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1.
Accid Anal Prev ; 203: 107617, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38772193

ABSTRACT

The rapid detection of internal rail defects is critical to maintaining railway safety, but this task faces a significant challenge due to the limited computational resources of onboard detection systems. This paper presents YOLOv8n-LiteCBAM, an advanced network designed to enhance the efficiency of rail defect detection. The network designs a lightweight DepthStackNet backbone to replace the existing CSPDarkNet backbone. Further optimization is achieved through model pruning techniques and the incorporation of a novel Bidirectional Convolutional Block Attention Module (BiCBAM). Additionally, inference acceleration is realized via ONNX Runtime. Experimental results on the rail defect dataset demonstrate that our model achieves 92.9% mAP with inference speeds of 136.79 FPS on the GPU and 38.36 FPS on the CPU. The model's inference speed outperforms that of other lightweight models and ensures that it meets the real-time detection requirements of Rail Flaw Detection (RFD) vehicles traveling at 80 km/h. Consequently, the YOLOv8n-LiteCBAM network is with some potential for industrial application in the expedited detection of internal rail defects.


Subject(s)
Railroads , Safety , Humans , Neural Networks, Computer , Algorithms
2.
Accid Anal Prev ; 192: 107267, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37708831

ABSTRACT

Safety is paramount in rail transportation. The International Safety Standard IEC 61508, issued by the International Electrotechnical Commission (IEC) in 2000, describes the modern concept of safety and the specifications for safety evaluation in a systematic manner. On this basis, the EN 50129 railway transportation safety standard and safety integrity level(SIL) are established. Through the above analysis, the relationship between safety-related system reliability, acceptable risk, and safety index is summarized. It is clear that the safety index is based on acceptable risks. Nonetheless, as the economy and society advance, the safety index mandated by the SIL falls behind. Consequently, the principles and methodologies for calculating the safety index are presented. The paper proposes a reference for the Chinese railway safety index based on actual data from the Chinese railways over the past few years.


Subject(s)
Accidents, Traffic , Transportation , Humans , Reproducibility of Results
3.
Accid Anal Prev ; 175: 106764, 2022 Sep.
Article in English | MEDLINE | ID: mdl-35878468

ABSTRACT

Safety is the precondition and guarantee of railway development. However, due to equipment failure, poor management, misoperation and so on, accidents on the railway occur from time to time. China and Japan, as leading countries in Railway Technology in the world, have done a lot of work in accident prevention and safety. Through the collection and comparison of transport data and typical casualty cases in China and Japan, this paper summarizes the main causes of accidents and the experience of accident prevention in the two countries. And further, puts forward suggestions for preventing accidents and large-scale casualty.


Subject(s)
Railroads , Accident Prevention , Accidents , Accidents, Traffic/prevention & control , China/epidemiology , Humans , Japan
4.
Accid Anal Prev ; 166: 106549, 2022 Mar.
Article in English | MEDLINE | ID: mdl-34974208

ABSTRACT

As the passage for passengers to get on and off, train plug doors directly affect the operation efficiency of the train and the personal safety of passengers. This paper proposes a non-contact fault diagnosis method for train plug doors based on sound signals. First, empirical mode decomposition (EMD) is utilized to process the raw sound signals. A signal reconstruction method by selecting intrinsic mode functions (IMFs) using hybrid selection criteria is then proposed. Second, novel feature named weighted fractional wavelet packet decomposition energy entropy (WFWPDE) is developed by introducing the idea of fractional calculus and weight to wavelet packet decomposition energy entropy (WDPE). Third, a synchronous optimization strategy is proposed to optimize the weights and hyperparameters of support vector machine (SVM) synchronously. Finally, the superiority and feasibility of the proposed method are verified on field-collected data. By comparing with different fault diagnosis methods, the proposed method performs best on fault diagnosis of train plug doors, with accuracy of 97.87%.


