Various addition-elimination approaches have been explored for diastereoselective construction of 1-amino- 1-cyclopropane-carboxylic acid (ACPC) derivatives, and the desired product was obtained from a reaction of cyc...Various addition-elimination approaches have been explored for diastereoselective construction of 1-amino- 1-cyclopropane-carboxylic acid (ACPC) derivatives, and the desired product was obtained from a reaction of cyclo(NAc-L-Val-NAc-Gly) and methyl α-bro-moacrylate under protonic solvent.展开更多
The title compound 1-（3-amino-[1,2,4]triazol-1-yl）-3,3-dimethyl-butan-2-one（3） was synthesized by Hofmann-alkylation reaction of 1-chloro-3,3-dimethyl-butan-2-one（1） and ~1H-[1,2,4]triazol-3-ylamine（2） with eq...The title compound 1-（3-amino-[1,2,4]triazol-1-yl）-3,3-dimethyl-butan-2-one（3） was synthesized by Hofmann-alkylation reaction of 1-chloro-3,3-dimethyl-butan-2-one（1） and ~1H-[1,2,4]triazol-3-ylamine（2） with equal amount of K_2CO_3 as acid acceptor. The structure of compound 3 was characterized by ~1H NMR, 13 C NMR, HRMS and single-crystal X-ray diffraction. The compound crystallizes in the monoclinic system, space group P21/n with a = 5.7227（8）, b = 27.924（4）, c = 6.2282（7） ？, β = 101.892（11）°, V = 973.9（2） ？~3, Z = 4, T = 180.00（10） K, μ（MoKα） = 0.087 mm^（-1）, Dc = 1.243 g/cm^3, 3832 reflections measured（3.648≤θ≤26.022°）, 1916 unique reflections（Rint = 0.0359, Rsigma = 0.0572） used in all calculations. The final R = 0.0557（I 〉 2σ（I）） and w R = 0.1276（all data）. Bioassay showed that 3 displayed excellent activity as plant growth regulator with inducing lateral root formation and enhancing primary root elongation at 0.27 mmol/L（50 ppm） in soybeen（He Feng-50）. Good water solubility was found with 50 mg in 1 m L of water. Therefore, application of 3 in agriculture is more environmentally friendly due to cosolvent-free condition, and results in improved abiotic-stress tolerance by affecting the root growth. And furthermore, it can be used as a precursor to investigate the function of regulating plant root growth.展开更多
Two new alkaline earth metal coordination polymers constructed from the deriva-tive of 1,2,4-triazole are presented herein,namely,{[Sr（AmTAZAc）2（H2O）]}（1） and {[Ba（AmTAZAc）2（H2O）]}（2）（AmTAZAc = 3-amino-1H...Two new alkaline earth metal coordination polymers constructed from the deriva-tive of 1,2,4-triazole are presented herein,namely,{[Sr（AmTAZAc）2（H2O）]}（1） and {[Ba（AmTAZAc）2（H2O）]}（2）（AmTAZAc = 3-amino-1H-1,2,4-triazole-5-carboxylate）,which have been synthesized by using the layering method and structurally characterized by elemental analysis,IR,and single-crystal X-ray diffraction.Complexes 1 and 2 are isostructural,and both crystallize in the orthorhombic system,space group Fdd2.X-ray structural analysis shows that 1 or 2 has an intriguing 3-D infinite network of（318.438.510） topology based on a 2-D sheet structure of（4,4） net.The result shows that noncovalent interactions play an important role in strengthening the whole structures of the compounds.展开更多
The hydrochloride of 1-(1-amino-3-methyl)butyl borate pinacol is prepared by using the isobutylbromide to form the Grignard agent.The product is protected with the pinacol,then reacted with the lithium diisopropylamid...The hydrochloride of 1-(1-amino-3-methyl)butyl borate pinacol is prepared by using the isobutylbromide to form the Grignard agent.The product is protected with the pinacol,then reacted with the lithium diisopropylamide and the anhydrous zinc chloride.Finally,the product is synthesized in the existence of the LHMDS.All the compounds are confirmed by MS and 1H-NMR.展开更多
目的:研究自发性癫痫大鼠皮质、海马中谷氨酸转运体-1(GLT-1)、兴奋性氨基酸载体-1(EAAC-1)的转录、表达水平及其意义。方法:选取自发性癫痫Wistar大鼠(癫痫组)和正常Wistar大鼠(正常组)各10只,采用反转录-聚合酶链式反应(RT-PCR)技术检...目的:研究自发性癫痫大鼠皮质、海马中谷氨酸转运体-1(GLT-1)、兴奋性氨基酸载体-1(EAAC-1)的转录、表达水平及其意义。方法:选取自发性癫痫Wistar大鼠(癫痫组)和正常Wistar大鼠(正常组)各10只,采用反转录-聚合酶链式反应(RT-PCR)技术检测2组大鼠皮质、海马中GLT-1、EAAC1 m RNA转录水平,采用蛋白质印迹技术检测2组大鼠皮质、海马中GLT-1、EAAC-1蛋白的表达水平。结果:癫痫组大鼠皮质中EAAC-1 m RNA相对灰度值为(0.67±0.21),明显低于正常组大鼠的(1.54±0.38)(P<0.01);2组大鼠皮质中GLT-1 m RNA和海马中GLT-1 m RNA、EAAC-1 m RNA相对灰度值差异无统计学意义(P>0.05)。癫痫组大鼠皮质中EAAC-1、GLT-1蛋白表达水平的相对灰度值分别为(72.6±8.7)和(103.7±12.6),显著低于正常组大鼠的(116.5±15.1)和(139.5±14.2)(P<0.01);癫痫组大鼠海马中GLT-1蛋白表达水平的相对灰度值(196.7±23.5)明显的高于正常组大鼠的(145.5±19.7)(P<0.01);2组大鼠海马中EAAC-1蛋白表达水平的相对灰度值差异无统计学意义(P>0.05)。结论:自发性癫痫大鼠皮质中GLT-1、EAAC-1表达水平下调可能与癫痫发生有关。展开更多
文摘Various addition-elimination approaches have been explored for diastereoselective construction of 1-amino- 1-cyclopropane-carboxylic acid (ACPC) derivatives, and the desired product was obtained from a reaction of cyclo(NAc-L-Val-NAc-Gly) and methyl α-bro-moacrylate under protonic solvent.
