- 4-(2-METHYL-1H-IMIDAZOL-1-YL)-2,2-DIPHENYLBUTANENITRILE SOLID FORM
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The present invention relates to a solid form of 4-(2-methyl-1 H-imidazol-1-yl)-2,2- diphenylbutanenitrile phosphate intermediate and its use for preparing imidafenacin, and an improved process for preparing 4-(2-methyl-1-imidazolyl)-2,2- diphenylbutanamide, also known as imidafenacin, in good yield and purity using said solid form.
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Page/Page column 24
(2016/09/26)
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- A method of preparing the new the onamot reaches
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The present invention discloses a preparation method of imidafenacin. In the method, 4-chloro-2, 2-diphenylbutaneamide and 2-methylimidazole are taken as raw materials for reaction in the presence of alkali, and then ethyl acetate is used for recrystallization. The method has advantages of high yield, mild reaction condition, and simple purification and is suitable for industrialized production.
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Paragraph 0036
(2016/10/10)
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- Preparation technology for imidafenacin
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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.
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- METHOD FOR PRODUCING 4-(2-METHYL-1-IMIDAZOLYL)-2,2-PHENYLBUTANE AMIDE
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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
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Paragraph 0008; 0017; 0018
(2016/12/22)
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- PROCESS FOR PRODUCING MUSCARINE RECEPTOR ANTAGONIST AND INTERMEDIATE THEREFOR
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The industrial production of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide, a urinary incontinence remedy, necessitates elimination of problems concerning the use of a synthetic adsorbent, e.g., HP-20, the efficiency of operation with the same, purification efficiency, etc. An acid salt, e.g., hydrochloride or phosphate, of 4-(2-methyl-1-imidazolyl)-2,2- diphenylbutanamide or a hydrate of any of these salts is used as an intermediate. This intermediate is neutralized and then purified. Thus, high-purity 4-(2-methyl -1-imidazolyl)-2,2-diphenylbutanamide is easily obtained in satisfactory yield. The industrial-scale production process has been thus established.
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Page/Page column 5
(2008/06/13)
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- Design, synthesis and antimuscarinic activity of some imidazolium derivatives
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A series of imidazolium salt derivatives was prepared as part of a search for subtype-selective antimuscarinic agents. On the basis of measurements of the antimuscarinic activity and subtype-selectivity for M2 and M3 muscarinic receptors, the structure-activity relationships of these compounds are discussed.
- Miyachi, Hiroyuki,Kiyota, Hiromi,Segawa, Mitsuru
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p. 3003 - 3008
(2007/10/03)
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- Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: Discovery of potent and subtype-selective antimuscarinic agents
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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.
- Miyachi, Hiroyuki,Kiyota, Hiromi,Uchiki, Hideharu,Segawa, Mitsuru
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p. 1151 - 1161
(2007/10/03)
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- Imidazole derivatives and process for preparing the same
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The invention relates to the imidazole derivatives as selective antagonistic substances against muscarinic acetylcholine and provides imidazole derivatives represented by a general formula (1) or (2) STR1 ?wherein R1 is a phenyl group which may have substituent or thienyl group, R2 is a cyano group, a carboxy group, CONR7 R8 group (wherein R7 and R8 each independently represent hydrogen atom or lower alkyl group, or R7 and R8 may form a ring by alkylene chain which may contain hetero atom) or COOR9 group (wherein R9 is a lower alkyl group), R3 is a hydrogen atom or lower alkyl group, R4, R5 and R6 each independently represent hydrogen atom, lower alkyl group which may have substituent or cycloalkyl groups, or may form a condensed ring at the positions of R5 and R6 with benzene ring, R10 is a lower alkyl group or aralkyl group which may have substituent, m is an integer from 1 to 6, and Z is a halogen atom!.
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