- A Simple Synthesis of the Ripening Agent 1-Aminocyclopropane-1-carboxylic Acid
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Conversion of chelated homoserine to 2-amino-4-bromobutyrate and treatment with aqueous base leads directly to chelated 1-aminocyclopropane-1-carboxylate.
- Angus, Patricia M.,Golding, Bernard T.,Sargeson, Alan M.
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- PRODUCTION METHOD FOR 1-AMINO CYCLOPROPANE CARBOXYLIC ACID NONHYDRATE
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1-Aminocyclopropanecarboxylic acid non-hydrate can be obtained by treating 1-aminocyclopropanecarboxylic acid hydrochloride with a tertiary amine in the presence of a C3-C4 alcohol and water, keeping the reaction mixture at 50° C. or below, collecting the precipitated crystal of 1-aminocyclopropanecarboxylic acid 0.5 hydrate by filtration, and contacting the obtained crystal with a C1-C2 alcohol.
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Paragraph 0053
(2021/05/14)
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- PRODUCTION METHOD FOR 1-AMINO CYCLOPROPANE CARBOXYLIC ACID NONHYDRATE
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1-Aminocyclopropanecarboxylic acid non-hydrate can be obtained by treating 1-aminocyclopropanecarboxylic acid hydrochloride with a tertiary amine in the presence of a C3-C4 alcohol and water, keeping the reaction mixture at 50° C. or below, collecting the precipitated crystal of 1-aminocyclopropanecarboxylic acid 0.5 hydrate by filtration, and heating the obtained crystal to 80 to 245° C.
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Paragraph 0046-0047
(2020/04/10)
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- Synthesis of the First Representatives of Spiro-1λ6-isothiazolidine-1,1,4-triones
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A strategy for the construction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones through the sulfonylation of 1-aminocyclopropane- and 1-aminocyclobutanecarboxylates with methanesulfonyl chloride followed by alkylation with methyl iodide and subsequent cyclization in the presence of potassium tert-butoxide in N,N-dimethylformamide is reported. An efficient synthesis of starting 1-aminocyclopropane- and 1-aminocyclobutanecarboxylic acids was developed. The reaction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones with N,N-dimethylformamide dimethyl acetal (DMF-DMA) gives 5′-[(Z)-(dimethylamino)methylene]spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones, the structure of which was confirmed by X-ray diffraction study.
- Dobrydnev, Alexey V.,Popova, Maria V.,Saffon-Merceron, Nathalie,Listunov, Dymytrii,Volovenko, Yulian M.
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p. 2523 - 2528
(2015/09/01)
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- NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
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Paragraph 0086; 0087
(2015/05/06)
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- NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
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Paragraph 0455-0457
(2015/08/04)
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- Synthesis of 2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazoles via the cyclopropyliminium rearrangement of substituted 2-cyclopropylbenzimidazoles
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2-Cyclopropylbenzimidazole derivatives with various substituents in the small ring undergo cyclopropyliminium rearrangement into 2,3- dihydropyrrolobenzimidazoles substituted at positions 1, 2 or 3. The substrates containing a functional group in position 1 of the cyclopropane ring form products substituted at position 3. Substituents at position 2 in most cases lead to the formation of a mixture of isomers. The reaction can be directed to yield one of the isomers predominantly by varying the solvent polarity.
- Salikov, Rinat F.,Platonov, Dmitry N.,Frumkin, Aleksandr E.,Lipilin, Dmitry L.,Tomilov, Yury V.
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supporting information
p. 3495 - 3505
(2013/04/23)
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- ALPHA KETOAMIDE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 69
(2010/11/24)
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- Hydrolysis of cyclopropane derivatives of aspartic and adipic acids
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Hydrolysis of substituted cyclopropane amino acids was performed. Free and partially substituted Z and E isomers of cyclopropane analogs of aspartic and adipic acids were obtained.
- Anisimova,Berkova,Deiko
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- New efficient synthesis of 1-aminocyclopropanecarboxylic acid (ACC)
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A new efficient synthesis of 1-aminocyclopropanecarboxylic acid (ACC) from methyl 2-diphenylmethyleneaminoacrylate in nearly quantitatie yield has been deeloped. The key step in the synthesis is the remoal of both protecting groups in mild conditions and
- Cativiela,Diaz-de-Villegas,Jimenez
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p. 2955 - 2963
(2007/10/02)
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- A New and Convenient Preparation of 1-Aminocyclopropanecarboxylic Acid from Acrolein
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Cyclopropanecarboxylic acid 3 and cyclopropanone hemiacetal 4 have been tested as possible convenient precursors of the α-aminocyclopropanecarboxylic acid (1), an immediate biosynthetic source of ethylene, the phytohormone which regulates plant growth.While acid 3 was aminated only in low yield and hemiacetal 4 did not submit to the Strecker synthesis, the benzophenone imine of 2-amino-4-chlorobutyronitrile 5, readily available from acrolein, did undergo quantitative base-induced cyclization smoothly under various conditions.
- Salauen, Jacques,Marguerite, Jacqueline,Karkour, Belkacem
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p. 4276 - 4281
(2007/10/02)
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- Decarboxylation of 1-Aminocyclopropanecarboxylic Acid and Its Derivatives
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The question of whether the title compounds could be decarboxylated to cyclopropanone derivatives was answered in the affirmative by the following observations. (1) Compound 11a was decarboxylated by 1,2,3-indantrione in acetonitrile, benzene, or methanol.The initially formed intermediate could be trapped by N-phenylmaleimide (to form 3), by diethyl azodicarboxylate (to form an unstable adduct), by ninhydrin itself (to form 5) or by a proton (in methanol, to form 8). (2) Compound 11d was decarboxylated by phenylbis(trifluoroacetato-O)iodine to yield carbinolamine 12d.cis-2,3-Dideuterio-11d yielded cis-2,3-dideuterio-12d under the same conditions. (3) ACC was decarboxylated by phenanthroquinone to yield oxazole 9, probably by way of oxazoline 10.
- Vaidyanathan, Ganesan,Wilson, Joseph W.
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p. 1810 - 1815
(2007/10/02)
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- Method and compositions for regulating plant growth using cycloalkane-carboxylic acid compounds
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Novel plant growth regulant composition comprising as an active ingredient at least one cycloalkanecarboxylic acid compound of the formula STR1 in which R is hydroxyl, alkoxy, aralkoxy, amino, alkylamino, dialkylamino or the radical wherein M≈
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- Synergistic compositions for inhibiting plant growth
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A plant growth-inhibiting composition comprising STR1 wherein the various radicals are as defined.
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