基金supported by the National Natural Science Foundation of China(No.2012BAD20B04)
文摘The title compound 1-（3-amino-[1,2,4]triazol-1-yl）-3,3-dimethyl-butan-2-one（3） was synthesized by Hofmann-alkylation reaction of 1-chloro-3,3-dimethyl-butan-2-one（1） and ~1H-[1,2,4]triazol-3-ylamine（2） with equal amount of K_2CO_3 as acid acceptor. The structure of compound 3 was characterized by ~1H NMR, 13 C NMR, HRMS and single-crystal X-ray diffraction. The compound crystallizes in the monoclinic system, space group P21/n with a = 5.7227（8）, b = 27.924（4）, c = 6.2282（7） ？, β = 101.892（11）°, V = 973.9（2） ？~3, Z = 4, T = 180.00（10） K, μ（MoKα） = 0.087 mm^（-1）, Dc = 1.243 g/cm^3, 3832 reflections measured（3.648≤θ≤26.022°）, 1916 unique reflections（Rint = 0.0359, Rsigma = 0.0572） used in all calculations. The final R = 0.0557（I 〉 2σ（I）） and w R = 0.1276（all data）. Bioassay showed that 3 displayed excellent activity as plant growth regulator with inducing lateral root formation and enhancing primary root elongation at 0.27 mmol/L（50 ppm） in soybeen（He Feng-50）. Good water solubility was found with 50 mg in 1 m L of water. Therefore, application of 3 in agriculture is more environmentally friendly due to cosolvent-free condition, and results in improved abiotic-stress tolerance by affecting the root growth. And furthermore, it can be used as a precursor to investigate the function of regulating plant root growth.
基金Supported by the National Natural Science Foundation of China (Nos. 20771006 and 20901004)
文摘Two new alkaline earth metal coordination polymers constructed from the deriva-tive of 1,2,4-triazole are presented herein,namely,{[Sr（AmTAZAc）2（H2O）]}（1） and {[Ba（AmTAZAc）2（H2O）]}（2）（AmTAZAc = 3-amino-1H-1,2,4-triazole-5-carboxylate）,which have been synthesized by using the layering method and structurally characterized by elemental analysis,IR,and single-crystal X-ray diffraction.Complexes 1 and 2 are isostructural,and both crystallize in the orthorhombic system,space group Fdd2.X-ray structural analysis shows that 1 or 2 has an intriguing 3-D infinite network of（318.438.510） topology based on a 2-D sheet structure of（4,4） net.The result shows that noncovalent interactions play an important role in strengthening the whole structures of the compounds.
文摘The hydrochloride of 1-(1-amino-3-methyl)butyl borate pinacol is prepared by using the isobutylbromide to form the Grignard agent.The product is protected with the pinacol,then reacted with the lithium diisopropylamide and the anhydrous zinc chloride.Finally,the product is synthesized in the existence of the LHMDS.All the compounds are confirmed by MS and 1H-NMR.
文摘目的:研究自发性癫痫大鼠皮质、海马中谷氨酸转运体-1(GLT-1)、兴奋性氨基酸载体-1(EAAC-1)的转录、表达水平及其意义。方法:选取自发性癫痫Wistar大鼠(癫痫组)和正常Wistar大鼠(正常组)各10只,采用反转录-聚合酶链式反应(RT-PCR)技术检测2组大鼠皮质、海马中GLT-1、EAAC1 m RNA转录水平,采用蛋白质印迹技术检测2组大鼠皮质、海马中GLT-1、EAAC-1蛋白的表达水平。结果:癫痫组大鼠皮质中EAAC-1 m RNA相对灰度值为(0.67±0.21),明显低于正常组大鼠的(1.54±0.38)(P<0.01);2组大鼠皮质中GLT-1 m RNA和海马中GLT-1 m RNA、EAAC-1 m RNA相对灰度值差异无统计学意义(P>0.05)。癫痫组大鼠皮质中EAAC-1、GLT-1蛋白表达水平的相对灰度值分别为(72.6±8.7)和(103.7±12.6),显著低于正常组大鼠的(116.5±15.1)和(139.5±14.2)(P<0.01);癫痫组大鼠海马中GLT-1蛋白表达水平的相对灰度值(196.7±23.5)明显的高于正常组大鼠的(145.5±19.7)(P<0.01);2组大鼠海马中EAAC-1蛋白表达水平的相对灰度值差异无统计学意义(P>0.05)。结论:自发性癫痫大鼠皮质中GLT-1、EAAC-1表达水平下调可能与癫痫发生有关。
