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Multistep continuous flow synthesis of Erlotinib

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Chinese Chemical Letters 2024年第4期35卷 371-375页

作者： Hui Jin Qin cai Peiwen liu yan Chen Derong Wang Weiping zhu Yufang Xu Xuhong Qian State Key Laboratory of Bioreactor Engineering Shanghai Key Laboratory of Chemical BiologySchool of PharmacyEast China University of Science and TechnologyShanghai 200237China

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.

关键词： Erlotinib Continuous flow synthesis Microchannel flow reactor Process optimization Continuous nitration Continuous hydrogenation

Genomes of Meniocus linifolius and Tetracme quadricornis reveal the ancestral karyotype and genomic features of core Brassicaceae

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Plant Communications 2024年第7期5卷 68-89页

作者： Jie liu Shi-Zhao Zhou Yun-Long liu Bin-yan Zhao Dongmei Yu Mi-cai Zhong Xiao-Dong Jiang Wei-hua Cui Jiu-Xia Zhao Juan Qiu Liang-Min liu Zhen-hua Guo Hong-Tao Li Dun-yan Tan Jin-Yong Hu De-zhu Li CAS Key Laboratory for Plant Diversity and Biogeography of East Asia&Yunnan Key Laboratory of Crop Wild Relatives Omics Kunming Institute of BotanyChinese Academy of SciencesKunming 650201China Germplasm Bank of Wild Species&Yunnan Key Laboratory for Crop Wild Relatives Omics Kunming Institute of BotanyChinese Academy of SciencesKunming 650201China College of Life Sciences Xinjiang Agricultural UniversityÜrümqi 830052China University of Chinese Academy of Sciences Beijing 100049China These authors contributed equally to this article

Brassicaceae represents an important plant family from both a scientific and economic ***,genomic features related to the early diversification of this family have not been fully characterized,especially upon the uplift of the Tibetan Plateau,which was followed by increasing aridity in the Asian interior,intensifying monsoons in Eastern Asia,and significantly fluctuating daily ***,we reveal the genomic architecture that accompanied early Brassicaceae diversification by analyzing two high-quality chromosome-level genomes for Meniocus linifolius(Arabodae;clade D)and Tetracme quadricornis(Hesperodae;clade E),together with genomes representing all major Brassicaceae clades and the basal *** reconstructed an ancestral core Brassicaceae karyotype(CBK)containing 9 pseudochromosomes with 65 conserved syntenic genomic blocks and identified 9702 conserved genes in *** detected pervasive conflicting phylogenomic signals accompanied by widespread ancient hybridization events,which correlate well with the early divergence of core *** identified a successive Brassicaceae-specific expansion of the class I TREHALOSE-6-PHOSPHATE SYNTHASE 1(TPS1)gene family,which encodes enzymes with essential regulatory roles in flowering time and embryo *** TPS1s were mainly randomly amplified,followed by expression *** results provide fresh insights into historical genomic features coupled with Brassicaceae evolution and offer a potential model for broad-scale studies of adaptive radiation under an ever-changing environment.

关键词： Cruciferae genomic features ancient hybridization core Brassicaceae karyotype CBK TREHALOSE-6-PHOSPHATE SYNTHASE 1 genes TPS1s

IoV environment exploring coordination:A federated learning approach

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Digital Communications and Networks 2024年第1期10卷 135-141页

作者： Tong Ding Lei liu Yi zhu Lizhen Cui Zhongmin yan School of Software Shandong UniversityJinan250101China

Exploring open fields with coordinated unmanned vehicles is popular in academia and *** of the most impressive applicable approaches is the Internet of Vehicles(lov).The IoV connects vehicles,road infrastructures and communication facilities to provide solutions for exploration ***,the coordination of acquiring information from multi-vehicles may risk data *** this end,sharing high-quality experiences instead of raw data has become an urgent *** paper employs a Deep Reinforcement Learning(DRL)method to enable IoVs to generate training data with prioritized experience and states,which can support the IoV to explore the environment more ***,a Federated Learning(FL)experience sharing model is established to guarantee the vehicles'*** numerical results show that the proposed method presents a better successful sharing rate and a more stable convergence within the comparison of fundamental *** experiments also suggest that the proposed method could support agents without full information to achieve the tasks.

