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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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    Catalytic enantioselective N-silylation of sulfoximine

    Xingfen HuangJiefeng ZhuChuan He
    352-356页
    查看更多>>摘要：A rhodium/diphosphine-catalyzed asymmetric cross-dehydrogenative coupling between sulfoximines and dihydrosilanes has been achieved.This is the first report on the enantioselective N-silylation of sulfox-imines.The protocol gives access to a variety of Si-stereogenic N-silylated sulfoximines in decent yield(up to 99％)with excellent stereoselectivity(up to 99％),featuring high atom economy,and a cleaner manner with H2 as the sole byproduct.The obtained bis-Si-stereogenic monohydrosilane product can be further converted into the corresponding chiral polymer with pendant sulfoximine groups.
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    Catalytic asymmetric dearomative azo-Diels-Alder reaction of 2-vinlyindoles

    Yu-Hang MiaoZheng-Xu ZhangXu-Yi HuangYuan-Zhao Hua...
    357-362页
    查看更多>>摘要：Due to the high electrophilic nature of azo-dienophiles,azo-Diels-Alder proceeds rapidly even without the need of a catalyst and is therefore regarded as the"click reaction".This spontaneity causes strong background reaction and poses a daunting challenge to chemists for developing the catalytic asymmetric version.Reported herein is the first catalytic asymmetric dearomative azo-Diels-Alder reaction between 2-vinylindoles and triazoledione.This protocol makes use of the high energy barrier of dearomatization to avert the strong background reaction of azo-Diels-Alder reaction,allowing the implementation of the projected reaction at ambient temperature.Density functional theory calculations have been performed to gain insights into the reaction mechanism and the origins of the enantioselectivity.By using this method,a variety of tetracyclic indole derivatives have been readily prepared in good to excellent yields and with excellent diastereo-and enantio-selectivities(33 examples,up to 97％yield and＞99％ee,＞20:1 dr).
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    Rhodium-catalyzed Doyle-Kirmse rearrangement reactions of sulfoxoniun ylides

    Ying-Di HaoZhi-Qian LinXiao-Yu GuoJiao Liang...
    363-366页
    查看更多>>摘要：Doyle-Kirmse rearrangement reactions have received continuous attention as an important method for constructing complex chemical structures.Herein,we disclosed an efficient rhodium-catalyzed Doyle-Kirmse rearrangement reaction,which can simultaneously construct C-C bonds and C-X(X=S/Se)bonds using sulfoxonium ylides as starting materials to obtain sulfur-or selenium-containing compounds.This strategy is characterized by the safer and greener carbene precursor,high yields and broad substrate scope,possessing a wide range of application.
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    Efficient capture of difluorocarbene by pyridinium 1,4-zwitterionic thiolates:A concise synthesis of difluoromethylene-containing 1,4-thiazine derivatives

    Zhiwei ChenHeyun ShengXue LiMenghan Chen...
    367-370页
    查看更多>>摘要：A practical method for the construction of difluoromethylene-containing 1,4-thiazine moieties using read-ily available diethyl bromodifluoromethanephosphonate(BrCF2PO(OEt)2)as difluorocarbene precusor has been developed.This transformation features the efficient capture of difluorocarbene by pyridinium 1,4-zwitterionic thiolates.A series of structurally novel and functionalized difluoromethylene-containing 1,4-thiazine derivatives were thus synthesized in good yields.
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    Multistep continuous flow synthesis of Erlotinib