Subject(s)
Algorithms , Signal Processing, Computer-Assisted , Accidents, Traffic , Entropy , Humans , Support Vector Machine
5.
Proc Natl Acad Sci U S A ; 118(41)2021 10 12.
Article in English | MEDLINE | ID: mdl-34607951

ABSTRACT

Cancer therapy reduces tumor burden via tumor cell death ("debris"), which can accelerate tumor progression via the failure of inflammation resolution. Thus, there is an urgent need to develop treatment modalities that stimulate the clearance or resolution of inflammation-associated debris. Here, we demonstrate that chemotherapy-generated debris stimulates metastasis by up-regulating soluble epoxide hydrolase (sEH) and the prostaglandin E2 receptor 4 (EP4). Therapy-induced tumor cell debris triggers a storm of proinflammatory and proangiogenic eicosanoid-driven cytokines. Thus, targeting a single eicosanoid or cytokine is unlikely to prevent chemotherapy-induced metastasis. Pharmacological abrogation of both sEH and EP4 eicosanoid pathways prevents hepato-pancreatic tumor growth and liver metastasis by promoting macrophage phagocytosis of debris and counterregulating a protumorigenic eicosanoid and cytokine storm. Therefore, stimulating the clearance of tumor cell debris via combined sEH and EP4 inhibition is an approach to prevent debris-stimulated metastasis and tumor growth.


Subject(s)
Eicosanoids/metabolism , Epoxide Hydrolases/biosynthesis , Macrophages/immunology , Neoplasm Metastasis/pathology , Receptors, Prostaglandin E, EP4 Subtype/biosynthesis , Animals , Antineoplastic Agents/adverse effects , Antineoplastic Agents/therapeutic use , Carcinoma, Hepatocellular/pathology , Cell Death/drug effects , Cell Line, Tumor , Cytokine Release Syndrome/immunology , Cytokine Release Syndrome/prevention & control , Cytokines/metabolism , Hep G2 Cells , Humans , Liver Neoplasms/drug therapy , Liver Neoplasms/pathology , Male , Mice , Mice, Inbred C57BL , Neoplasm Metastasis/prevention & control , Pancreatic Neoplasms/drug therapy , Pancreatic Neoplasms/pathology , Phagocytosis/immunology , RAW 264.7 Cells
7.
Sensors (Basel) ; 19(1)2018 Dec 20.
Article in English | MEDLINE | ID: mdl-30577450

ABSTRACT

As the only entry/exit for passengers getting on and off a train, the train plug door is of great importance to keep train operation safe and reliable. As signal processing technologies develop rapidly, taking the easy acquisition advantages of sound signals, a novel fault diagnosis method for train plug doors using multi-scale normalized permutation entropy (MNPE) and an improved particle swarm optimization based multi-class support vector machine (IPSO-MSVM) is proposed. Firstly, sound samples are collected using high-precision audio sensor. In the features extraction process, a hybrid method blending empirical mode decomposition (EMD), multi-scale permutation entropy (MNPE) with Fisher discrimination criterion is utilized. First, EMD is used to decompose each sound signal into several intrinsic mode functions (IMFs) and a residue for stationary processing. Then, MNPE features are extracted from the IMFs. To obtain the most significant features, the Fisher discrimination criterion is further applied. To address the time-consuming defects of traditional grid based method for selecting the optimal parameters of multi-class SVM, an improved PSO (IPSO) is proposed. The superiority of the IPSO-MSVM model and the hybrid feature extraction method was tested on the collected sound samples by comparing to commonly applied methods. Results indicate the identification accuracy of the proposed method is highest, which reaches 90.54%, demonstrating its feasibility.

8.
ISA Trans ; 73: 201-207, 2018 Feb.
Article in English | MEDLINE | ID: mdl-29287610

ABSTRACT

Chattering alarms are the most found nuisance alarms that will probably reduce the usability and result in a confidence crisis of alarm systems for industrial plants. This paper addresses the chattering alarm reduction using median filters. Two rules are formulated to design the window size of median filters. If the alarm probability is estimated using process data, one rule is based on the probability of alarms to satisfy some requirements on the false alarm rate, or missed alarm rate. If there are only historical alarm data available, the other rule is based on percentage reduction of chattering alarms using alarm duration distribution. Experimental results for industrial cases testify that the proposed method is effective.

