- Preparation method of diacid
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The invention relates to a preparation method of diacid, and belongs to the field of medicinal chemistry. The preparation method provided by the invention comprises: carrying out carboxylation reaction on raw materials under the action of acid under a continuous flow reaction condition. The method provided by the invention has the advantages of cheap and easily available raw materials, simple process, low cost, high product purity and yield, green and environment-friendly process, and facilitation of industrialization.
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Paragraph 0006; 0032; 0034-0040; 0045-0050
(2021/05/12)
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- Method for synthesizing 2 -propyl imidazole -4 and 5 - dicarboxylic acid (by machine translation)
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The invention provides 2 -propyl imidazole -4 and 5 - dicarboxylic acid synthesis method which uses sodium tungstate and oxidant hydrogen peroxide to synthesize 2 -propylimidazole 2 - and -4 dicarboxylic acid, and the HPLC content of the product is 5 - and the HPLC content of 2 -propylimidazole -4 and 5 - dicarboxylic acid is lower than 99.2percent, namely -4-propyl imidazole 5 - and 0.5percent dicarboxylic acid in a yield of 2 - The present invention provides a method for synthesizing the dicarboxylic acid by co-oxidizing -4-propyl 5 - imidazole with oxidant hydrogen peroxide in PH 85.5percent (by machine translation)
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Paragraph 0020; 0033-0063
(2020/08/09)
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- Influence of Oxidation Conditions on the Yield of 2-Substituted Imidazole-4,5-dicarboxylic Acids
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Conditions were found which allow 2-alkyl-substituted imidazole-4,5-dicarboxylic acids to be synthesized in preparative quantities by the oxidation of 2-alkylbenzimidazoles with hydrogen peroxide. It was shown that optimal results can be obtained at the concentration of 2-alkylimidazole in sulfuric acid of 1 M and the hydrogen peroxide: 2-alkylbenzimidazole molar ratio of 11: 1. Oxidation under these conditions results in higher yields of the target 2-alkylimidazole-4,5-dicarboxylic acids, including those with a branched alkyl group.
- Brusina,Gubina, Yu. A.,Nikolaev,Ramsh,Piotrovskii
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p. 874 - 878
(2018/07/06)
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- A class of 4, 5 - disubstituted imidazole derivatives and its preparation and use (by machine translation)
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The invention relates to a compound of general formula I indicated by the 4, 5 - disubstituted imidazole compound, or its pharmaceutically acceptable salt, pharmaceutical composition containing the same and its preparation and use, the compounds can be used as a xanthine oxidase (Xanthine oxidase, XO) inhibitor, used for the treatment of uric acid crystallization at the joints to the deposition of Gout and its complications. (by machine translation)
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Paragraph 0187-0189
(2017/07/22)
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- Olmesartan high purity intermediate 2-propyl imidazole -4,5-dicarboxylic acid preparation method and application
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The invention provides a preparation method of 2-propylimidazolyl-4,5-dicarboxylic acid (1). According to the method, the concentration of the sulfuric acid solution, the volume/mass ratio of the sulfuric acid solution to 2-propyl benzimidazole, the volume ratio of the oxydol to the sulfuric acid water solution, reaction time, added water volume and cooling recrystallization temperature are accurately controlled to obviously lower the content of the impurity imidazolyl-4,5-dicarboxylic acid (8), thereby further obtaining the high-purity olmesartan medoxomil. The invention also provides a compound disclosed as Formula 9 and application thereof in olmesartan medoxomil preparation as a control quality standard substance.