    Hui JinQin CaiPeiwen LiuYan Chen...
    371-375页
    查看更多>>摘要：Erlotinib is an orally administered,highly effective,specific epidermal growth factor receptor tyrosine kinase inhibitor,used to treat non-small cell lung cancer and pancreatic cancer.The traditional synthetic methods for Erlotinib exhibit long reaction time and safety concern.Herein,we describe a novel five-step route for the synthesis of Erlotinib in flow.These five steps comprise etherification,nitration,reduction,addition and cyclization reactions.All steps were optimized and converted to continuous flow process,which drastically reduces the reaction time and considerably improves the process safety as well as the total yield.Enabled by five continuous flow units,Erlotinib is efficiently afforded with an E-factor of 38,an overall yield of 83％,and a total residence time of 25.1 min.Majority steps in this process have been optimized for quantitative conversion,which offers the possibility of telescoping the entire process.
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    Mechanism of nanoparticle aggregation in gas-liquid microfluidic mixing

    Hongxia LiXiyang WangDu QiaoJiahao Li...
    376-381页
    查看更多>>摘要：Using gas-liquid segmented micromixers to prepare nanoparticles that have a homogeneous particle size,controllable shape,and monodispersity advantages.Although nanoparticle aggregation within a mi-crofluid has been shown to be affected by the shear effect,the shear effect triggering conditions in gas-liquid two-phase flow is unclear and the aggregation behavior of nanoparticles under the shear effect is difficult to predict,resulting in uncontrollable physical and chemical properties of nanoparticle ag-gregates.In this study,a numerical simulation of nanoparticle aggregation in gas-liquid two-phase flow under the shear effect is performed using the CFD-DEM method.Then,the effects of total flow rate,gas-liquid two-phase flow ratio,and particle volume fraction on particle aggregation were analyzed to achieve control of particle aggregation shape and size.Meanwhile,the triggering mechanism of the shear effect and the mechanism of the shear effect on the aggregation of nanoparticles were clarified.The re-sults show that increasing the total flow rate or decreasing the gas-liquid two-phase flow rate ratio can induce the shear effect,which reduces the particle aggregation size and makes the morphology tend to be spherical.Moreover,increasing the particle volume fraction,and total flow rate or decreasing the gas-liquid two-phase flow rate ratio also increases the number of particle collisions and induce interpar-ticle adhesion.Hence,particle adhesion and the shear effect compete with each other and together affect particle aggregation.
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    Computational fluid dynamics simulation and experimental study on mixing performance of a three-dimensional circular cyclone-type microreactor

    Shiyu HouMaolin SunLiming CaoChaoming Liang...
    382-388页
    查看更多>>摘要：Microchannels enable the fast and efficient mixing of multiphase fluids.In this study,a millimeter-scale three-dimensional(3D)circular cyclone-type microreactor was designed for the mixing.The flow char-acteristics and mixing intensity were simulated by computational fluid dynamics simulations at a flow rate range of 12-96 mL/min using a water/ethyl acetate system.In the 3D variable-diameter structure,the microreactor induced paired opposite vortices and abruptly changed the local pressure to achieve a stable turbulent effect within the theoretical range of laminar flow.Tracer injection simulations indicated that sufficient mixing units successfully promote fluid dispersion.Diazo-coupling experiments showed a segregation index of Xs=0.00,039 within a residence time of 9 s.Extraction experiments on the n-butanol/succinic acid/water system showed that the 3D circular cyclone-type microreactor achieved 100％extraction efficiency(E)in 4.25 s,and the overall volume mass transfer coefficient(KLa)reached 0.05-1.5 s-1 in 12-96 mL/min.The isolated yield of the phase transfer alkylation and oxidation reactions in the 3D circular cyclone-type microreactor achieved 99％within 36 s,which was superior to the coil microreactor and batch reactor.
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    A convenient method for measuring gas-liquid volumetric mass transfer coefficient in micro reactors

