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中国化学快报(英文版)
中国化学快报(英文版)

梁晓天

月刊

1001-8417

cclbj@imm.ac.cn

010-63165638

100050

北京市先农坛街1号

中国化学快报(英文版)/Journal Chinese Chemical LettersCSCDCSTPCD北大核心SCI
查看更多>>本刊是由中国科协主管、中国化学会主办、中国医学科学院药物所承办的学术期刊,是由著名化学家梁晓天院士主编。是中国化学界通向世界的窗口,内容覆盖化学全领域。本刊的办刊宗旨是“新、快、准”,我们将坚持这个宗旨,力求及时反映化学研究中各个相关领域内的最新进展及热点问题,主要读者群是科研人员、研究生、大学教师。现已被国内外多家数据库收录,如SCI Search、Chemical Abstract、Research Alert、Chemistry Citation Index、《日本科技文献速报》、万方数据数字化期刊群、中国学术期刊过刊全文数据库、中国学术期刊(光盘版)、中国学术期刊文摘、中文期刊全文数据库、俄罗斯Рж期刊源等。
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    A sequential continuous flow synthesis and purification process of calcium dibutyryladenosine cyclophosphate

    Liming CaoMaolin SunChaoming LiangLei Yang...
    402-406页
    查看更多>>摘要:Calcium dibutyryladenosine cyclophosphate is a widely used cardiovascular drug.The traditional batch synthesis process suffers from long reaction times,tedious operations,and unstable yields.Herein,a se-quential continuous flow synthesis combined with a multistage in-line purification process of calcium dibutyryladenosine cyclophosphate was developed.The acylation reaction was completed in a continu-ous coil reactor at 160 ℃ in 20 min.And the high toxic solvent pyridine was replaced by acetonitrile.Furthermore,the multistage in-line purification process was integrated into the homemade 3D circular cyclone-type micromixer chip.Combining with the membrane phase separators,the residence time of the purification step was 30 s.The isolated yield of this sequential continuous process was 92%with 99%purity.

    Mo@PANI-catalyzed oxidative deoximation reaction

    Yiyang ZhangWen LiZuofeng HuXiaobi Jing...
    407-410页
    查看更多>>摘要:Deoximation is an important transformation in synthetic industry.It can be employed in protection,characterization and purification of the carbonyls,and in the synthesis of ketones from non-carbonyl molecules.In the field,oxidative deoximation reaction can utilize the driving force caused by the oxida-tion process so that the reaction can occur under relatively mild conditions.Recently,we designed and prepared polyaniline-supported molybdenum(Mo@PANI)just by immersing PANI into the EtOH/H2O so-lution of MoCl5.The material was successfully applied as the efficient catalyst for oxidative deoximation reactions,which were performed in ethanol using H2O2 as the clean oxidant.The substrate scope of the reaction was wide.It could be applied on heterocycle-containing substrates,making this protocol prefer-able for pharmaceutical intermediate synthesis.Since Mo is a necessary trace element for both animals and plants,this method is environment-friendly and is suitable for large-scale preparation.This work as the first example of Mo-catalyzed oxidative deoximation reaction may inspire novel ideas for both cata-lyst design and synthetic process development.

    Charge transfer complex enabled photoreduction of ether phosphonium salts for the selective oxyalkylation of enamides

    Sen QiaoKunquan ChenQiang LiuZhixiang Wang...
    411-414页
    查看更多>>摘要:A charge transfer complex(CTC)-enabled photoreduction of ether phosphonium salts for the generation of oxyalkyl radicals was described.The photoreduction provides a convenient method to achieve selective oxyalkylation of enamides with broad substrate scope.The method features operational simplicity,mild and inherent green conditions.

    Additive-free synthesis of S-substituted isothioureas via visible-light-induced four-component reaction of α-diazoesters,aryl isothiocyanates,amines and cyclic ethers

    Yufen LvHongyu DingJinmao YouWei Wei...
    415-419页
    查看更多>>摘要:An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting from α-diazoesters,aryl isothiocyanates,amines and cyclic ethers.This methodology features simple operation,mild reaction conditions,favorable functional group tolerance,easily available starting materials and high efficiency.

    Palladium-catalyzed multi components oxy-aminofluorination and aminofluorination of gem-difluoroalkenes

    Fen WuXin LiJunbiao ChangDachang Bai...
    420-425页
    查看更多>>摘要:Organofluorine compounds are widely used in the realm of drug discovery and material science.Herein,we developed palladium catalyzed intermolecular aminofluorination and oxy-aminofluorination of gem-difluoroalkenes with N-fluorobenzenesulfonimide(NFSI),in which NFSI was used as the nitrogen source and oxidant.The reaction provides an efficient and straightforward synthesis route of a series of α-trifluoromethyl benzylic amines.Notably,three/four components oxy-aminofluorination processes were realized to give α-trifluoromethyl benzylic ether with a terminal amino group,which proceed through C(sp3)-O bond cleavage of easily available ether and simultaneous introduced a fluorine,an amino and an oxy substituent in one pot with excellent regioselectivity.The divergent reactivity not only included the incorporation of one ether molecular,but also much more challenged two ether insertion with excel-lent selectivity through succession C(sp3)-O bonds cleavage.This protocol allows for concise synthesis of high value amines with fluoroalkyl-substituents and selectively transformation of easily available ethers by high-valent palladium catalysis.

