共查询到19条相似文献,搜索用时 109 毫秒
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目的合成血管紧张素Ⅱ受体拮抗剂替米沙坦.方法以3-甲基-4-硝基苯甲酸为起始原料,经酯化、还原、丁酰化、硝化、还原、环合、水解得2-正丙基-4-甲基-6-羧基苯并咪唑,在多聚磷酸的作用下与N-甲基邻苯二胺缩合,生成的产物再与4′-溴甲基联苯-2-甲酸甲酯缩合、水解得替米沙坦.结果目标物收率从文献的20.9%提高到26.3%.结论与文献相比,该合成工艺具有原料易得、操作简便、收率较高、易于工业化生产等优点. 相似文献
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2''''-乙酰基-3-酮基-10,11-脱水-6-O-甲氧基红霉素的合成 总被引:1,自引:0,他引:1
目的:合成泰利霉素中间体2'-乙酰基-3-酮基-10,11-脱水-6-O-甲氧基红霉素.方法:以6-O-甲氧基红霉素为起始原料,经脱水、酸水解、乙酰化和氧化得到目标产物.结果:以6-O-甲氧基红霉素计,总收率79.9%.目标产物的光谱数据与文献报道一致.结论:该方法合成操作简单,反应条件温和. 相似文献
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东北红豆杉化学成分的分离与鉴定 总被引:1,自引:1,他引:0
目的对东北红豆杉(Taxus cuspidtaSibe.et Zucc.)的化学成分进行研究。方法采用硅胶柱色谱等方法进行分离纯化,根据理化性质和NMR波谱数据进行结构鉴定。结果分离得到8个化合物,分别鉴定为大黄素甲醚(physcion,1)、油酸甲酯(methyl oleate,2)、紫杉宁(taxinine,3)、5α-羟基-9α,10β,13α-三乙酰氧紫杉烷-4(20),11-二烯(5α-hydroxy-9α,10β,13α-triacetoxytaxa-4(20),11-diene,4)、云南紫杉宁C(taxuyunnanine C,5)、2-去乙酰氧-5α-羟基紫杉宁J(2-deacetoxydecin-namoyl taxinine J,6)、2-去乙酰氧紫杉宁J(2-deacetoxytaxinine J,7)、11-羟基-12-甲氧基松香烷-8,11,13-三烯-3,7-二酮(11-hydroxy-12-methoxyabieta-8,11,13-triene-3,7-dione,8)。结论化合物1、2为首次从红豆杉属植物中分离得到,化合物4、8为首次从该种植物中分离得到。 相似文献
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10-去乙酰基-7-表紫杉醇转化为紫杉醇的研究 总被引:1,自引:0,他引:1
目的将天然紫杉烷类物质10-去乙酰基-7-表紫杉醇高效地转化为抗癌药物紫杉醇.方法首先将10-去乙酰基-7-表紫杉醇中的2'-OH选择性保护、7-OH乙酰化、去保护3步一锅反应获得7-表紫杉醇,再在DBU的催化下差向异构化为紫杉醇.结果本方法以10-去乙酰基-7-表紫杉醇为起始原料,以40%的总收率制备得到紫杉醇.结论建立了一条将天然紫杉烷类物质以较高的化学选择性以及良好的收率转化为紫杉醇的途径. 相似文献
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目的合成加巴喷丁并进行工艺改进.方法以环己酮为原料,经环合、水解、缩合、氨解和Hoffman降解5步反应合成加巴喷丁.结果所得产物化学结构经红外光谱、核磁共振谱及质谱等确证,总收率为45%.结论改进的合成工艺简便、合理且可行. 相似文献
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东北红豆杉枝叶化学成分的研究 总被引:20,自引:0,他引:20
东北红豆杉(Taxus cuspidata SibeetZucc)枝叶乙醇提取物的二氯甲烷溶部分显示有较强的抗肿瘤活性,从这部分中已分离出十二个紫杉烷类二萜化合物,经理化常数测定和光谱解析证明其中十个为已知化合物taxinine(I),taxinineA(II),taxinineB(III),taxacin(V),taxagifine(VI),taxol(VII),cephalomannine(VIII),taxinineM(IX),10-deacetyl baccatinIII(X)和taxayuntin(XI),另二个化合物为新成分,分别命名为10-deacetyl taxinineB(IV)和taxacustin(XII),其中化合物VII,VIII,IX,X和XI均为首次从该植物枝叶中分离得到。 相似文献
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云南红豆杉抗肿瘤活性成分的研究 总被引:26,自引:0,他引:26
