- 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; 0032-0033; 0041-0044
(2021/05/12)
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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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- Efficient synthesis of trisimidazole and glutaric acid bearing porphyrins: Ligands for active-site models of bacterial nitric oxide reductase
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Ligands (1) for active-site models of bacterial nitric oxide reductase (NOR) have been efficiently synthesized. These compounds (1) feature three imidazolyl moieties and one carboxylic acid residue at the FeB site, which represent the closest available synthetic model ligands of NOR active center. The stereo conformations of these ligands are established on the basis of steric effects and 1H NMR chemical shifts under the ring current effect of the porphyrin.
- Collman, James P.,Yan, Yi-Long,Lei, Jianping,Dinolfo, Peter H.
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p. 923 - 926
(2007/10/03)
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- Synthesis of 4,5-dicyanoimidazoles
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The effective procedure of preparation of 2-trifluoromethyl-4,5- dicyanoimidazole (3a) from diaminomaleonitrile (1) and trifluoroacetic anhydride has been elaborated. The syntheses of five other 2-substituted imidazoles from appropriate acyl derivatives of 1 have been attempted. Out of them only 4,5-dicyanoimidazole (3b) could be obtained in good yield.
- Bukowska,Prejzner,Szczecinski
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p. 417 - 422
(2007/10/03)
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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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