9.
Org Lett ; 12(18): 4201-3, 2010 Sep 17.
Article in English | MEDLINE | ID: mdl-20735080

ABSTRACT

A general method for the enantioselective hydrogenation of protected allylic amine derivatives is described. This procedure relies on the generation of a cationic ruthenium complex with the axially chiral ligand (-)-TMBTP. The utility is highlighted by the highly enantioselective hydrogenation of a diene substrate that can then be elaborated to prepare Telcagepant, a compound currently in Phase III clinical trials. The scope of the hydrogenation reaction was studied, and a variety of substituted allylic amine derivatives could be hydrogenated with enantiomeric ratios of 92:8 or higher.


Subject(s)
Allyl Compounds/chemistry , Amines/chemistry , Azepines/chemical synthesis , Caprolactam/chemical synthesis , Catalysis , Hydrogenation , Imidazoles/chemical synthesis , Molecular Structure , Stereoisomerism
10.
J Am Chem Soc ; 132(7): 2124-5, 2010 Feb 24.
Article in English | MEDLINE | ID: mdl-20104899

ABSTRACT

Homogeneous asymmetric hydrogenation of unprotected benzophenone N-H imines 1a-r using Ir-(S)-N-benzyl-N-methyl-MonoPhos as a catalyst provides chiral amines 2a-r in 80-96% yield with enantioselectivities up to 98% ee (18 examples) for ortho-substituted substrates.


Subject(s)
Amines/chemical synthesis , Benzophenones/chemistry , Imines/chemistry , Catalysis , Hydrogenation , Iridium/chemistry , Ligands , Organometallic Compounds/chemistry , Organophosphorus Compounds/chemistry , Stereoisomerism
11.
J Am Chem Soc ; 131(29): 9882-3, 2009 Jul 29.
Article in English | MEDLINE | ID: mdl-19569686

ABSTRACT

N-H ketoimines 3a-3v are readily prepared in high yield via organometallic addition to nitriles and isolated as corresponding bench-stable hydrochloride salts. Homogeneous asymmetric hydrogenation of unprotected N-H ketoimines 3a-3v using Ir-(S,S)-f-binaphane as catalyst provides chiral amines 4a-4v in 90-95% yield with enantioselectivities up to 95% ee.


Subject(s)
Imines/chemical synthesis , Hydrogenation , Imines/chemistry , Stereoisomerism
12.
J Am Chem Soc ; 131(32): 11316-7, 2009 Aug 19.
Article in English | MEDLINE | ID: mdl-19637921

ABSTRACT

Asymmetric reductive amination of beta-keto amides catalyzed by the chiral catalyst Ru(OAc)(2)((R)-dm-segphos) produces unprotected beta-amino amides with high yields and high enantioselectivities (94.7-99.5% ee). This "one-pot" methodology is general in substrate scope and has been successfully employed to produce sitagliptin with 99.5% ee and 91% assay yield. The excellent reaction efficiency is attributed to the remarkable tolerance to high concentrations of ammonium ion, the high chemoselectivity, and the high enantioselectivity (99.5% ee) of the Ru catalyst system.


Subject(s)
Amides/chemistry , Ruthenium Compounds/chemistry , Amination , Catalysis , Molecular Structure , Oxidation-Reduction , Stereoisomerism
13.
J Am Chem Soc ; 131(25): 8798-804, 2009 Jul 01.
Article in English | MEDLINE | ID: mdl-19507853

ABSTRACT

A highly efficient synthesis of sitagliptin, a potent and selective DPP-4 inhibitor for the treatment of type 2 diabetes mellitus (T2DM), has been developed. The key dehydrositagliptin intermediate 9 is prepared in three steps in one pot and directly isolated in 82% yield and >99.6 wt % purity. Highly enantioselective hydrogenation of dehydrositagliptin 9, with as low as 0.15 mol % of Rh(I)/(t)Bu JOSIPHOS, affords sitagliptin, which is finally isolated as its phosphate salt with nearly perfect optical and chemical purity. This environmentally friendly, 'green' synthesis significantly reduces the total waste generated per kilogram of sitagliptin produced in comparison with the first-generation route and completely eliminates aqueous waste streams. The efficiency of this cost-effective process, which has been implemented on manufacturing scale, results in up to 65% overall isolated yield.