    Haoyang WangRonghao ZhangYanlun RenLi Zhang...
    389-392页
    查看更多>>摘要：The research on gas-liquid multiphase reactions using micro reactors is becoming increasingly widespread,given their excellent mass transfer performance.Establishing an accurate and reliable method to measure the gas-liquid mass transfer performance of micro reactors is crucial for evaluating and op-timizing the design of micro reactor structure.In this paper,the physical absorption method of aqueous solution-CO2 and the chemical absorption method of sodium carbonate solution-CO2 were proposed.By analyzing the chemical reaction equilibrium during the absorption process,the relationship between the mass transfer of CO2 and the solubility of hydroxide ions in the solution was established,and the total gas-liquid mass transfer coefficient was immediately obtained by measuring the pH value.The corre-sponding testing platform and process have been established based on the characteristics of the pro-posed method to ensure fast and accurate measurement.In addition,the chemical absorption method takes into account temperature factors that were not previously considered.The volumetric mass transfer coefficient measured by these two methods is in the same range as those measured by other methods using the same microchannel structure in previous literature.The methods have the advantages of low equipment cost,faster measurement speed,and simpler procedures,which can facilitate its wide applica-tion to the evaluation of the mass transfer performance and hence can guide the structure optimization of microchannel reactors.
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    Controlling solid form and crystal habit of triphenylmethanol by antisolvent crystallization in a microfluidic device

    Jun LuJinrui YanYaohao GuoJunjie Qiu...
    393-398页
    查看更多>>摘要：Crystal habit and crystal form are critical elements in determining product properties and functions.In this work,we developed a microfluidic antisolvent crystallization technique to rapidly screen and accu-rately control the solid form and crystal habit of triphenylmethanol(Ph3COH).This advanced technique separates the primary mixing of solutions from crystal formation(nucleation and growth)by introducing the microfluidic device,avoiding clogging in microchannels to obtain high-quality crystals.The results show that we can achieve controllable preparation of pure 2Ph3COH·DMSO(DMSO solvate),pure Ph3COH(form β),and mixed crystals with different mass ratios.Moreover,the microscale can prompt the DMSO solvate to grow into hexagonal sheet-like and bulk crystals.We can regulate the aspect ratio of hexag-onal sheet-like crystals in binary solvents and control the crystal habit of the form β to transition be-tween long needle-like shapes and short hexagonal prisms in DMF-H2O.Meanwhile,we revealed that the solvent ratio,the antisolvent flow rate,and the initial concentration of Ph3COH are the main factors affecting the solid form selectivity and morphology transition.Such a novel method would be considered as a promising technique to be extended to screen and control key crystallization parameters of other substances.
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    Efficient continuous synthesis of 2-hydroxycarbazole and 4-hydroxycarbazole in a millimeter scale photoreactor

    Zhixiang LiZhirong YangChang YaoBin Wu...
    399-403页
    查看更多>>摘要：2-Hydroxycarbazole and 4-hydroxycarbazole are important chemicals with extensive applications in op-toelectronic materials and pharmaceutical field.State of the art yield of 2-hydroxycarbazole is～30％and the reaction time is typically in hours or days.Herein,we developed a green route for the continuous and high-throughput synthesis of 2-hydroxycarbazole and 4-hydroxycarbazole via photochemical intramolecu-lar cyclization of 3-hydroxy-2'-chloro-diphenylamine using a self-designed millimeter scale photoreactor,which was designed based on sizing-up and numbering-up strategies for a decent liquid holdup(6.8 mL)and fabricated via femtosecond laser engraving technique.The photochemical synthesis was carried out continuously under the illumination of 365 nm UV-LED with dimethyl sulfoxide as solvent and potassium t-butoxide as catalyst.It was found that under optimized conditions a 2-hydroxycarbazole yield of 31.6％and a 4-hydroxycarbazole yield of 11.1％were obtained with a residence time of 1 min.Compared to semi-batch operations,the reaction time was shortened by 1-2 orders of magnitude.As a result,a throughput of 11.3g/day 2-hydroxycarbazole and 4.0g/day 4-hydroxycarbazole can be achieved from the photoreac-tor.It was proposed that the short reaction time and high product yield are resulted from higher photon transfer rates and more uniform photon distribution provided by the millimeter scale photoreactor,which enhances the reaction rates and mitigates overreaction.
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