关键词： Internet of vehicle Deep reinforcement learning Federated learning Data privacy

Retrospective analysis of patients with hepatocellular carcinoma complicated with human immunodeficiency virus infection after hepatectomy

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World Journal of Gastrointestinal Oncology 2024年第9期16卷 3851-3864页

作者： Jia-Jie Lu Shuai yan Lin Chen Lin-Ling Ju Wei-hua cai Jin-zhu Wu Department of Hepatobiliary Surgery Nantong Third People's HospitalMedical School of Nantong UniversityNantong 226000Jiangsu ProvinceChina Department of Medical School Nantong UniversityNantong 226300Jiangsu ProvinceChina Institute of Liver Disease Nantong Third People’s HospitalAffiliated Nantong Hospital 3 of Nantong UniversityNantong 226000Jiangsu ProvinceChina Department of Hepatobiliary Surgery Affiliated Nantong Hospital 3 of Nantong UniversityNantong 226006Jiangsu ProvinceChina

BACKGROUND Hepatocellular carcinoma(HCC)is the third leading cause of cancer death worldwide,with a 5-year relative survival rate of approximately 18%.The similarity between incidence and mortality(830000 deaths per year)underscores the bleak prognosis associated with the *** is the fourth most common malignancy and the second leading cause of cancer death in *** patients with HCC have a history of chronic liver disease such as chronic hepatitis B virus(HBV)or hepatitis C virus(HCV)infection,alcoholism or alcoholic steatohepatitis,nonalcoholic fatty liver disease,or nonalcoholic *** diagnosis and effective treatment are the keys to improving the prognosis of patients with *** the total number of human immunodeficiency virus(HIV)-infected patients is declining globally the incidence of HCC is increasing in HIVinfected patients,especially those who are coinfected with HBV or *** a result,people infected with HIV still face unique challenges in terms of their risk of developing *** To investigate the survival prognosis and clinical efficacy of surgical resection in patients with HCC complicated with HIV *** The clinical data of 56 patients with HCC complicated with HIV admitted to the Third Affiliated Hospital of Nantong University from January 2013 to December 2023 were retrospectively *** these,27 patients underwent hepatectomy(operation group)and 29 patients received conservative treatment(nonoperation group).All patients signed informed consents in line with the provisions of medical *** general data,clinicopathological features and prognoses for the patients in the two groups were analyzed and the risk factors related to the prognoses of the patients in the operation group were *** The median disease-free survival(DFS)and overall survival(OS)of HIV-HCC patients in the surgical group were 13 months and 17 months,respectively,and the median OS of patients in the nonsurgic

关键词： Hepatocellular carcinoma Human Immunodeficiency virus Liver resection Retrospective analysis Prognosis

Multi-omics analysis of attenuated variant reveals potential evaluation marker of host damaging for SARS-CoV-2 variants

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Science China(Life Sciences) 2024年第1期67卷 83-95页

作者： Guangshan Xie Lin zhu Siwen liu cun Li Xin Diao yanhao Zhang Xiuli Su Yuanyuan Song Guodong Cao Li Zhong Pui Wang Xiaojuan liu Bobo Wing-Yee Mok Shusheng Zhang Dong-yan Jin Jie Zhou Honglin Chen Zongwei cai State Key Laboratory of Environmental and Biological Analysis Hong Kong Baptist UniversityHong Kong SARChina State Key Laboratory for Emerging Infectious Diseases and Department of MicrobiologyLi Ka Shing Faculty of MedicineThe University of Hong KongHong Kong SARChina College of Chemistry Zhengzhou UniversityZhengzhou 450001China School of Biomedical Sciences The University of Hong KongHong Kong SARChina HKBU Shenzhen Institute of Research and Continuing Education Shenzhen 518000China

SARS-CoV-2 continues to threaten human society by generating novel variants via mutation and *** high number of mutations that appeared in emerging variants not only enhanced their immune-escaping ability but also made it difficult to predict the pathogenicity and virulence based on viral nucleotide *** markers for evaluating the pathogenicity of new variants are therefore *** comparing host responses to wild-type and variants with attenuated pathogenicity at proteome and metabolome levels,six key molecules on the polyamine biosynthesis pathway including putrescine,SAM,dc-SAM,ODC1,SAMS,and SAMDC were found to be differentially upregulated and associated with pathogenicity of *** validate our discovery,human airway organoids were subsequently used which recapitulates SARS-CoV-2 replication in the airway epithelial cells of COVID-19 *** ODC1 as a proof-ofconcept,differential activation of polyamine biosynthesis was found to be modulated by the renin-angiotensin system(RAS)and positively associated with ACE2 *** experiments demonstrated that ODC1 expression could be differentially activated upon a panel of SARS-CoV-2 variants of concern(VOCs)and was found to be correlated with each VOCs’pathogenic ***,the presented study revealed the discriminative ability of key molecules on polyamine biosynthesis as a predictive marker for virulence evaluation and assessment of SARS-CoV-2 variants in cell or organoid *** work,therefore,presented a practical strategy that could be potentially applied as an evaluation tool for the pathogenicity of current and emerging SARS-CoV-2 variants.

