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1.
目的:合成并筛选新的抗抑郁活性化合物。方法:以间氯苯丙酮、苯丙酮、6-甲氧基-2-丙酰萘为起始化合物,经溴化反应合成2-溴-3-氯苯丙酮,2-溴苯丙酮,6-甲氧基-2-(2-溴丙酰基)萘,然后分别与外消旋化合物3-苯基-2-氨基-1-丙醇反应得到目标化合物。参照Porsolt法小鼠强迫游泳药理实验模型对所合成的化合物进行了初步抗实验性抑郁活性研究。结果:合成了目标化合物,目标化合物结构经IR,~1HNMR,MS确证。口服剂量为50 mg·kg~(-1)化合物4a的小鼠组强迫游泳静止时间显著低于空白对照组(P<0.01)。结论:本合成方法反应时间短,溶剂无毒性,收率较理想。化合物4a显示良好的抗实验性抑郁活性,值得进一步研究。 相似文献
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盐酸安非他酮的合成研究 总被引:4,自引:0,他引:4
目的 合成抗抑郁药盐酸安非他酮。方法 采用氯化铜高选择性氯化3-氯苯丙酮得2-氯-(3-氯苯基)-1-丙酮,再经叔丁胺胺化、盐酸-异丙醇酸化成盐制得盐酸安非他酮。运用IR、^1H-NMR、^13C-NMR和MS进行结构鉴定。结果 合成的盐酸安非他酮总收率为76%(以3-氯苯丙酮计)。结论 本法氯代反应选择性高,操作简便,总收率较高。. 相似文献
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对甲氧基苯甲醛(3)和2-氨基乙醇进行还原胺化反应得2-(4-甲氧基苄胺基)乙醇(4),4和乙醛酸经成环反应得2-羟基-4-对甲氧基苄基吗啉-3-酮(5),5和三氟乙酐反应得6后与(R)-1-[3,5-二(三氟甲基)苯基]乙醇(7)缩合,再经结晶诱导不对称转化、格氏反应、氢化脱保护及成盐反应制得阿瑞吡坦关键中间体(2R,3S)-2-[(R)-1-[3,5-二(三氟甲基)苯基]乙氧基]-3-(4-氟苯基)吗啉盐酸盐,总收率约18%(以3计)。 相似文献
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溴化铜对芳基烷基酮的选择性溴化反应研究 总被引:16,自引:2,他引:16
研究溴化铜对苯丙酮、间-氯苯丙酮、6-甲氧基-2-丙酰基萘、6-甲氧基-2-乙酰基萘、对-甲氧基苯乙酮和苯乙酮等芳基烷基酮的α-溴化反应,在乙醇或乙酸乙酯-氯仿混合溶剂中,溴化铜对芳基丙酮(苯丙酮、间-氯苯丙酮和6-甲氧基-2-丙酰基萘)溴化,高收率、高选择性地得到α-溴化产物。芳基乙酮(6-甲氧基-2-乙酰基萘、对-甲氧基苯乙酮和苯乙酮)的溴化铜溴化,在乙醇中反应,选择性得到α-溴化产物。 相似文献
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3-氯-4-甲基苯胺经氯甲酸苄酯酰化、与(R)-正丁酸缩水甘油酯环合、甲磺酰化、叠氮化、叠氮还原成胺、氨基乙酰化、苄位溴化得(固-5-乙酰胺甲基-3-[(3-氯-4-溴甲基)苯基]-2-噁唑烷酮(Ⅷ),后者与胺类化合物进行取代反应生成(D-5-乙酰胺甲基-3-[(3-氯-4-取代胺甲基)苯基]-2-噁唑烷酮。35个新化合物的结构经^1HNMR、元素分析或MS确证,并测定了它们的体外抗菌活性,发现化合物113对金葡菌和表葡菌的活性与吗啉噁酮相当。11和113对肠球菌的活性优于诺氟沙星。 相似文献
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用苄氧羰基氨基乙酸在N-甲基吗啉的催化下与氯甲酸异丁酯反应后,无需分离直接与氨基丙二酸二乙酯盐酸盐反应得到(2-苄氧羰基氨基乙酰胺基)丙二酸二乙酯,经Pd/C催化氢解、环合后在二氯甲烷中与Me3OBF4反应制得α-取代丝氨酸的合成中间体3,6-二甲氧基-2,5-二氢吡嗪-2-羧酸乙酯,总收率35.1%. 相似文献
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Michael Addition with Acylamino Acid Esters II. – Preparation of 3-Aryl-2,4-bis(ethoxycarbonyl)-2-methyl-5-pyrrolidones Michael addition of DL-acetylalanineethyl ester with diethyl arylidenemalonate yields a mixture of the 3-aryl-2,4-bis(ethoxycarbonyl)-2-methyl-5-pyrrolidones 3 and 4 . In contrast to analogous reactions this synthesis is not stereoselective. 相似文献
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V. L. Gein L. F. Gein M. V. Chirkova V. A. Mikhalev E. V. Voronina 《Pharmaceutical Chemistry Journal》2005,39(8):413-417
Reactions of 5-methyl-1-aryl-ethoxycarbonylpyrrolidine-2,3-diones (I, II, III, IV) with hydrazine hydrate, phenylhydrazine,
isoniazid, benzoylhydrazine, and thiosemicarbazide were used to synthesize a series of 3-hydrazones of 1-aryl-5-methyl-5-ethoxycarbonylpyrrolidine-2,3-diones
(V – VIII), 3-phenylhydrazones of 1-aryl-5-methyl-5-ethoxycarbonylpyrrolidine-2,3-diones (IX – XII), 3-isonicotinoylhydrazones
of 1-aryl-5-methyl-5-ethoxycarbonylpyrrolidine-2,3-diones (XIII – XV), 3-benzoylhydrazone of 5-methyl-1-phenyl-5-ethoxycarbonylpyrrolidine-2,3-dione
