang Jie Zhang Yi-Xun Liu Yang Zhao 《Journal of Asian natural products research》2016,18(6):520-527
A new sesquiterpenoid glycoside, cryptomeridiol 11-O-β-d-xylopyranosyl-(1→6)-β-d- glucopyranoside (1), two new phenylpropanoid glycosides, 3,4-dihydroxy-allylbenzene 3-O-β-d-glucopyranosyl-4-O-β-d-apiofuranosyl-(1→6)-β-d-glucopyranoside (2), and 3,4,5-trihydroxy-allylbenzene 3-O-β-d-glucopyranosyl-4-O-β-d-glucopyranoside (3), along with four known phenylpropanoid glycosides (4–7), were isolated from the tuber of Ophiopogon japonicus. Compounds 4–7 were obtained from the genus Ophiopogon for the first time. Their structures were elucidated by spectroscopic methods, including 1D and 2D NMR and HR-ESI-MS. 相似文献
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Jin-Ming Chang Chien-Chang Shen Yu-Ling Huang 《Journal of Asian natural products research》2013,15(9):740-744
Two new glycosides, 1,6-di-O-syringoyl-β-d-glucopyranose (1) and quercetin 3-O-[(3-O-syringoyl-α-l-rhamnopyranosyl)-(1 → 6)-β-d-glucopyranoside] (2), along with seven known compounds were isolated from the MeOH extract of Leonurus japonicus. The structures of these compounds were elucidated by spectral analysis. 相似文献
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Hong-Bo Dong Ming Hou Wen-Bo Ma Jing-Xia Zhang Zhe-Yu Li Hong-Bing Luo 《Journal of Asian natural products research》2013,15(12):1154-1161
AbstractPhenylpropanoid glycoside compound 1, the natural anti-tumor compound isolated from the erial parts of Cirsium japonicum, was first totally synthesized using easily available materials in short, convenient route with overall yield of 13.9%. 相似文献