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1.
Lansoprazole (Prevacid) is an antiulcerative drug used for the treatment of duodenal and gastric ulcers, reflux oesophagitis, and Zollinger–Ellison syndrome. During the bulk synthesis of lansoprazole, we have observed five impurities: lansoprazole N-oxide, lansoprazole sulfone N-oxide, lansoprazole sulfide, lansoprazole sulfone and N-aralkyl lansoprazole. The present work describes the synthesis and characterization of these impurities. 相似文献
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Ganta Madhusudhan Reddy V. V. N. K. V. Prasada Raju J. Moses Babu Ch. Praveen Mayur Khunt K. Mukkanti 《合成通讯》2013,43(11):1725-1736
Tenatoprazole (Ulsacare®) is a recently developed antiulcerative drug used for the treatment of both erosive and nonerosive gastroesophageal reflux disease. During the bulk synthesis of tenatoprazole, we have observed four impurities (tenatoprazole N‐oxide, tenatoprazole sulfone N‐oxide, N‐methyl tenatoprazole, and desmethoxy tenatoprazole) and two metabolites (tenatoprazole sulfide and tenatoprazole sulfone). The present work describes the synthesis and characterization of these impurities. 相似文献
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Synthesis and Characterization of Potential Impurities of the Antimigraine Drug,Rizatriptan Benzoate
P. Seetharama Sarma C. Nageswar Rao M. V. Surayanarayana Padi Pratap Reddy M. Khalilluah 《合成通讯》2013,43(4):603-612
Rizatriptan benzoate is a recently developed antimigraine drug used for the treatment of migraines and severe headaches. In the synthesis of rizatriptan benzoate in bulk,various impurities are formed. The present work details the development of a simple and novel process for the preparation of hydrazone impurity (6), rizatriptan N‐oxide (7), rizatriptan dimer (9), desmethyl rizatriptan (13), 5‐(1H‐1,2,4‐triazol‐1‐yl‐methyl)‐1H‐indole‐3‐ethanamine hydrochloride (14), N‐methyl rizatriptan oxalate (15), and impurities. 相似文献
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Nandu Baban Bhise Dhananjay Govind Sathe Tarur Radhakrishanan Raviraj Deore 《合成通讯》2013,43(9):1516-1526
Bicalutamide is an oral nonsteroidal, anti-androgen drug used for prostate cancer. It binds to the androgen receptor. During the bulk synthesis of bicalutamide, various impurities are formed. The present work details the development of simple processes for the preparation of impurities of bicalutamide, viz bical-sulfoxides (6), bical-deshydroxy (10), bical-desfluoro (10a), bical-2-fluoro (10b), and bical-3-fluoro (10c). 相似文献
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Rabeprazole sodium (Aciphex®) is a gastric proton pump inhibitor used for the prevention and treatment of gastric acid–related diseases. During the synthesis of bulk drug of rabeprazole sodium, we have observed metabolites rabeprazole sulfide and rabeprazole sulfone and related substances rabeprazole-N-oxide, rabeprazole sulfone-N-oxide, N-aralkyl rabeprazole, chloro rabeprazole, and methoxy rabeprazole as impurities in the drug substance. The present work describes the synthesis and characterization of these compounds. 相似文献
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以苯胺或对硝基苯胺为起始原料,通过重氮偶合法合成了4种分别含有硝基、氨基和不同数目偶氮基的偶氮苯化合物(1~4),其结构经1H NMR和FT-IR确证。研究了1~4在紫外灯(12 W)照射下随时间变化的UV-Vis谱图。结果表明:含有给电子基团(NH2)偶氮苯的光致异构化速率较含有吸电子基团(NO2)时更快,NO2对分子的异构化有一定抑制作用;分子中偶氮基的数目增加时,顺反异构化过程也受到影响。 相似文献
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建立了降压药阿雷地平新的合成路线, 并讨论了新合成方法的优化条件, 反应整体收率提高了20%; 结合阿雷地平的结构特点和合成工艺分析出6种杂质, 并提供了其制备方法和表征结果; 采用高效液相色谱(HPLC)法测定阿雷地平中的相关杂质, 为其质量标准的制定提供了实验依据. 相似文献
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Synthesis and Spectral Characterization of Related Substances of Lacidipine,an Antihypertensive Drug
V. V. N. K. V. Prasada Raju Ganta Madhusudhan Reddy Vedantham Ravindra Vijayavitthal T. Mathad P. K. Dubey 《合成通讯》2013,43(12):2137-2145
Five related substances (impurities) were detected in lacidipine bulk drug substance by a simple high-performance liquid chromatographic method (HPLC) and were identified by liquid chromatography–mass spectrometry (LC-MS). These related substances were independently synthesized, characterized, and co-injected with the sample containing impurities. 相似文献
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N. Senthilkumar Y. S. Somannavar Brajesh Kumar Sinha G. K. A. S. S. Narayan Ramesh Dandala 《合成通讯》2013,43(2):268-276