(XVI), and 3-thiosemicarbazone of 5-methyl-1-phenyl-5-ethoxycarbonylpyrrolidine-2,3-dione (XVII). All target products were
obtained with a yield of 51 – 90%. The reactions of 3-hydrazone of 1-phenyl-5-methyl-5-ethoxycarbonylpyrrolidine-2,3-dione
(V) with 5-aryl-2,3-dihydro-2,3-furandiones yielded 3-N-aroylpyruvoylhydrazones of 5-methyl-1-phenyl-5-ethoxycarbonylpyrrolidine-2,3-dione
(XVIII, XIX), and the heating of 3-hydrazone of 5-methyl-1-(4-chlorophenyl)-5-ethoxycarbonylpyrrolidine-2,3-dione (VI) with
4-methoxybenzaldehyde yielded 5-methyl-3-N-4-methoxybenzylidene-hydrazino-1-(4-chlorophenyl)-5-ethoxycarbonyl-3-pyrrolidin-2-one
(XX). The synthesized compounds are characterized by physicochemical constants and the parameters of IR and 1H NMR spectra. Some compounds were tested for antimicrobial activity.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 8, pp. 19 – 22, August, 2005. 相似文献
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目的制备新型离子液体催化剂,用于改进喹唑啉酮衍生物的合成工艺。方法以低成本开发新型离子液体,用于催化邻氨基苯甲酰胺与系列芳香醛缩合制备2-芳基-2,3-二氢喹唑啉-4(1H)-酮化合物。结果用一锅法合成了苯并噻唑六氟磷酸盐离子液体;使用该离子液体催化制备2-芳基-2,3-二氢喹唑啉-4(1H)-酮化合物的收率为77%~91%,产物易于分离且离子液体可循环使用5次以上。结论所开发的离子液体制备成本低、过程环保;以该离子液体为催化剂建立的2-芳基-2,3-二氢喹唑啉-4(1H)-酮化合物的合成方法简便易行。 相似文献
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Syntheses of 5-Aryl-2-cyclohexenones The 5-aryl-3-isopropyl-6,6-dimethyl-2-cyclohexenones 4a-f were synthesized by base-catalysed reactions of aromatic aldehydes with 3-methyl-2-butanone in ethanol/water at 70°C. Benzaldehyde and butanone react in the same way. Two of the four possible 5-aryl-2-cyclohexenones are formed in low yields and were isolated as their oximes. 相似文献
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目的研究3-芳基-2-甲基-1-吡咯并[1,2-a]吡嗪酮(2)类化合物抗炎镇痛作用的构效关系.方法通过吡咯-2-甲酸甲酯与α-溴代芳基乙酮的烃基化反应,制得1-(2-氧代-2-芳基)乙基吡咯-2-甲酸甲酯(4),4与甲胺反应经过环合直接生成目的化合物2;用小鼠测试了所合成化合物的抗炎镇痛活性.结果与结论合成了15个目标化合物;小鼠试验表明,一些所合成的化合物具有明显的抗炎和/或镇痛作用,其中化合物2o的作用活性与阳性对照药布洛芬相似. 相似文献
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Di Nunno L Vitale P Scilimati A Tacconelli S Patrignani P 《Journal of medicinal chemistry》2004,47(20):4881-4890
3,4-Diarylisoxazole analogues of valdecoxib [4-(5-methyl-3-phenylisoxazol-4-yl)-benzensulfonamide], a selective cyclooxygenase-2 (COX-2) inhibitor, were synthesized by 1,3-dipolar cycloaddition of arylnitrile oxides to the enolate ion of phenylacetone regioselectively prepared in situ with lithium diisopropylamide at 0 degrees C. The corresponding 3-aryl-5-methyl-4-phenylisoxazoles were easily generated by a dehydration/aromatization reaction under basic conditions of 3-aryl-5-hydroxy-5-methyl-4-phenyl-2-isoxazolines and further transformed into their benzenesulfonamide derivatives. The biochemical COX-1/COX-2 selectivity was evaluated in vitro by using the human whole blood assays of COX isozyme activity. Three compounds not bearing the sulfonamide group present in valdecoxib were selective COX-1 inhibitors. 相似文献
