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2-(4-硝基苯基)乙醇的制备 总被引:2,自引:0,他引:2
韦长梅 《中国医药工业杂志》2004,35(1):7-8
用2-苯乙醇为原料,经乙酸酯化、混酸硝化、碱性水解得到2-(4-硝基苯基)乙醇,考察了混酸和酯化物的最佳投料比以及反应温度,利用邻、对位终产物的不同熔点确定了最佳结晶温度,总收率79.8%,对位产物含量98.6%. 相似文献
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对羟基苯乙酮经硝化得到4-羟基-3-硝基苯乙酮,再在Na2CO3/KI作用下与氯苄进行O-烷基化反应后进行α-氯代得到4-苄氧基-3-硝基-α-氯代苯乙酮,总收率38%. 相似文献
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目的合成4-苄氧基-3-硝基-α-溴代苯乙酮,并进行工艺改进。方法以对羟基苯乙酮为原料,经过硝化、苄基化、溴代三步反应合成得到4-苄氧基-3-硝基-α-溴代苯乙酮,总收率达到45.2%。结果合成产物经熔点、红外光谱、核磁共振谱等分析确定结构正确;与文献报道一致。结论与其他文献方法比较,该法具有操作简单、收率高、污染小、成本低等特点,并可用于工业生产。 相似文献
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目的研究1-(4-溴苄基)-1-(4-溴苄氧基)脲(HY-D11)在大鼠体内药代动力学过程及其在大鼠肝脏中的代谢途径。方法建立HY-D11的UV-HPLC生物样本检测方法,灌胃给予HY-D11 66.7 mg·kg-1后,观察HY-D11在大鼠体内的药代动力学过程。研究CYP1A抑制剂(α-萘黄酮)、CYP2B抑制剂(舍曲林)、CYP2C抑制剂(槲皮素)、CYP2D抑制剂(育亨宾)、CYP2E抑制剂(双硫仑)及CYP3A抑制剂(醋竹桃霉素)对HY-D11在大鼠肝微粒体温孵液中代谢的影响。结果 HY-D11在大鼠体内的药代动力学过程符合二室模型。药代动力学参数t max为(3.67±0.52)h,C max为(1.61±0.13)mg·L-1,t1/2z为(3.41±3.91)h,平均滞留时间MRT0-∞为(7.05±0.29)h。HY-D11在大鼠微粒体温孵液中呈现明显的酶促动力学特征。醋竹桃霉素组与对照组相比,对HY-D11代谢有明显抑制作用(P<0.01);而与对照组相比,萘黄酮组、舍曲林组、槲皮素组、育亨宾组、双硫仑组对HY-D11的代谢均无抑制作用(P>0.05)。结论 HYD11在大鼠体内吸收、代谢速度较快,在大鼠体内代谢可能主要由CYP3A介导。 相似文献
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以对羟基苯乙酮为原料 ,经硝化和苄醚化合成了平喘药福莫特罗的重要中间体 4′ 苄氧基 3′ 硝基苯乙酮 ,反应总收率为 6 9% ,方法简单、可行 ,适于工业化生产。 相似文献
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N-(4-氯-3-三氟甲基苯基)-N'-(4-溴苯基)脲的合成 总被引:1,自引:0,他引:1
4-氯-3-三氟甲基苯胺和三光气在乙酸乙酯中反应制得4-氯-3-三氟甲基苯异氰酸酯,不经分离纯化,直接与对溴苯胺反应制得抗肿瘤药索拉非尼的中间体N-(4-氯-3-三氟甲基苯基)-N'-(4-溴苯基)脲,总收率约75%,纯度99.8%. 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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Mishra SK Sahoo S Panda PK Mishra SR Mohanta RK Ellaiah P Panda CS 《Acta poloniae pharmaceutica》2007,64(4):359-364
A series of 1-(2,4-dinitrophenyl)-3-(3-nitrophenyl)-5-(4-substituted phenyl)-2-pyrazolin-4-ones (4a-e) have been synthesized by the oxidation of 1-(2,4-dinitrophenyl)-3-(3-nitrophenyl)-5-(4-substituted phenyl)-4-bromo-2-pyrazolines (3a-e) with dimethylsulfoxide. The structure has been established on the basis of spectral data (IR,1H NMR). The synthesized compounds have been screened in vitro for their possible antimicrobial activity. 相似文献
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The determination of enantiomeric purity by Differential Scanning Calorimetry (DSC) was applied in the case of (1R,2R)-2-amino-1-(4-nitrophenyl)-1,3-propanediol. In the range of enantiomeric excess (greater than 95%), the direct and indirect methods gave identical results. 相似文献
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Davide Pitr 《Archiv der Pharmazie》1991,324(1):63-63