    Anion cascade reactions Ⅲ:Synthesis of 3-isoquinuclidone bridged polycyclic lactams

    Zhiguo ZhangBingbing ShiXiyang CaoNana Ma...
    426-430页
    查看更多>>摘要:Bridged polycyclic lactams are important structural units in organic functional materials,natural products,and pharmaceuticals.A flexible and efficient anion cascade reaction was developed for the preparation of bridged polycyclic lactams from readily available malonamides and 1,4-dien-3-ones.Various highly sub-stituted bridged polycyclic lactams were synthesized in good to excellent yields by tandem nucleophilic sequences in the presence of tBuOK in commercially available EtOH solvent at 60 ℃.Notably,the simple reactions can be run on a gram scale.Mechanistically,bis-Michael addition reaction and hemiaminaliza-tion reactions are involved in the tandem transformation.

    Chemoselective electrochemical seleno-cyclization of dienes to medium-sized benzo[b]azocines

    Zhichuan WangXin WangQuanxin LiShaofei Ni...
    431-435页
    查看更多>>摘要:The preparation of medium-sized benzo[b]azocines has always been challenging because of inher-ently unfavorable enthalpy and entropy factors.This report presents a novel approach for accessing 8-membered seleno-benzo[b]azocines via electrochemically-driven seleno-cyclization.This method enables room-temperature preparation of various structurally diverse medium-sized seleno-benzo[b]azocines.The facile deselenation of the seleno-cyclization products to generate functionalized dienes is an additional benefit of this indispensable reaction.Mechanistic insights are presented based on radical inhibition ex-periments and cyclic voltammetry measurements,which elucidate the radical pathway.Finally,density functional theory calculations further rationalize the rate-determining step and the unique chemoselec-tivity observed in this transformation.

    Single-cell mass spectrometry studies of drug metabolism heterogeneity and primary resistance to gefitinib in non-small cell lung cancer cells

    Guizhen ZhuYaoyao ZhaoWenmei ZhangYuanyuan Wu...
    436-440页
    查看更多>>摘要:Patients with epidermal growth factor receptor(EGFR)wild-type non-small cell lung cancer(NSCLC)of-ten show primary resistance to gefitinib therapy.It is thus necessary to study the metabolism of gefitinib in NSCLC cells to comprehensively reveal the reasons for the primary resistance of tumors.Herein,we develop a platform for studying drug metabolism heterogeneity based on single-cell mass spectrometry(sDMH-scMS)by integrating living-cell electrolaunching ionization MS(ILCEI-MS)and high-performance liquid chromatography-MS(HPLC-MS)analysis,and the primary resistance of NSCLC cells to gefitinib was studied using this platform.The ILCEI-MS analysis showed that approximately 11.9%of NSCLC single cells contained the gefitinib metabolite M11;HPLC-MS detection diluted the intensity of M11 in subpopula-tions and concealed the heterogeneity of drug metabolism in tumor single cells.The intensity of gefitinib in EGFR wild-type A549 cells was markedly lower than in mutant PC9 cells,and the intensity of gefitinib metabolites was significantly higher than in PC9 cells,suggesting that the primary resistance of NSCLC cells is related to gefitinib metabolism.Moreover,the combination of gefitinib and the drug-metabolizing enzyme inhibitor α-naphthoflavone was shown to overcome the primary resistance of the NSCLC cells.Overall,the results of this study are expected to be applicable for clinical drug resistance diagnosis and treatment at the single-cell level.

    Highly efficient labelling of extracellular vesicles for enhanced detection on a microfluidic platform

    Shi HuRui HaoZitong YuHuitao Zhang...
    441-445页
    查看更多>>摘要:Developing precise extracellular vesicles(EVs)labelling techniques with minimal disturbance is of great importance to the follow-up EVs detection and analysis.However,currently available methods such as using probes to conjugate phospholipids or membrane proteins have certain limitations due to EV steric hindrance,dye aggregation,etc.Here,we present a microfluidic platform to enhance EVs'labelling ef-ficiency and improve their detection.This platform provides excellent sample throughput and high-efficiency EV labelling at lower label concentrations with an optimized flowing rate.Flow cytometry analysis(FCM)and cellular uptake results show that EV labelling by utilizing this platform possesses the merits of a higher labelling efficiency with 64.1%relative improvement than conventional co-incubation method and a lower background noise.Moreover,this technique maintains EVs'size,morphology and biological activities.After the recipient cells uptake the EVs treated by the microfluidic platform,the spa-tial and temporal distribution of EVs in the cells are clearly observed.These results demonstrate that our method holds great potential in efficient labelling of EVs,which is essential to subsequent EV quantifica-tion and analysis.

    Enhanced visible-light photocatalytic hydrogen evolution using two-dimensional carbon nitride sheets with the removal of amine groups

    Yu ZhangLiting WuShaopeng WangDingyi Yang...
    446-450页
    查看更多>>摘要:Two-dimensional(2D)carbon nitride sheets(CNs)with atomically thin structures are regarded as one of the most promising materials for solar energy conversion.However,due to their substantially en-larged bandgap caused by the strong quantum size effect and their incomplete polymerisation with a large number of non-condensed surface amino groups,the practical applicability of CNs in photocatalysis is limited.In this study,CNs with broad visible-light absorption were synthesised using a 5-min fast ther-mal annealing.The removal of uncondensed amine groups reduces the bandgap of CNs from 3.06 eV to 2.60 eV,increasing their absorption of visible light.Interestingly,the CNs were distorted after annealing,which can differentiate the spatial positions of electrons and holes,enhancing the visible-light absorption efficiency.As a result,when exposed to visible light,the photocatalytic hydrogen production activity of atomically thin 2D CNs rose by 8.38 times.This research presents a dependable and speedy method for creating highly effective visible-light photocatalysts with narrowed bandgaps and improved visible-light absorption.