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Four novel series of pyrazolyl-4(3H)-quinazolinones have been prepared through the reaction of 3-aryl-2-hydrazino-4(3H)-quinazolinones with antipyrylazo-derivatives of ethyl acetoacetate, acetylacetone or diethyl malonate. These series of compounds are 3-aryl-2-[1-ethoxycarbonyl-1-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H - pyrazol-4-yl)hydrazono-2-propylidene]hydrazino-4(3H)-quinazo linones; 3-aryl-2-[4-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl) hydrazono-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]-4(3H)-quinaz olinones; 3-aryl-2-[4-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)azo -3,5- dimethyl-1H-pyrazol-1-yl]-4(3H)-quinazolinones and 3-aryl-2-[4-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl) hydrazono-3,5-dioxo-pyrazolidin-2-yl]-4(3H)-quinazolinones. The antiinflammatory activity of some representatives of the prepared compounds was studied. 相似文献
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以丙酰乙酸乙酯为起始原料,先溴化得到4-溴丙酰乙酸乙酯,再在甲苯中与苯甲酰胺回流环合得到2-(5-甲基-2-苯基-4-(口恶)唑)-乙酸乙酯,最后经氢化铝锂还原,得到目标杂环中间体2-(5-甲基-2-苯基-4-(口恶)唑)-乙醇.该合成方法反应步骤少,原料便宜,目标物的总收率为67.3%. 相似文献
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Nitration and Halogenation of Some 2-Aryl-4-chloro-methyl-oxazoles The nitration and bromination of the 2-aryl-4-chloro-methyl-oxazole is studied. The bromination in the position 5 of the oxazole ring is especially easy. The nitro group in the benzene ring is always introduced in ortho-position to the existing substituent. In the case of 2-phenyl-4-chloro-methyl-oxazole a mixture of 2 isomers is obtained: 2-(p-nitro)-and 2-(m-nitro)-phenyl-4-chloro-methyl-oxazole. 相似文献
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Benkli K Karaburun AC Gündoğdu-Karaburun N Demirayak S Güven K 《Archives of pharmacal research》2003,26(10):773-777
In this study, some new nitroimidazole derivatives were obtained from 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethylamine dihydrochloride (4) and 1-(2-bromoethyl)-2-methyl-5-nitroimidazole (5), which were prepared using metronidazole. Compound 4 was reacted with arylisothiocyanates (6) to obtain 1-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-3-arylthioureas (7) and the latter with alpha-bromoacetophenones (8) to give 3-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-2-arylimino-4-aryl-4-thiazolines (9). Also 1-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-2-phenyl-4-arylideneimidazolin-5-ones (11) were prepared by reaction of 4 with 2-phenyl-4-arylidene-5-oxazolones (10). The reaction of the other starting material 5 with 5-arylidenethiazolidin-2,4-dione (12) gave 3-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-5-arylidenethiazolidin-2,4-dione (13) derivatives. Structural elucidation of the compounds was performed by IR, 1H-NMR and MASS spectroscopic data and elemental analysis results. Antimicrobial activities of the compounds were examined and moderate activity was obtained. 相似文献