云南红豆杉(Taxus yunnanensis Cheng et L.K.Fu)树皮的乙醇提取物显示较强的抗肿瘤活性,从中分离得到8个紫杉烷类二萜及其生物碱。经光谱分析和化学反应鉴定7个已知物为taxinine E(1),taxinine J(2),1-acetoxy-5-deacetvl baccatin Ⅰ(4),baccatin Ⅲ(5),taxol(6),cephalomannine(7)和7-xylosyl-10-deacetyl taxol(8)。化合物3命名为云南红豆杉甲素(ymlnanxane),为一新的紫杉烷二萜化合物,其结构为taxa-4(20),11-diene-2α,5α,10β,14β-tetraol-2α,5α,10β-triacetate-14β-αmethyl-β-hydroxyl butyrate,并通过X-射线单晶衍射予以证实.经体外筛迭化合物3具有抗肿瘤活性。 相似文献
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In addition to taxol A (1), 10-deacetyltaxol A (2), 10-deacetyl-7-epi-taxol A (3), 10-deacetylbaccatin III (5), taxuspine Z, taxezopidine G, 5 alpha-cinnamoyloxy-9 alpha,10 beta,13 alpha-triacetoxytaxa-4(20)11-diene, taxinine J, and taxinine M, a new bicyclic taxoid named taxumairol M (4), has been isolated from the seeds of Taxus mairei. The structure of 4 was determined on the basis of spectral analysis. 相似文献
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Guerra AS Malta DJ Laranjeira LP Maia MB Colaço NC de Lima Mdo C Galdino SL Pitta Ida R Gonçalves-Silva T 《International immunopharmacology》2011,11(11):1816-1822
Non-steroidal anti-inflammatory drugs (NSAIDs) represent a group of approximately 50 different medicines that are widely prescribed for the management of inflammation and that exhibit variable anti-inflammatory, anti-pyretic and analgesic activities. Most NSAIDs also exhibit a shared set of adverse effects, particularly related to gastrointestinal complications; thus, the development of new drugs for the treatment of chronic inflammation and pain continues to be an issue of high interest. Hydantoin and indole derivatives are reported to possess various pharmacological effects, including anti-inflammatory and analgesic activities. Therefore, the aim of this study was to evaluate the potential anti-inflammatory and antinociceptive activities of hybrid molecules containing imidazole and indole nuclei. The anti-inflammatory activities of 5-(1H-Indol-3-yl-methylene)-2-thioxo-imidazolidin-4-one (LPSF/NN-56) and 3-(4-Bromo-benzyl)-5-(1H-indol-3-yl-methylene)-2thioxo-imidazolidin-4-one (LPSF/NN-52) were evaluated using air pouch and carrageenan-induced peritonitis models as well as an acetic acid-induced vascular permeability model followed by IL-1β and TNF-α quantification. To evaluate the antinociceptive activities of the compounds, acetic acid-induced nociception, formalin and hot plate tests were also performed. The anti-inflammatory activities of the compounds were evidenced by a reduction