Subject(s)
Dipeptidyl-Peptidase IV Inhibitors/chemical synthesis , Green Chemistry Technology/methods , Pyrazines/chemical synthesis , Triazoles/chemical synthesis , Green Chemistry Technology/economics , Hydrogenation , Sitagliptin Phosphate , Stereoisomerism
14.
Org Lett ; 11(2): 369-72, 2009 Jan 15.
Article in English | MEDLINE | ID: mdl-19099496

ABSTRACT

An efficient synthesis of HIV integrase inhibitor (S)-(-)-1 via a unique asymmetric hydrogenation of a mixture of imines/enamine 5a-5b/5c is described. Hydrogenation of the imines/enamine by a Rh(I)-Josiphos complex afforded 6 in 90% yield and 90% ee. Amide formation completed the synthesis of 1 in 58% overall yield from 2, which is readily available from 3,4-dihydro-2H-pyran in a seven-step sequence. A deuterium labeling study suggests the asymmetric hydrogenation proceeds predominantly via the enamine tautomer.


Subject(s)
HIV Integrase Inhibitors/chemical synthesis , HIV Integrase , Amines/chemistry , Catalysis , HIV Integrase Inhibitors/chemistry , Hydrogenation , Imines/chemistry , Stereoisomerism
15.
J Am Chem Soc ; 128(51): 17063-73, 2006 Dec 27.
Article in English | MEDLINE | ID: mdl-17177459

ABSTRACT

Ruthenium complexes employing axially chiral ligands were found to be effective asymmetric hydrogenation catalysts for the reduction of alpha,beta-unsaturated ene acid 1-E to give 2, a prostaglandin D2 (PGD2) receptor antagonist. With [(S-BINAP)Ru(p-cymene)Cl2]2 (3, S-BINAP = (S)-(+)-2,2'-bis(diphenylphospino)-1,1'-binapthyl), it was discovered that low hydrogen pressures (<30 psi) were essential to achieve high enantioselectivities (92% ee). A detailed mechanistic study was undertaken to elucidate this pressure dependence. It was determined that compound 1-E is in a ruthenium-catalyzed equilibrium with endocylic isomer 1-Endo and in photochemical equilibrium with Z isomer 1-Z. Each isomer could be hydrogenated to give 2, albeit with different rates and enantioselectivities. Hydrogenation of 1-Endo with 3 was found to give 2 in high enantiomeric excess, regardless of pressure and at a rate substantially faster than that of hydrogenation of 1-E and 1-Z. In contrast, isomers 1-E and 1-Z exhibited pressure-dependent enantioselectivities, with higher enantiomeric excesses obtained at lower pressures. A rationale for this pressure dependence is described. Deuterium labeling studies with 1-Endo and tiglic acid were used to elucidate the mechanism of hydride insertion and product release from ruthenium. Under neutral conditions, protonolysis was the major pathway for metal-carbon cleavage, while under basic conditions, hydrogenolysis of the metal-carbon bond was predominant.


Subject(s)
Carboxylic Acids/chemical synthesis , Carboxylic Acids/pharmacology , Receptors, Immunologic/antagonists & inhibitors , Receptors, Prostaglandin/antagonists & inhibitors , Alkenes/chemistry , Carboxylic Acids/chemistry , Deuterium/chemistry , Hydrogen/chemistry , Hydrogenation , Kinetics , Molecular Structure , Pressure , Stereoisomerism , Temperature
16.
Org Lett ; 8(22): 5161-4, 2006 Oct 26.
Article in English | MEDLINE | ID: mdl-17048868

ABSTRACT

Aryl carboxylic esters were synthesized by Pd-catalyzed carbonylation of aryl p-fluorobenzenesulfonates or -tosylates. A unique Josiphos ligand was discovered through high-throughput catalyst screening, which was the key for the successful carbonylation of various substrates. This catalyst is effective and works well for both electron-rich and electron-poor aryl arenesulfonates. Isolated yields of up to 90% were obtained for aryl p-fluorobenzenesulfonates and -tosylates. [reaction: see text]


