共查询到20条相似文献,搜索用时 125 毫秒
1.
2-氨基-4-甲基吡啶在过量浓盐酸/亚硝酸钠作用下与氯化亚铜/盐酸反应后,在偶氮二异丁腈(AIBN)作用下与硫酰氯反应制得2-氯-4-(氯甲基)吡啶,再在DMF中与哌啶缩合,得到拉呋替丁的关键中间体2-氯-4-(哌啶-1-基甲基)-吡啶,总收率约62%. 相似文献
2.
目的改进骨质疏松治疗药米诺膦酸的关键中间体2-(咪唑并[1,2-a]吡啶-3-基)乙酸的合成工艺。方法以反式-4-氧基-2-丁烯酸乙酯和2-氨基吡啶为起始原料,经环合、水解得到2-(咪唑并[1,2-a]吡啶-3-基)乙酸。结果与结论该合成方法首次以纯水替代有机溶剂作为反应溶剂,采用"一锅法"合成目标化合物,降低了该中间体的制备成本,而且环境友好,更适合于工业化生产。 相似文献
3.
4.
本文报告了以有机碱(吡啶)为催化剂合成γ-(4,5-二呋喃基-2-噁唑基)丁酸的合成程序及精制方法,并对影响产物合成的一些因素做了优化条件实验。 相似文献
5.
3,5-二硝基三氟甲苯(2)与氟化四甲铵进行氟代反应,所得单氟中间体再与4-甲基-1H-咪唑进行取代反应得到5-三氟甲基-3-(4-甲基-1H-咪唑-1-基)-硝基苯(3),然后在Pd/C催化下氢化还原制得抗肿瘤药尼罗替尼的中间体5-三氟甲基-3-(4-甲基-1H-眯唑-1-基)-苯胺(1),总收率约50%(以2计). 相似文献
6.
7.
8.
9.
以易得的4-咪唑甲醇(3)为起始物,经Ni~m三苯甲基保护的醛(5)与二膦酸酯(6)发生Wittig Horner反应,生成咪唑基氨基膦酸(7),用50%甲酸选择性地脱去三苯甲基保护得(8),以3%钠汞齐或Pd/C中压氢化、浓盐酸水解,最后得目的物组氨酸的膦等排物——α-氨基-β-(4-咪唑基)-乙基膦酸(9)(His-(P)]。 相似文献
10.
以3-吡啶甲醛为原料,与氰化钠、一氯化硫反应合成选择性M1受体激动剂占诺美林的关键中间体3-(3-氯-1,2,5-噻二唑-4-基)吡啶,目标化合物的结构经^1H-NMR谱确证。改进后的工艺操作简单,反应条件温和,收率由文献报道的40%提高到52%,更适合工业化生产。 相似文献
11.
右旋肌醇甲醚经缩酮制化得3-O-甲基-1,2:5,6-二-O-异亚丙基-D-肌醇,经甲磺酰化、水解、与4-苯基哌嗪缩合制得左羟丙哌嗪类似物4-(4-苯基哌嗪-1-基)-3-O-甲基-D-肌醇,总收率38%。镇咳药效实验表明,目标物对致咳小鼠的镇咳作用明显,但不及左羟丙哌嗪。 相似文献
12.
Raffa D Daidone G Plescia F Schillaci D Maggio B Torta L 《Il Farmaco; edizione pratica》2002,57(3):183-187
N-(1-Phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides 6, with a Benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 5 with potassium iodide for 1 h in order to study the role on the antifungal activity of the N-substitution with an aromatic heterocyclic system on benzamide moiety. Among the tested iododerivatives, compounds 6d,f,g,h possess interesting activities toward some phytopathogenic fungal strains. 相似文献
13.