The conglomerate being more soluble than its enantiomers is the sole racemic modification that can be resolved in a direct way. Some classical cases requiring a single operation are known and they have been defined as the simultaneous and separate crystallization of enantiomers1). Much better known is the resolution of enantiomers by a sequence of alternate crystallization which takes place in the resolution by entrainment2) also appropriately called “seesaw method”3). (IR,2R)-2-Amino-1-(4-nitrophenyl)-1,3-propanediol. In an Erlenmeyer 250 ml flask with a reflux condenser 4.8 g (0.025 mol) of quinic acid and 10.6 g (0.05 mol) of (1RS,2RS)-2-amino-1-(4-nitrophenyl)-1,3-propanediol were dissolved in 110 ml of methanol by heating at reflux for a few min. The clear solution so obtained was left overnight at room tem. (20–24°C). 相似文献
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Hantzch’s type reaction of methyl acetopyruvate(2a), methyl 3-aminocrotonate(3) and 3-nitrobenzaldehyde(4) led to dimethyl 3-acetyl-6-methyl-4-(3′-nitrophenyl)-2,5-dicarboxylate(5a) and methyl 2,6-dimethyl-5-(1′, 2′-dioxo-2′-methoxyethyl)-4-(3′-nitrophenyl)-1,4-dihydropyridine-3-carboxylate(6a) in 26.7 and 9.2% yield, respectively. On the other hand, methyl 2,6-dimethyl-4-(3′-nitrophenyl)-1, 4-dihydropyridine 3-carboxylate(9) was acylated by ethyl oxaly chloride to give methyl 2,6-dimethyl-5-(1′,2′-dioxo-2′-ethoxyethyl)-4-(3′-nitrophenyl)-1,4-dihydropyridine-3-carboxylate(6b) in 76.8% yield. 相似文献
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M. Madesclaire S. Kh. Sharipova A. V. Lyamin A. A. Osipova E. A. Botkin Yu. V. Zaitseva V. P. Zaitsev 《Pharmaceutical Chemistry Journal》2012,45(11):668-670
A series of urea derivatives were synthesized from (1S,2S)-2-amino-1-(4-nitrophenyl)-1,3-propanediol and their antimicrobial activity was studied. The compounds synthesized here showed
the greatest levels of activity against strains of Bacillus cereus, Staphylococcus aureus, and Streptococcus haemolyticus. 相似文献
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Suárez-García Juana Cano-Herrera Ma-Angeles Ramírez-Villalva Alejandra Fuentes-Benites Aydeé Zavala-Segovia Nieves García-Eleno Marco A. Unnamatla M. V. Basavanag Cuevas-Yañez Erick 《Pharmaceutical Chemistry Journal》2021,55(5):436-440
Pharmaceutical Chemistry Journal - Aseries of 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivatives (Miconazole analogs) was obtained via copper catalyzed azide-alkyne cycloaddition as the key... 相似文献
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目的 优化(2R,4R)-4-甲基-2-哌啶甲酸乙酯的合成工艺.方法 以S-(-)-α-甲基苄胺为原料,与乙醛酸乙酯反应得到[(S)-1-苯乙基亚胺基]乙酸乙酯,与异戊二烯进行环合后,再经不对称氢化和脱保护反应制得(2R,4R)-4-甲基-2-哌啶甲酸乙酯.结果 总收率从17.0%提高至47.6%.结论 本工艺可有效地降低生产成本. 相似文献