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  • 1
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1979 (1979), S. 1534-1546 
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis and Reactions of 4-Aminoisothiazolesα-(Tosyloximino)nitriles 2 react with the thiols 1 having an active methylene group in one or two steps via α-(alkylthioimino)nitriles 3 to yield the substituted 4-aminoisothiazoles 4. 4-Aminoisothiazoles unsubstituted at the 5-position are obtainable by decarboxylation; 4-aminoisothiazole-3-carboxylic acid (7) affords 4-(acetylamino)isothiazole (8). From 4 are synthesized the substituted isothiazolo[4,3-d]triazinones 9, the isothiazolo[4,3-d]pyrimidones and isothiazolo[4,5-d]pyrimidones 10, 11 and isothiazolo[4,5-b]pyridines 12
    Notes: α-(Tosyloximino)nitrile 2 reagieren mit den methylenaktiven Thiolen 1 in ein oder zwei Stufen über die α-(Alkylthioimino)nitrile 3 zu den substituierten 4-Aminoisothiazolen 4. 4-Amino-isothiazole mit freier 5-Stellung sind durch Decarboxylierung erhältlich; 4-(Acetylamino)isothiazol (8) entsteht aus 4-Aminoisothiazol-3-carbonsäure (7). Aus 4 werden die substituierten Isothiazolo[4,3-d]triazinone 9, Isothiazolo[4,3-d]pyrimidone und -[4,5-d]pyrimidone 10 bzw. 11, sowie Isothiazolo[4,5-b]pyridine 12 gewonnen.
    Additional Material: 1 Tab.
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  • 2
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1980 (1980), S. 1623-1629 
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: 4-Aminoisoxazoles by Thorpe CyclizationCyclization of α-(acylmethoxyimino)nitriles 1 in the presence of lithium hydroxide yields 5-acyl-4-aminoisoxazoles 2. Compounds 2f and 2a can be converted into the isoxazolo[4,3-d]pyrimidone 3 and the isoxazolo[4,5-b]pyridine 4.
    Notes: α-(Acylmethoxyimino)nitrile 1 cyclisieren in Gegenwart von Lithiumhydroxid zu 5-Acyl-4-amino-isoxazolen 2. Die Verbindungen 2f und 2a wurden zu Isoxazolo[4,3-d]pyrimidon 3 bzw. Isoxazolo[4,5-b]pyridin 4 umgesetzt.
    Additional Material: 2 Tab.
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  • 3
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1984 (1984), S. 1702-1710 
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis of 2-Acyl-3-aminofurans by Thorpe CyclizationThe substituted β-(acylmethoxy)acrylonitriles 2 and 11, obtainable by O-alkylation of β-cyanoketones with halomethyl ketones or by the reaction of α-hydroxymethyl ketones with β-chloro-α-cyanocinnamonitrile are cyclized in the presence of bases to yield 2-acyl-3-aminofurans 3 and 12. The phenacyl and acetonyl esters 5 and 8 of 2-(arylhydrazono)-2-cyanoacetic acid and 2-(anilinomethylene)-2-cyanoacetic acid, respectively, can be cyclized in the presence of triethylamine to form substituted 5-acyl-4-amino-2-furanones 6, 9.
    Notes: Die substituierten β-(Acylmethoxy)acrylnitrile 2 und 11, erhältlich durch O-Alkylierung von β-Cyanketonen mit Halogenmethylketonen oder von α-Hydroxymethylketonen mit β-Chlor-α-cyanzimtsäurenitril, cyclisieren basenkatalysiert zu 2-Acyl-3-aminofuranen 3 und 12. - Phenacyl- und Acetonylester 5 und 8 von 2-(Arylhydrazono)-2-cyanessigsäuren und der 2-(Anilinomethylen)-2-cyanessigsäure cyclisieren in Gegenwart von Triethylamin zu substituierten 5-Acyl-4-amino-2-furanonen 6, 9.
    Additional Material: 2 Tab.
