Unprecedented divergent synthesis of gem-difluorovinylacetic acid and glutaric acid derivatives fromα-CF_(3)alkenes with formate as the carbonyl source was disclosed.The reaction can undergo selective mono-or triple ...Unprecedented divergent synthesis of gem-difluorovinylacetic acid and glutaric acid derivatives fromα-CF_(3)alkenes with formate as the carbonyl source was disclosed.The reaction can undergo selective mono-or triple C-F bond cleavage by simply switching the photocatalyst and hydrogen atom transfer(HAT)catalyst under visible-light-induced conditions at room temperature.Foramte acts as both the C1 source and the reductant through the generation of CO_(2)^(·-)species,which underwent Giese radical addition to electron-deficient alkenes to trigger the consecutive C-F bond cleavage and carboxylation process.展开更多
The contents of total phenolics, flavonoid and chlorogenic acid in two types of sand pear fruits 〔\%Pyrus pyrifolia \%(Burm. f.) Nakai〕, and antioxidant activities in its juice were analysed. The results showed that...The contents of total phenolics, flavonoid and chlorogenic acid in two types of sand pear fruits 〔\%Pyrus pyrifolia \%(Burm. f.) Nakai〕, and antioxidant activities in its juice were analysed. The results showed that the contents of total phenolics and flavonoid in fruit of black sand pear were higher than that of red sand pear fruit obviously, but chlorogenic acid contents were not different in two types of sand pear fruit. The CI\-\{50\}of scavenging ·OH of their juice were 30.6 μL and 69.5 μL respectively. And their juice could inhibit lipid peroxidation significantly in brain and liver homogenates of rat. These implied that sand pear fruits have large quantity of antioxidant matters and were worthy to be further researched.展开更多
目的 8 异前列腺素F2α(8 iso PGF2α)是一种敏感、特异性反映缺血 再灌注后氧自由基增加的生 化指标。抗氧化剂N 乙酰半胱氨酸(NAC)具有清除氧自由基的作用。本研究旨在分析实验性心肌缺血大鼠血浆 与心肌8 iso PGF2α相关性以及...目的 8 异前列腺素F2α(8 iso PGF2α)是一种敏感、特异性反映缺血 再灌注后氧自由基增加的生 化指标。抗氧化剂N 乙酰半胱氨酸(NAC)具有清除氧自由基的作用。本研究旨在分析实验性心肌缺血大鼠血浆 与心肌8 iso PGF2α相关性以及NAC的治疗效果,探讨血浆8 iso PGF2α反映心肌氧自由基损伤程度的可能性和 NAC的干预效果。方法 45只雄性成年Wistar大鼠随机分为3组(每组15只):对照组、缺血组和NAC组。缺血 组和NAC组腹腔注射垂体后叶素(20U/kg)制成大鼠急性心肌缺血模型,以心电图上ST段的抬高作为心肌缺血 的指标。对照组仅腹腔注射生理盐水。NAC组缺血前2周开始用NAC(每日0.1g/kg)灌胃,共3周。应用ELISA 方法测定各组大鼠血浆及心肌组织8 iso PGF2α含量。结果 缺血组大鼠的血浆和心肌组织含量分别为(187.1± 45.8)pg/mL和(259.3±47.5)pg/g,明显高于正常对照组(60.4±13.7)pg/mL和(88.6±16.9)pg/g (P<0.01);NAC组的血浆和心肌组织8 iso PGF2α含量为(88.2±16.4)pg/mL和(109.4±24.7)pg/g明显低于 缺血组(P<0.01)。血浆与心肌8 iso PGF2α水平相关(r=0.856,P<0.01)。与正常组比较,缺血组的心电图 ST段明显抬高(心肌缺血45min时抬高最为明显,达0.34±0.05mV)(P<0.05);展开更多
Construction of C-F bonds is a direct and efficient method for introducing fluorine into pharmaceuticals,agrochemicals,and materials.Strategies such as nucleophilic,electrophilic,radical,and transition-metal catalyzed...Construction of C-F bonds is a direct and efficient method for introducing fluorine into pharmaceuticals,agrochemicals,and materials.Strategies such as nucleophilic,electrophilic,radical,and transition-metal catalyzed fluorination have been developed to meet the demand of diverse C-F bond formation.Among them,radical fluorination has been witnessed with substantial advancement in a recent decade.Herein,we reviewed methods for formation of C-F bonds with carbon-centered radicals as key intermediates,especially in recent five years.We introduce in the paper with different fluorinating reagents,strategies for radical generation,and application in late-stage functionalization and synthesis of PET tracers.We also indicate the current limitations and propose the direction of the field for the future development.展开更多
基金supported by the National Natural Science Foundation of China(22001224)the Natural Science Foundation of Jiangsu Province(BK20201014,BK20200106)+2 种基金the Start-up Funding provided by Xuzhou Medical Universityalso supported by the Jiangsu Specially-Appointed Professor Program(Xu Zhu)Jiangsu Province Shuangchuang PhD Program(Pei Xu,JSSCBS20211267)。
文摘Unprecedented divergent synthesis of gem-difluorovinylacetic acid and glutaric acid derivatives fromα-CF_(3)alkenes with formate as the carbonyl source was disclosed.The reaction can undergo selective mono-or triple C-F bond cleavage by simply switching the photocatalyst and hydrogen atom transfer(HAT)catalyst under visible-light-induced conditions at room temperature.Foramte acts as both the C1 source and the reductant through the generation of CO_(2)^(·-)species,which underwent Giese radical addition to electron-deficient alkenes to trigger the consecutive C-F bond cleavage and carboxylation process.
