- SUBSTITUTED DIHYDROPYRROLOPYRAZOLE COMPOUND
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Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.
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Paragraph 0869-0871
(2017/09/12)
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- Synthesis method of O-methyl-D-serine
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The invention discloses a synthesis method of O-methyl-D-serine. The synthesis method includes the following steps that 1, acrylic acid methyl ester is added into a reaction bottle, after the temperature is raised, bromine is dropwise added, after an addition reaction is conducted, decompression and distillation are conducted to remove excessive bromine, methyl alcohol is added to residues, after the temperature is lowered, sodium methylate is added, after an alcoholysis reaction, decompression and distillation are conducted to remove methyl alcohol, ammonium hydroxide is added, after an ammonium hydroxide, concentrated crystallization is conducted, and O-methyl-DL-serine is obtained; 2, acetic acid is added into the reaction bottle, the O-methyl-DL-serine, D-tartaric acid and salicylaldehyde are added in sequence, after the temperature is raised for a reaction, cooling and crystallization are conducted, separation is conducted, and O-methyl-D-serine double salt is obtained; 3, the O-methyl-D-serine double salt is dissolved in a methyl alcohol aqueous solution, ammonium hydroxide is added to regulate PH to be 7-8, crystallization and separation are conducted, and the O-methyl-D-serine is obtained. The synthesis method is mild in reaction temperature, safe to operate, low in cost and high in chirality purity, and raw materials are easy to obtain.
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Paragraph 0041
(2017/01/02)
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- NEW PROCESS
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There is provided a process for the preparation of Lacosamide in a particular polymorphic form, which process involves the isolation of a salt of formula I : according to the methods defined in the application.
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Page/Page column 38
(2014/05/24)
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- N-Substituted amino acid N′-benzylamides: Synthesis, anticonvulsant, and metabolic activities
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Amino acid amides (AAA) were prepared and evaluated in seizure models. The AAA displayed moderate-to-excellent activity in the maximal electroshock seizure (MES) test and were devoid of activity in the subcutaneous Metrazol-induced (scMet) seizure test. The AAA anticonvulsant activity was neither strongly influenced by the C(2) substituent nor by the degree of terminal amine substitution. An in vitro metabolism study suggested that the structure-activity relationship pattern was due, in part, to metabolic processes that occurred at the N-terminal amine unit.
- Beguin, Cecile,LeTiran, Arnaud,Stables, James P.,Voyksner, Robert D.,Kohn, Harold
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p. 3079 - 3096
(2007/10/03)
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- QUINOLIN-, ISOQUINOLIN-, AND QUINAZOLIN-OXYALKYLAMIDES AND THEIR USE AS FUNGICIDES
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Fungicidal compounds of the general formula (1) wherein one of X and Y is N or N-oxide and the other is CR or both of X and Y are N.
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- N-ALKYNYL-2- (SUBSTITUTED PHENOXY) ALKYLAMIDES AND THEIR USE AS FUNGICIDES
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Fungicidal compounds of the general formula (1) wherein X, Y, Z, R1, R2, R3, R4 and R5 have the definitions given in claim 1.
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- N-ALKYNYL-2-HETEROARYLOXYALKYLAMIDES FOR USE AS FUNGICIDES
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Compounds of the general formula (I) are useful as fungicides wherein Het is a 5- or 6- linked group of the formula (a) or (b), and the variables are as defined in the claims.
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- Structure-Function Relationship of Acyl Amino Acid Surfactants: Surface Activity and Antimicrobial Properties
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Amino acid surfactants (AAS), having the general structure α-amino-(N-acyl)-β-alkoxypropionate, were synthesized chemically.Surface activity and antimicrobial properties of the AAS were evaluated.Increases in acyl chain length (i.e., C10-C14) resulted in a linear reduction in surface tension (i.e., 43-36 mN*m-1), as well as dramatic decreases in critical micelle concentrations (cmc) (i.e., 17.9-0.43 mM).Strong correlations existed between the cmc of AAS and their minimal inhibitory concentrations (mic) against Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger, and Saccharomyces cerevisiae.Sensitivity of the microorganisms to the various AAS followed the order Staphylococcus aureus > A. niger= S. cerevisiae> E. coli> P. aeruginosa.In comparison with methyl p-hydroxybenzoate, AAS (MN14) showed 2-8, 64, and 4-8 times the activity against Gram-negative bacteria, Gram-positive bacteria, and fungi, respectively.Surface adsorption and/or bifunctional binding to the cell membrane may account for AAS action on microorganisms.