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  • 4
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1995 (1995), S. 787-791 
    ISSN: 0947-3440
    Keywords: Pyridines ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: 2-[(Chloroacetyl)amino]acrylonitriles 1 and 3-[(chloroacetyl)-amino]propionitriles 4 were allowed to react with pyridine to form the 1-(4-amino-3-pyridyl)pyridinium salts 3 and 1-(4-amino-5,6-dihydro-3-pyridyl)pyridinium salts 6. Dehydrogenation of 6 with bromine in glacial acetic acid afforded 1-(4-amino-3-pyridyl)pyridinium bromides 7. Treatment of 3 and 7 with hydrazine hydrate yielded the 3,4-diamino-2(1H)-pyridinones 8. Analogously to other ortho-diamines, the substituted [1,2,5]thiadiazolo[3,4-c]pyridin-4-one 10, [1,2,5]selenadiazolo[3,4-c]pyridin-4-one 11, and further derivatives were obtained from 8. N-(Chloroacetyl) derivatives of acetylacetoneimide 13 and 3-oxo-3-phenyl-2-(phenylhydrazono)propionamide 17 were treated with pyridine to give 1-(3-pyridyl)-pyridinium salts 14 and 18, respectively.
    Additional Material: 2 Tab.
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  • 5
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 124 (1991), S. 1237-1241 
    ISSN: 0009-2940
    Keywords: Quinolin-2(1H)-ones ; 4-amino-3-pyridinio- ; Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: 4-Amino-3-pyridinioquinolin-2(1H)-one Chlorides and 3,4-Diaminoquinolin-2(1H)-onesN;-(Chloroacetyl)anthranilonitriles 1 react with the pyridines 2 to form the 4-amino-3-pyridinioquinolin-2(1H)-one chlorides 4, which are converted into the pyrido[1',2′ : 1,2]imidazo[5,4-c]- quinolin-6(5H)-ones 6 in the presence of sodium hydroxide or by cyclooxidation with bromine. Treatment of 4 with hydrazine hydrate yields the 3,4-diaminoquinolin-2(1H)-ones 9. Analogously to other o-diamines the substituted imidazo [4,5-c]- quinolinones 12, the pyrazino[2,3-c]quinolinones 13, 14, the 1,2,5-thiadiazolo[3,4-c]quinolin-4-one 15a and the 1,2,5-selena-diazolo[3,4-c]quinolin-4-one 15b are obtainable from 9a. With chloroacetyl chloride 9a provides the oxazino[2,3-b]quinolin-2-one 11.
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  • 6
    Publication Date: 2019-10-17
    Description: Standard feature engineering involves manually designing measurable descriptors based on some expert knowledge in the domain of application, followed by the selection of the best performing set of designed features for the subsequent optimisation of an inference model. Several studies have shown that this whole manual process can be efficiently replaced by deep learning approaches which are characterised by the integration of feature engineering, feature selection and inference model optimisation into a single learning process. In the following work, deep learning architectures are designed for the assessment of measurable physiological channels in order to perform an accurate classification of different levels of artificially induced nociceptive pain. In contrast to previous works, which rely on carefully designed sets of hand-crafted features, the current work aims at building competitive pain intensity inference models through autonomous feature learning, based on deep neural networks. The assessment of the designed deep learning architectures is based on the BioVid Heat Pain Database (Part A) and experimental validation demonstrates that the proposed uni-modal architecture for the electrodermal activity (EDA) and the deep fusion approaches significantly outperform previous methods reported in the literature, with respective average performances of 84.57 % and 84.40 % for the binary classification experiment consisting of the discrimination between the baseline and the pain tolerance level ( T 0 vs. T 4 ) in a Leave-One-Subject-Out (LOSO) cross-validation evaluation setting. Moreover, the experimental results clearly show the relevance of the proposed approaches, which also offer more flexibility in the case of transfer learning due to the modular nature of deep neural networks.
    Electronic ISSN: 1424-8220
    Topics: Chemistry and Pharmacology , Electrical Engineering, Measurement and Control Technology
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