Y. W. Kim Y. K. Kim J. Y. Lee K. T. Chang H. J. Lee D.-K. Kim 《Xenobiotica; the fate of foreign compounds in biological systems》2013,43(3):325-339
The authors investigated the pharmacokinetics and metabolism of 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide (IN-1130), a novel ALK5 inhibitor, which suppresses renal and hepatic fibrosis, and also exerts anti-metastatic effects on breast cancer-bearing MMTV-cNeu mice model. Plasma half-lives of orally administered IN-1130 were 62.6 min in mice, 76.6?±?10.6 min in dogs, 156.1?±?19.3 min in rats, and 159.9?±?59.9 min in monkeys. IN-1130 showed a high apparent permeability coefficient (Papp) of (45.0?±?2.3)?×?10?6 cm s?1 in in vitro permeability tests in a Caco-2 cell monolayer model. The bioavailability of orally administered IN-1130 was 84.9% in dogs and 34.4% in monkeys (oral dose, 5.5 mg kg?1), 11.4% in rats and 8.95% in mice (oral dose, 50.3 mg kg?1), respectively. Orally given IN-1130 was readily distributed into liver, kidneys and lungs. The major metabolite of IN-1130 (M1) was detected in the systemic circulation of rat and mouse and was purified and tentatively identified as 3-((4-(3-hydroxyquinoxaline-6-yl)-5-(6-methylpyridine-2-yl)-1H-imidazol-2-yl)methyl)benzamide or 3-((4-(2-hydroxyquinoxalin-6-yl)-5-(6-methylpyridine-2-yl)-1H-imidazol-2-yl)methyl)benzamide. The highest levels of M1 were found in liver. The results of this study suggest that IN-1130 has the potential to serve as an effective oral anti-fibrotic drug. 相似文献
14.
Raffa D Daidone G Maggio B Cascioferro S Plescia F Schillaci D 《Il Farmaco; edizione pratica》2004,59(6):451-455
3-(3-Methylisoxazol-5-yl) and 3-(pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones 8a-l and 9a,c-e,h-l were synthesized by refluxing in acetic acid the corresponding 2-methylquinazolinones 6 and 8 with the opportune benzoic aldehyde for 12 h. The synthesized styrylquinazolinones 8a-l and 9a,c-e,h-l were tested in vitro for their antileukemic activity against L-1210 (murine leukemia), K-562 (human chronic myelogenous leukemia) and HL-60 (human leukemia) cell lines showing in some cases good activity. 相似文献
15.
2,6,6-三甲基-1-环己烯-1-甲醛与(3-甲氧基-2-甲基烯丙基)膦酸二乙酯经Wittig-Homer缩合制得1-甲氧基-2-甲基-4-(2,6,6-三甲基-1-环己烯-1-基)-1,3-丁二烯,然后经酸催化水解得到维生素A的关键中间体2-甲基-4-(2,6,6-三甲基-1-环己烯-1-基)-2-丁烯醛,总收率约47%. 相似文献
16.
17.
7-(1-咪唑)-烷氧基黄酮衍生物的合成 总被引:6,自引:1,他引:5
黄酮类化合物和1-取代咪唑衍生物都具有较强的抑制血小板聚集活性,本文报道了由二溴代烷和咪唑及7-羟基黄酮衍生物合成8个新的7-(1-咪唑)烷氧基黄酮衍生物。 相似文献
18.
Seven new 2-(3-(4-aryl)-1-phenyl-1H-pyrazol-4-yl) chroman-4-ones (4a-4g) have been synthesized by cyclization of 2-hydroxychalcone analogues of pyrazole 3a-3g using conc. HCl in acetic acid. The structures of the compounds 4a-4g were established by the combined use of (1)HNMR, IR and mass spectra. All the seven compounds were tested in vitro for their antibacterial activity against two Gram positive bacteria namely Staphylococcus aureus and Bacillus subtilis and two Gram negative bacteria Escherichia coli and Pseudomonas aeruginosa. The compounds 4b, 4c, 4e, 4f, 4g have displayed good antibacterial activity when compared with commercially available antibiotic, ciprofloxacin. These compounds also were screened for their antifungal activity against two ear pathogenic fungi, namely Aspergillus Niger and A. flavus. The compounds 4a, 4c, 4d, 4g exhibited good antifungal activity when compared with commercially available antifungal, fluconazole. 相似文献
19.
目的 建立测定SD大鼠血浆中(E)-3-(4-((3,5,6-三甲基吡嗪-2-基)甲氧基)-3-甲氧基苯基)丙烯酸浓度的反相高效液相色谱(LC-UV)方法,并用于其在SD大鼠体内的药动学研究。方法 采用Diamonsil-C18(2)柱(100 mm×4.6 mm,5 μm),以乙腈:水(含5 mM的醋酸铵,用醋酸调节pH至4.0)=30:70为流动相,测定70只SD大鼠单剂量尾静脉给药15 mg/kg后不同时刻血浆中药物的浓度,并由此计算其在SD大鼠体内的药动学参数。结果 SD大鼠 相似文献
20.
以邻苯二胺为起始原料,经过缩合、氯代、烷基化和取代反应来合成4-[[1-[(4-氟苯基)甲基]-1H-2-苯并咪唑基]氨基]-1-哌啶甲酸乙酯。该合成方法操作简单,总收率达到30.7%。 相似文献