in both leukocyte migration and the release of TNF-α and IL-1β in air pouch and peritonitis models. Upon acetic acid-induced nociception, a decrease in the level of abdominal writhing in the groups treated with LPSF/NN-52 (52.1%) or LPSF/NN-56 (63.1%) was observed. However, in the hot plate test, none of the derivatives tested exhibited an inhibition of nociception. These results indicate that the compounds tested exhibited promising anti-inflammatory and antinociceptive activities that likely involved the modulation of the immune system. 相似文献
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曼地亚红豆杉针叶中紫杉烷二萜类化学成分 总被引:1,自引:0,他引:1
目的 研究栽培于我国辽宁本溪的曼地亚红豆杉(Taxus media ‘Hicksii’)针叶中紫杉烷二萜类化学成分。方法 采用大孔树脂、硅胶柱色谱、ODS柱色谱、凝胶柱色谱及MDS柱色谱等方法进行分离纯化,通过NMR分析鉴定化学结构。结果 从曼地亚红豆杉针叶的乙醇提取物中得到6个已知化合物,分别鉴定为10-去乙酰基-10 β-羟基丁酸酯基紫杉醇A(1)、紫杉宁B(,2)、5 α-桂皮酰基红豆杉素(3)、紫杉宁A(4)、5 α-去桂皮酰基紫杉欧吉酚(5)、10-去乙酰基巴卡亭(6)。结论 化合物1、2、3、5为首次从曼地亚红豆杉中分离得到。 相似文献
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目的设计合成一系列新型紫杉烷类化合物并进行逆转多药耐药肿瘤细胞耐药活性的筛选。方法以本所生物合成的紫杉烷,Sinenxan A为原料,合成了10个(I1~7, II1,2, III)新的紫杉烷类化合物,其结构经FABMS,2DNMR确证,并对多药耐药癌细胞进行了逆转耐药性的试验。结果9个(I2~7,II1,2,III)化合物对多药耐药的人口腔上皮癌细胞KB/V200,能够显著逆转其耐药性,增强抗癌药的活性,其中化合物I2, I3, I4逆转活性明显好于已知对照药Verapamil。结论紫杉烷类化合物作为多药耐药逆转剂有较好的逆转耐药活性,值得进一步研究。 相似文献
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Shi QW Oritani T Sugiyama T Murakami R Yamada T 《Journal of Asian natural products research》1999,2(1):71-79
A new taxoid and a taxinine analogue were isolated from the seeds of the Chinese yew, Taxus yunnanensis. The structures were established as 13 alpha-acetoxy-5 alpha-(3'-dimethylamino-3'-phenyl)-propionyloxy-11(15-->1)-abeotaxa- 4(20),11-diene-9 alpha, 10 beta-diol and 2 alpha-acetoxy-5 alpha-cinnamoyloxy-9 alpha, 10 beta-dihydroxy-taxa- 4(20),11-diene-13-one on the basis of 1D, 2D NMR, and MS spectral analysis. 相似文献
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栽培曼地亚红豆杉针叶化学成分的分离与鉴定 总被引:1,自引:1,他引:0
目的对栽培于我国辽宁本溪的曼地亚红豆杉(Taxus media)针叶的化学成分进行研究。方法采用大孔树脂、硅胶柱色谱、ODS柱色谱、凝胶柱色谱及MDS柱色谱等方法进行分离纯化,通过NMR数据分析鉴定化学结构。结果从曼地亚红豆杉针叶的乙醇提取物中分离得到8个化合物,分别鉴定为二萜类化合物:紫杉宁(taxinine,1)、东北红豆杉素(taxacin,2)、紫杉欧吉酚(taxa-gifine,3)、2-去乙酰氧基紫杉宁J(2-deacetoxytzxinine J,4)、东北红豆杉素I5-O-桂皮酰基三乙酸酯(5-O-cinnamoyltaxacin I triacetate,5);黄酮类化合物:芹菜素(apigenin,6)、银杏双黄酮(ginkget-in,7)、金松双黄酮(sciadopitysin,8)。结论化合物2、5、7、8为首次从栽培曼地亚红豆杉针叶中分离得到。 相似文献