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Paragraph 0086-0089
(2017/02/28)
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- 2-aminoalkylimidazole -4, 5-dicarboxilic manufacturing method
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PROBLEM TO BE SOLVED: To provide a method for producing inexpensively with a high yield, 2-alkylimidazole-4,5-dicarboxylic acid which is useful as a medicinal intermediate. SOLUTION: In this method for producing 2-alkylimidazole-4,5-dicarboxylic acid, tartaric acid is dissolved into nitric acid and then reacted with concentrated sulfuric acid, and a nitrate of tartaric acid acquired by the reaction is added into a solvent containing at least one kind of organic solvent selected from among N-methyl-2-pyrrolidone, dimethylformamide, dimethylacetamide, methylcyclohexane and toluene. Thereafter, a mixed liquid of aldehyde and ammonia is added to the reaction liquid, to thereby produce 2-alkylimidazole-4,5-dicarboxylic acid. COPYRIGHT: (C)2012,JPOandINPIT
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Paragraph 0087; 0088
(2016/12/12)
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- PROCESS FOR (5-METHYL-2-OXO-1,3-DIOXOLEN-4-YL)METHYL4-(1-HYDROXY-1-METHYLETHYL)-2-PROPYL-1-[4-[2-TETRAZOL-5-YL)PHENYL]PHENYL]METHYLIMIDAZOLE-5-CARBOXYLATE
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The present invention relates to an improved process for the preparation of (5-methyl-2-oxo- 1,3-dioxolen-4-yl)methyl4-(1-hydroxy- 1-methylethyl)-2-propyl-1-[4-[2-(tetrazol-5-yl)phenyl]phenyl]methyl imidazole-5-carboxylate.
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Page/Page column 18
(2011/04/13)
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- Efficient synthesis of olmesartan medoxomil, an antihypertensive drug
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This document describes a simple and robust process for the synthesis of olmesartan medoxomil. This tailored process allows us to synthesize olmesartan medoxomil on a large scale with 50% overall yield. Also, our process has excellent control of the impurity profile in all the stages. Copyright Taylor & Francis Group, LLC.
- Babu, Karrothu Srihari,Reddy, Mallepalli Srinivasa,Tagore, Amirisetty Ravindranath,Reddy, Gade Srinivas,Sebastian, Sony,Varma, Mudunuru Satish,Venkateswarlu, Gandu,Bhattacharya, Apurba,Reddy, Padi Pratap,Anand, Ramasamy Vijaya
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experimental part
p. 291 - 298
(2009/05/07)
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- ANGIOTENSIN II ANTAGONIST 1-BIPHENYLMETHYLIMIDAZOLE COMPOUNDS AND THEIR THERAPEUTIC USE
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Compounds of the following formula (I) or the formula (I) p : STR1 wherein R 1 is alkyl or alkenyl; R 2 and R 3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R 4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula--SiR a R b R c, in which R a, R b and R c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R 5 is carboxy or--CONR 8 R 9, wherein R 8 and R 9 hydrogens or alkyl, or R 8 and R 9 together form alkylene; R 6 is hydrogen, alkyl, alkoxy or halogen; R. sup.7 is carboxy or tetrazol-5-yl; R p. sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R p 2 is a single bond, alkylene or alkylidene; R p 3 and R p 4 are each hydrogen or alkyl; R. sub.p 6 is carboxy or tetrazol-5-yl; and X p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.
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- Nonpeptide angiotensin II receptor antagonists: Synthesis, biological activities, and structure - Activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds
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A series of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds were prepared and evaluated for their antagonistic activities to the angiotensin II (AII) receptor. Among them, the 4-(1-hydroxyalkyl)-imidazole derivatives had strong binding affinity to the AII receptor and potently inhibited the AII-induced pressor response by intravenous administration. Various esters of these acids showed potent and long-lasting antagonistic activity by oral administration. The most promising compounds were (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (CS-866) and (pivaloyloxy)-methyl esters of 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[(2′-1H-tetrazol-5-ylbiphenyl-4-yl) -methyl]imidazole-5-carboxylic acid (26c). A study involving stereochemical comparison of 26c with the acetylated C-terminal pentapeptide of AII was also undertaken.
- Yanagisawa, Hiroaki,Amemiya, Yoshiya,Kanazaki, Takuro,Shimoji, Yasuo,Fujimoto, Koichi,Kitahara, Yoshiko,Sada, Toshio,Mizuno, Makoto,Ikeda, Masahiro,Miyamoto, Shuichi,Furukawa, Youji,Koike, Hiroyuki
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p. 323 - 338
(2007/10/03)
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