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Sonogashira coupling reaction of homopropargyl ether with aryl bromides and synthesis of 2,5-disubstituted 3-bromofurans

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Science China Chemistry 2009年第9期52卷 1314-1320页

作者： WANG Xin LIU LingYan CHANG WeiXing LI Jing State Key Laboratory and Research Institute of Elemento-organic Chemistry Nankai UniversityTianjin 300071China

This paper presents Sonogashira coupling reaction of aryl bromides with protected homopropargyl alcohols such as tert-butyldimethyl(1-phenylbut-3-ynyloxy)silane and tert-butyldimethyl(1-(2,4-dichlorophenyl)but-3-ynyloxy)silane in piperidine catalyzed by PdCl2/PPh3 without copper(I). The coupling products, disubstituted acetylene, are obtained in good or excellent yields. These products can be further used for the synthesis of 2,5-disubstituted 3-bromofurans.

关键词： Sonogashira protected homopropargyl alcohol 2 5-disubstituted 3-bromofurans

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Synthesis and <i>in Vitro</i>Biological Activities of 4,5-disubstituted 1,2,4-Triazole-3-Thiols

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Advances in Microbiology 2013年第4期3卷 366-375页

作者： Humaira Nadeem Muhammad Mohsin Hasan Afzaal Sadaf Riaz Ammar Zahid Syed Aun Muhammad Department of Pharmaceutics Riphah Institute of Pharmaceutical Sciences Riphah International University Islamabad Islamabad Pakistan

Purpose: The triazole nucleus is an important part of the therapeutically interesting drug candidate as antimicrobial, analgesic, anticancer, anticonvulsant and anti-inflammatory agents. Methods: Therefore, in this study, twelve 4,5-disubstituted-1,2,4-triazole-3-thiols were synthesized by the reaction of substituted isothiocyanates and hydrazides using the common method of base catalysed intramolecular dehydrative cyclization of substituted thiosemicarbazides 3(a-f) and 4(a-f). The structures of these compounds were characterized by means of FT-IR, 1H-NMR, and elemental analysis data. All these compounds were screened for antibacterial, antioxidant, antitumor and cytotoxic activities. Results: Among these compounds: 5c, 5f and 6f were found active against gram positive cocci, the compounds 5a, 5b, 5d, 6a and 6f showed 85% free radical scavenging effect at 3 ppm when tested for antioxidant activity, 75% tumors inhibition was recorded using 5c, 5d and 6a and brine shrimps lethality assay declared 5a, 5b and 6d was 129.62 μg/ml, 161.577 μg/ml and 81.56 μg/ml respectively. Conclusion: Compounds carrying significant bioactivity can be further studied using animal models to establish their safety profile prior to initiating clinical trials.

关键词： 4 5-disubstituted 1 2 4-Triazole-3-Thiols Antibacterial Antitumor Antioxidant Cytotoxic

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Facile Synthesis of Novel Chiral Bicyclic Thioureas and Their Crystal Structures

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International Journal of Organic Chemistry 2012年第1期2卷 15-20页

作者： Ping An Wang Hui Fang Nie Lin Jie Yan Sheng Yong Zhang Department of Medicinal Chemistry School of Pharmacy Fourth Military Medical University Xi’an China

The novel well-defined chiral bicyclic thioureas based on enantiopure unsymmetric cis-2,5-disustituted pyrrolidine skeleton were firstly synthesized and fully characterized by their 1H NMR, 13C NMR and HRMS. Their abs... 详细信息

关键词： Chiral Bicyclic Thiourea cis-2 5-disubstituted Pyrrolidine X-Ray Analysis

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