- 2,4-(1H, 3H)-quinazolinedione derivative and synthesis method and use thereof
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The present invention discloses a 2,4-(1H,3H)-quinazolinedione derivative and a synthesis method and use thereof, belongs to the technical field of medicines, and relates to the 2,4-(1H, 3H)-quinazolinedione derivative shown as general formula(I), wherein R1 is O(CH2)n-1H, n=1-10; or NH(CH2)n-2H, n=2-10; or NH(CH2)n-3(CH3)2, n=3-10; or N(CH2)n-4, n=6-10; or NH(CH2)n-5 C6H4-L, n=5-10; R2 is H; or X-O(CH2)n-1H, n=1-10; or X-NH(CH2)n-2(CH3)2, n=2-10; X is m-CH2C6H4CO; L is independently selected from the group consisting of H, F, Cl, Br, I, CN, NO2, CF3, OCF3, SCF3, OH, SH, NH2, COOR, R, OR, SR, NHR, NRR, OCOR, SCOR and NHCOR, wherein R is C1-6 straight chain alkyl, branched alkyl or alicyclic alkyl or phenyl. Structures and the synthesis method and in-vitro acetylcholin esterase inhibition activity of the compounds are disclosed, and the compounds can be further developed as drugs for treating Alzheimer's disease.
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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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- 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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(2008/06/13)
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