214777-43-2Relevant articles and documents
Preparation technology for imidafenacin
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Paragraph 0014; 0015, (2016/11/24)
The invention discloses a preparation technology for imidafenacin and belongs to the pharmaceutical chemistry field. The method is as follows: 2-halogenated ethyl diphenylacetonitrile and 2-methyl imidazole are employed as initial raw materials, alcohol compounds are employed as a solvent, polyethylene glycol is employed as a phase-transfer catalyst, replacement and hydrolysis reactions are combined in an alkali metal hydroxide condition, and imidafenacin is prepared through one step. The technology is advantageous in that reaction steps are reduced, dosage of 2-methyl imidazole and the reaction temperature are lowered substantially, the reaction time is shortened, the synthesis yield is raised obviously, and the preparation technology is suitable for industrial production.
METHOD FOR PRODUCING 4-(2-METHYL-1-IMIDAZOLYL)-2,2-PHENYLBUTANE AMIDE
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Paragraph 0008; 0020; 0021, (2016/12/22)
PROBLEM TO BE SOLVED: To provide a method for industrially producing 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutane amide (imidafenacin), which is a selective muscarine receptor antagonist, in a high yield and purity. SOLUTION: Imidafenacin is produced by once isolating methane sulfonate or p-toluensulfonate of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutyronitrile, purifying it, and thereafter hydrolyzing it in a lower alcohol in the presence of an alkali metal oxide without neutralizing. COPYRIGHT: (C)2015,JPOandINPIT
Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: Discovery of potent and subtype-selective antimuscarinic agents
Miyachi, Hiroyuki,Kiyota, Hiromi,Uchiki, Hideharu,Segawa, Mitsuru
, p. 1151 - 1161 (2007/10/03)
In a study directed toward the development of new, selective agents with potential utility in the treatment of altered smooth muscle contractility and tone, for example, as seen in urinary incontinence associated with bladder muscle instability, a series of 4-(1-imidazolyl)-2,2-diphenylbutyramide derivatives was prepared. These compounds were examined for M1, M2, and M3 muscarinic receptor subtype selectivity in isolated tissue assays. The compounds that showed potency and/or selectivity in these tests were further evaluated for in vivo anticholinergic effects on various organs and tissues, including urinary bladder, salivary gland, and eye in rats. The structure-activity relationships for the series of 4-(1-imidazolyl)-2,2-diphenylbutyramide derivatives are also discussed. This study led to the identification of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutyramide (KRP-197) as a candidate drug for the treatment of urinary bladder dysfunction. Copyright (C) 1999 Elsevier Science Ltd.