- Xia, Jiding,Xia, Yongmei,Nnanna, Ifendu A.
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p. 867 - 871
(2007/10/02)
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- AMINO ACIDS; 13. INVESTIGATIONS ON THE SYNTHESIS OF DL-SERINE FROM α-HALOACRYLIC ACID DERIVATIVES
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The alkoxide-catalyzed addition of alcohols 2 to α-chloroacrylonitrile (1) at -35 degC gives rise to 3-alkoxy-2-chloropropanenitriles 3; at 0-5 degC with excess 2 alkyl 3-alkoxy-2-chloropropanimidates 4 are obtained.The yields of 3 or 4 decrease with increasing pKa values of the alcohols 2.In the basecatalyzed addition of phenols 5 to 1, a temperature-dependent addition equilibrium is set up in which the position of equilibrium is shifted in favour of the addition products 6 with increasing pKa values of 5.The 3-alkoxy-2-chloropropanoates 8, which are readily accessible by hydrolysis of 4, react smoothly with sodium azide in the presence of a phase transfer catalyst to furnish the 3-alkoxy-2-azidopropanoates 10.Starting from benzyl 2-azido-3-benzyloxy-propanoate (10b), the specific syntheses of DL-serine (14), DL-serine hydrochloride (14*HCl), DL-serine methyl ester hydrochloride (13a*HCl), O-benzyl-DL-serine (12b), and O-benzyl-DL-serine benzyl ester hydrochloride (11b*HCl) are possible by variation of the hydrogenation conditions.
- Effenberger, Franz,Zoller, Gerhard
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p. 5573 - 5582
(2007/10/02)
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- Reactions de cyclopropanation par double addition de Michael.
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The addition of nucleophiles to alkyl α bromoacrylates in aprotic media leads to the stereospecific formation of cylopropanes by a double Michael addition reaction.
- Joucla, Marc,Fouchet, Bernard,le Brun, Jacques,Hamelin, Jack
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p. 1221 - 1224
(2007/10/02)
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- Herbicidal 4-((benzimidazol-1-yl)phenoxy)alkanoic acids, esters and salts
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Certain 4-((benzimidazol-1-yl)phenoxy)alkanoic acids, esters and salts, useful as herbicides.
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- Boron Trifluoride Promoted Reaction of Alkyl Hypohalites with Alkenes. A New Synthesis of Fluoro Halides
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The reactions of the following alkenes with alkyl hypohalites and boron trifluoride (BF3) were investigated: cyclohexene (3), 1-hexene (8), trans-1,2-dichloroethylene (15), methyl acrylate (18), methyl crotonate (25), methyl isocrotonate (29), butadiene (33), methyl vinyl ketone (42), and styrene (45).Reactions of these alkenes with methyl hypochlorite (1) and BF3 in dichloromethane give fluoro chloride adducts as well as methoxy chlorides with the percentage of fluoro chlorides varying from 75percent for 29 to 8percent for 45.Fluoro bromide adducts are obtained with methyl hypobromite (2).Reactions with the tert-butyl hypohalites and BF3 also give fluoride incorporation.The percentage of fluoride incorporation with 1 or 2 is significantly greater in carbon tetrachloride than in dichloromethane.
- Heasley, Victor L.,Gipe, Robert K.,Martin, Jody L.,Wiese, Harry C.,Oakes, Melanie L.,Shellhamer, Dale F.
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p. 3195 - 3199
(2007/10/02)
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