关键词： SARS-CoV-2 multi-omics attenuated variant predictive pathogenic marker polyamine biosynthesis

Computation of the exact time delay margin for vehicle platoon under generic communication topologies

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Journal of Traffic and Transportation Engineering(English Edition) 2024年第4期11卷 761-775页

作者： Xu zhu Maode yan Panpan yang Yongtao liu School of Electronic and Control Engineering Chang'an UniversityXi'an 710064China School of Automobile Chang'an UniversityXi'an 710064China

Due to the limited bandwidth and transmission congestion of the vehicle platoon's communication,it is inevitable to induce time delay,which significantly degrades the control performance of the vehicle platoon,even resulting in *** paper focuses on analyzing the internal stability under generic communication topologies and presents a method of computing the exact time delay margin(ETDM).The proposed method can offer a necessary and sufficient internal stability condition with no ***,to reduce the analytical complexity and computational burden elegantly,we decompose the closed-loop platoon dynamics into a set of individual subsystems via similarity transformation and matrix *** decomposition approach is applicable for any general communication ***,an explicit formula is deduced to compute the ETDM by surveying the characteristic roots'distribution of all these individual *** is further demonstrated that only the positive purely imaginary roots need to be considered to compute the ***,simulations are conducted to demonstrate the effectiveness of the theoretical claims.

关键词： Vehicle platoon Exact time delay margin Generic communication topologies System decomposition Characteristic roots'distribution

Garnet and Zircon U-Pb Geochronology and Geochemistry Reveal Genesis of the Dafang Au-Pb-Zn-Ag Deposit,Southern Hunan

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Acta Geologica Sinica(English Edition) 2024年第3期98卷 717-735页

作者： JIANG hua KONG hua liu Biao TAN Fucheng QIN Yixue huaNG Jingang zhu Yu Key Laboratory of Metallogenic Prediction of Nonferrous Metals and Geological Environment Monitoring Ministry of EducationSchool of Geosciences and Info-PhysicsCentral South UniversityChangsha 410083China School of Geosciences and Info-Physics Central South UniversityChangsha 410083China Hunan Baoshan Nonferrous Metals and Minerals Co. Ltd.ChenzhouHunan 424402China

Garnet is a primary mineral in skarn deposits and plays a significant role in recording copious mineralization and metallogenic *** study systematically investigates the geochemistry and geochronology of garnet and zircon in the Dafang Au-Pb-Zn-Ag deposit,which represents prominent gold mineralization in southern Hunan,*** samples with distinct zoning patterns and compositional variations were identified using various analytical techniques,including Backscattered Electron(BSE)imaging,Cathodoluminescence(CL)response,textural characterization,and analysis of rare-earth elements(REE),major contents,and trace element *** garnet was dated U-Pb dating,which yielded a lower intercept age of 161.06±1.93 *** age is older than the underlying granodiorite porphyry,which has a concordia age of 155.13±0.95 Ma determined by zircon U-Pb *** results suggest that the gold mineralization may be related to the concealed *** groups of garnet changed from depleted Al garnet to enriched Al garnet,and the rare earth element(REE)patterns of these groups were converted from light REE(LREE)-enriched and heavy REE(HREE)-depleted with positive europium(Eu)anomalies to medium REE(MREE)-enriched from core to rim *** different REE patterns of garnet in various zones may be attributed to changes in the fluid environment and late superposition *** development of distal skarn in the southern Hunan could be a significant indicator for identifying gold mineralization.

关键词： garnet and zircon U-Pb dating LA-ICP-MS mapping Dafang Southern Hunan

TRPC6 Knockout Alleviates Renal Fibrosis through PI3K/AKT/GSK3B Pathway

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Current Medical Science 2024年第3期44卷 589-602页