A simple synthetic route for active metabolites of carvedilol is reported. The metabolites 4′-hydroxycarvedilol and 5′-hydroxycarvedilol have exhibited high activity for β-blockade. We have disclosed syntheses of 4′-hydroxycarvedilol and 5′-hydroxycarvedilol from commercially available vanillin and isovanillin, respectively. 相似文献
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以没食子酸为原料。经烷基化、肼解得3,4,5-三甲氧基苯甲酰肼(2),2与芳香醛进行缩合反应合成了9个新的酰腙化合物。其结构经元素分析。IR,1H NMR和MS表征。 相似文献
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A simple, sensitive, and rapid reversed-phase high-performance liquid chromatographic method has been developed for determination of famotidine (FMT) and its impurities in pharmaceutical formulations. Separations were performed on a Supelcosil LC18 column with an isocratic mobile phase—13:87 (v/v) acetonitrile–0.1 M dihydrogen phosphate buffer containing 0.2% triethylamine (pH 3.0). The mobile phase flow rate was 1 mL min–1 and the detection wavelength was 265 nm. Response was linearly dependent on concentration between 1 and 80 g mL–1 (regression coefficient, R2, from 0.9981 to 0.9999). RSD from determination of method repeatability (intraday) and reproducibility (interday) were <2% (n=6). Lowest detectable concentrations ranged from 0.08 to 0.14 g mL–1. The proposed liquid chromatographic method can be satisfactorily used for routine quality control of famotidine in pharmaceutical formulations. 相似文献
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Vajrala Venkata Reddy Mandava Venkata Naga Brahmeswara Rao Ghanta Mahesh Reddy Khagga Mukkanti 《合成通讯》2013,43(23):3513-3523
Abstract Vardenafil hydrochloride trihydrate (Levitra) is used to treat erectile dysfunction (ED) and is an inhibitor of phosphodiesterase type 5 (PDE-5) enzyme. It maintains higher levels of cyclic guanosine monophosphate (cGMP), relaxes smooth muscles, promotes penile blood flow, and enhances erectile function. During the bulk drug synthesis of vardenafil hydrochloride trihydrate, six related substances (impurities), vardenafil dimer, vardenafil N-oxide, vardenafil glycene, vardenafil oxopiperazine, vardenafil oxoacetic acid, and phenyl vardenafil were identified, and these are reported herein for the first time. The present work describes the synthesis and characterization of these impurities. 相似文献
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Korrapati V. V. Prasada Rao Vijay K. Handa Inti V. Subramanyeswara Rao Ananta Rani Andra Naidu 《合成通讯》2013,43(17):2897-2905
New methods for the preparation of irbesartan 1 have been described. The dehydration and tetrazole formation in one step from substituted cyclopentane derivative 7 with tributyltin chloride and sodium azide is described. Selective hydrolysis of nitrile 3 with HCl has also been described in the preparation of N‐acylaminocyclopentane‐2‐carboxylic acid 4, which is the key intermediate for the preparation of irbesartan. The impurity profiling of irbesartan has also been discussed. 相似文献
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Zhanghua Gao Dr. Yingfa Li Dr. John P. Cooksey Dr. Thomas N. Snaddon Dr. Stefan Schunk Dr. Eddy M. E. Viseux Dr. Stephen M. McAteer Dr. Philip J. Kocienski Prof. Dr. 《Angewandte Chemie (International ed. in English)》2009,48(27):5022-5025
Caught in the middle : The ionomycin calcium complex (see structure; O red, Ca green) was the target of an approach featuring the efficient asymmetric synthesis of an allene by a copper(I)‐mediated anti‐selective SN2′ reaction, a highly stereoselective gold(III)‐catalyzed cycloisomerization of an α‐hydroxyallene, and a Rh‐catalyzed rearrangement of an α‐diazo‐β‐hydroxyketone.
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Synthesis,Spectroscopic Properties and Crystal Structural Characterization of a Triphenyltin(IV) Complex with 5-Bromonicotinic Acid 总被引:1,自引:0,他引:1
1 INTRODUCTION Organotin esters of carboxylic acids are widely used as biocides, fungicides and homogeneous ca- talysts in industry[1~3]. Recently, pharmaceutical pro- perties of organotin esters of carboxylic acids have been investigated for their antitumour activity[4, 5]. Studies on organotin compounds containing car- boxylate ligands with additional donor atoms (e.g. N, O or S) that are available for coordination to the tin atom have revealed that new structural types may lead to di… 相似文献
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褪黑激素的合成与表征 总被引:1,自引:0,他引:1
以吲哚为起始原料,经4步反应合成了褪黑激素(MLT) 吲哚(1)在甲醇中羟基化得到5-羟基吲哚(2),(2)同2-氯乙胺在乙酸乙酯中进行胺乙基化反应得到5-羟基色胺(3),(3)与硫酸二甲酯在甲苯中对羟基进行醚化,得到5-甲氧基色胺(4),(4)经乙酰化得到产物MLT,收率80% 相似文献