Subject(s)
Arylsulfonates/chemistry , Hydrocarbons, Fluorinated/chemistry , Tosyl Compounds/chemistry , Catalysis , Combinatorial Chemistry Techniques , Esters , Molecular Structure , Palladium
17.
Org Lett ; 7(16): 3405-8, 2005 Aug 04.
Article in English | MEDLINE | ID: mdl-16048303

ABSTRACT

A novel and highly enantioselective Ru-catalyzed hydrogenation of N-sulfonylated-alpha-dehydroamino acids has been discovered and demonstrated in the synthesis of an anthrax lethal factor inhibitor (LFI). Herein, this methodology is used to prepare N-sulfonylated amino acids in up to 98% ee. This unprecedented hydrogenation uses a chiral Ru catalyst rather than Rh as typical for acylated dehydroamino acids and esters, and this work reports the first asymmetric hydrogenation of a tetrasubstituted dehydroamino acid derivative using a Ru catalyst. [reaction: see text]


Subject(s)
Amino Acids/chemical synthesis , Bacterial Toxins/antagonists & inhibitors , Ruthenium/chemistry , Amino Acids/chemistry , Amino Acids/pharmacology , Antigens, Bacterial , Bacillus anthracis/chemistry , Bacillus anthracis/pathogenicity , Catalysis , Hydrogenation , Stereoisomerism
18.
J Am Chem Soc ; 126(32): 9918-9, 2004 Aug 18.
Article in English | MEDLINE | ID: mdl-15303855

ABSTRACT

A direct asymmetric hydrogenation of unprotected enamino esters and amides is described. Catalyzed by Rh complexes with Josiphos-type chiral ligands, this method gives beta-amino esters and amides in high yield and high ee (93-97% ee). No acyl protection/deprotection is required.


Subject(s)
Amides/chemical synthesis , Amines/chemistry , Amino Acids/chemistry , Esters/chemical synthesis , Alkenes/chemistry , Catalysis , Hydrogenation , Stereoisomerism
19.
Proc Natl Acad Sci U S A ; 101(15): 5379-84, 2004 Apr 13.
Article in English | MEDLINE | ID: mdl-15056759

ABSTRACT

Enantiomerically enriched, deuterated branched carbonates (Z)-(S)-PhCH(OCO(2)Me)-CH = CHD (1-D), (Z)-(R)-PhCH(OCO(2)Me)CH = CHD (2-D), and linear carbonate (E)-(S)-PhCH = CHCHD(OCO(2)Me) (3-D) were used as probes in the Mo-catalyzed asymmetric allylic alkylation with sodium dimethyl malonate, catalyzed by ligand-complex 11 derived from the mixed benzamide/picolinamide of (S,S)-transdiaminocyclohexane and (norbornadiene)Mo(CO)(4). The results of these studies, along with x-ray crystallography and solution NMR structural analysis of the pi-allyl intermediate, conclusively established the reaction proceeded by a retention-retention pathway. This mechanism contrasts with that defined for Pd-catalyzed allylic alkylations, which proceed by an inversion-inversion pathway. A proposed rationale for the retention pathway for nucleophilic substitution involves CO-coordination to form a tri-CO intermediate, followed by complexation with the anion of dimethyl malonate to produce a seven-coordinate intermediate, which reductively eliminates to afford product with retention of configuration.

20.
J Am Chem Soc ; 126(10): 3048-9, 2004 Mar 17.
Article in English | MEDLINE | ID: mdl-15012124

ABSTRACT

Pure (Z)-enamines readily prepared from beta-ketoesters and amides using (S)-phenylglycine amide were hydrogenated with very high diastereoselectivities (up to 200:1) using heterogeneous catalysis. Hydrogenolytic cleavage of the (S)-phenylglycine amide afforded the corresponding chiral beta-aminoesters and amides. The high geometrical purity of the (Z)-enamine and a simple activation procedure for the PtO2 catalyst are essential in achieving high selectivity.


Subject(s)
Amines/chemistry , Amino Acids/chemistry , Amides/chemical synthesis , Amides/chemistry , Amino Acids/chemical synthesis , Catalysis , Crystallography, X-Ray , Deuterium , Esters/chemical synthesis , Esters/chemistry , Hydrogenation , Stereoisomerism
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