作者： An-bang SUN Fang-hua LI Lin zhu Xi-xi ZENG Min zhu Qing-hua LEI yan-hong LIAO Department of Anatomy School of Basic MedicineTongji Medical CollegeHuazhong University of Science and TechnologyWuhan430030China Department of Transfusion Medicine Wuhan Hospital of Traditional Chinese and Western MedicineTongji Medical CollegeHuazhong University of Science and TechnologyWuhan430030China Department of Nephrology The First Affiliated Hospital of Zhengzhou UniversityZhengzhou450052China Department of Thoracic Surgery Tongji HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan430030China National Basic Medical Teaching Demonstration Center Tongji Medical CollegeHuazhong University of Science and TechnologyWuhan430030China Key Laboratory of Neurological Diseases of Ministry of Education Tongji Medical CollegeHuazhong University of Science and TechnologyWuhan430030China

Objective Renal fibrosis is the ultimate pathway of various forms of acute and chronic kidney ***,the knockout of transient receptor potential channel 6(TRPC6)has shown promise in alleviating renal ***,the regulatory impact of TRPC6 on renal fibrosis remains *** In vivo,TRPC6 knockout(TRPC6−/−)mice and age-matched 129 SvEv(WT)mice underwent unilateral renal ischemia-reperfusion(uIR)injury surgery on the left renal pedicle or sham *** and serum were collected on days 7,14,21,and 28 after *** vitro,primary tubular epithelial cells(PTECs)were isolated from TRPC6−/−and WT mice,followed by treatment with transforming growth factorβ1(TGFβ1)for 72 *** anti-fibrotic effect of TRPC6−/−and the underlying mechanisms were assessed through hematoxylin-eosin staining,Masson staining,immunostaining,qRT-PCR,and Western *** Increased TRPC6 expression was observed in uIR mice and PTECs treated with TGFβ***6−/−alleviated renal fibrosis by reducing the expression of fibrotic markers(Col-1,α-SMA,and vimentin),as well as decreasing the apoptosis and inflammation of PTECs during fibrotic progression both in vivo and in ***,we found that the phosphatidylinositol 3-kinase(PI3K)/protein kinase B(AKT)/glycogen synthase kinase 3 beta(GSK3β)signaling pathway,a pivotal player in renal fibrosis,was down-regulated following TRPC6 *** These results suggest that the ablation of TRPC6 may mitigate renal fibrosis by inhibiting the apoptosis and inflammation of PTECs through down-regulation of the PI3K/AKT/GSK3β*** TRPC6 could be a novel therapeutic strategy for preventing chronic kidney disease.

关键词： transient receptor potential channel 6 ischemia-reperfusion injury renal fibrosis renal tubular epithelial cells

Effects of impregnation sequence on the NH_(3)-SCR activity and hydrothermal stability of a Ce-Nb/SnO_(2) catalyst

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Journal of Environmental Sciences 2024年第4期138卷 450-457页

作者： Ying zhu Wenpo Shan Zhihua Lian Jingjing liu yan Zhang Hong He Center for Excellence in Regional Atmospheric Environment and Key Laboratory of Urban Pollutant Conversion Institute of Urban EnvironmentChinese Academy of SciencesXiamen 361021China Zhejiang Key Laboratory of Urban Environmental Processes and Pollution Control Ningbo Urban Environment Observation and Research StationInstitute of Urban EnvironmentChinese Academy of SciencesNingbo 315800China State Key Joint Laboratory of Environment Simulation and Pollution Control Research Center for Eco-Environmental SciencesChinese Academy of SciencesBeijing 100085China University of Chinese Academy of Sciences Beijing 100049China

Hydrothermal stability is crucial for the practical application of deNO_(x)catalyst on diesel vehicles,for the selective catalytic reduction of NO_(x)with NH_(3)(NH_(3)-SCR).SnO_(2)-based materials possess superior hydrothermal stability,which is attractive for the development of NH_(3)-SCR *** this work,a series of Ce-Nb/SnO_(2)catalysts,with Ce and Nb loading on SnO_(2)support,were prepared by impregnation *** was found that,the NH_(3)-SCR activities and hydrothermal stabilities of the Ce-Nb/SnO_(2)catalysts significantly varied with the impregnation sequences,and the Ce-Nb(f)/SnO_(2) catalyst that firstly impregnated Nb and then impregnated Ce exhibited the best *** characterization results revealed that CeNb(f)/SnO_(2)possessed appropriate acidity and redox ***,the strong synergistic effect between Nb and Sn species stabilized the structure and maintained the dispersion of acid *** study may provide a new understanding for the effect of impregnation sequence on activity and hydrothermal stability and a new environmental-friendly NH_(3)-SCR catalyst with potential applications for NO_(x)removal from diesel and hydrogenfueled engines.

关键词： NO_(x)emission control NH_(3)-SCR Hydrothermal stability Ce-Nb/SnO_(2)catalyst Impregnation sequence