文摘The contents of total phenolics, flavonoid and chlorogenic acid in two types of sand pear fruits 〔\%Pyrus pyrifolia \%(Burm. f.) Nakai〕, and antioxidant activities in its juice were analysed. The results showed that the contents of total phenolics and flavonoid in fruit of black sand pear were higher than that of red sand pear fruit obviously, but chlorogenic acid contents were not different in two types of sand pear fruit. The CI\-\{50\}of scavenging ·OH of their juice were 30.6 μL and 69.5 μL respectively. And their juice could inhibit lipid peroxidation significantly in brain and liver homogenates of rat. These implied that sand pear fruits have large quantity of antioxidant matters and were worthy to be further researched.
文摘目的 8 异前列腺素F2α(8 iso PGF2α)是一种敏感、特异性反映缺血 再灌注后氧自由基增加的生 化指标。抗氧化剂N 乙酰半胱氨酸(NAC)具有清除氧自由基的作用。本研究旨在分析实验性心肌缺血大鼠血浆 与心肌8 iso PGF2α相关性以及NAC的治疗效果,探讨血浆8 iso PGF2α反映心肌氧自由基损伤程度的可能性和 NAC的干预效果。方法 45只雄性成年Wistar大鼠随机分为3组(每组15只):对照组、缺血组和NAC组。缺血 组和NAC组腹腔注射垂体后叶素(20U/kg)制成大鼠急性心肌缺血模型,以心电图上ST段的抬高作为心肌缺血 的指标。对照组仅腹腔注射生理盐水。NAC组缺血前2周开始用NAC(每日0.1g/kg)灌胃,共3周。应用ELISA 方法测定各组大鼠血浆及心肌组织8 iso PGF2α含量。结果 缺血组大鼠的血浆和心肌组织含量分别为(187.1± 45.8)pg/mL和(259.3±47.5)pg/g,明显高于正常对照组(60.4±13.7)pg/mL和(88.6±16.9)pg/g (P<0.01);NAC组的血浆和心肌组织8 iso PGF2α含量为(88.2±16.4)pg/mL和(109.4±24.7)pg/g明显低于 缺血组(P<0.01)。血浆与心肌8 iso PGF2α水平相关(r=0.856,P<0.01)。与正常组比较,缺血组的心电图 ST段明显抬高(心肌缺血45min时抬高最为明显,达0.34±0.05mV)(P<0.05);
基金the National Natural Science Foundation of China(22301224)Wuhan Science and Technology Project(2023020201020273),and Wuhan University for financial support.We thank Prof.Wen-Bo Liu(Wuhan University)for proof reading.
文摘Construction of C-F bonds is a direct and efficient method for introducing fluorine into pharmaceuticals,agrochemicals,and materials.Strategies such as nucleophilic,electrophilic,radical,and transition-metal catalyzed fluorination have been developed to meet the demand of diverse C-F bond formation.Among them,radical fluorination has been witnessed with substantial advancement in a recent decade.Herein,we reviewed methods for formation of C-F bonds with carbon-centered radicals as key intermediates,especially in recent five years.We introduce in the paper with different fluorinating reagents,strategies for radical generation,and application in late-stage functionalization and synthesis of PET tracers.We also indicate the current limitations and propose the direction of the field for the future development.