- Preparation method of dihydropyridine compound (by machine translation)
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Compared with the prior art, the method disclosed by the invention is suitable, for industrial production, II is, suitable for industrial production, is suitable for, industrial production, and is suitable for I. industrial production. (by machine transla
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Paragraph 0040-0052
(2020/01/08)
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- A high-purity butyric acid clevidipine preparation method (by machine translation)
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The invention discloses a high-purity butyric acid clevidipine preparation method, is in 3-amino-crotonic acid cyanogen ethyl ester and 2,3- two chlorine Asia phenmethyl acetyl acetic acid methyl ester as the starting material, the cyclization, hydrolysis
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Paragraph 0065; 0066; 0067
(2016/11/07)
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- Novel synthesis method of clevidipine butyrate important intermediate
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The invention discloses a preparation method of a clevidipine butyrate important intermediate. The preparation method comprises the steps that 3-Hydroxypropionitrile and diketene are condensed to obtain ethyl 2-cyanoacetoacetate (intermediate I); ethyl 2-cyanoacetoacetate, 2,3-dichlorobenzaldehyde and methyl 3-aminocrotonate are mixed, Hantzsch reaction is performed to obtain 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridine phthalate methyl ester-(2-cyano ethyl)-ester (intermediate II); the 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridine phthalate methyl ester-(2-cyano ethyl)-ester is hydrolyzed to obtain 4-(2,3- dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridine mono-Methyl phthalate, namely the clevidipine butyrate important intermediate. The intermediate involved in the synthesis process is not needed to be chromatographic separation and purification, the materials for synthesis are cheap and easy to obtain, the reaction speed is high, the conditions are mild, operation is simple and convenient, the process reliability is good, the yield is high, the purity of the obtained clevidipine butyrate important intermediate is above 99%, and the preparation method is suitable for mass production.
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Paragraph 0021
(2016/10/07)
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- Butyric acid clevidipine preparation method
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The invention discloses a preparation method of clevidipine butyrate, comprising the following steps: (1) carrying out one-pot reaction by putting 2,3-dichlorobenzaldehyde, methyl acetoacetate and 3-amino crotonic acid ethyl cyanide in a solvent under the action of a catalyst; (2) carrying out recrystallization to obtain a pure product (+/-)-3-(2-cyanoethyl)-5-methyl-4-(2',3'-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid; (3) carrying out a reaction between the pure product and alkali; (4) adding water and hydrochloric acid, and collecting an intermediate from reaction products; and (5) carrying out a reaction between the intermediate and n-chloromethyl butyrate in the presence of an alkaline substance and an iodide catalyst, and finally collecting the target product clevidipine butyrate from reaction products. The preparation method provided by the invention has advantages of high yield, stable product quality and low cost, is simple to operate, and is suitable for industrial product of clevidipine butyrate.
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Paragraph 0040; 0051-0052
(2017/01/17)
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- A dihydropyridine compound method for the preparation of
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The invention discloses a preparation method of a dihydropyridine compound (IV), comprising the following steps: using a compound VII and a compound VIII as initial raw materials and carrying out a cyclization reaction in a solvent to prepare an intermedi
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Paragraph 0058-0060; 0063
(2016/10/10)
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- Butyric acid clevidipine synthetic method
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The invention discloses a synthetic method of cleviprex. The method comprises the following steps: reacting a compound 1 with a compound 2 in the presence of tetrahydrofuran and triethylamine to generate a compound 3, dissolving the compound 3, a compound
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Paragraph 0047-0049; 0057-0072
(2016/10/10)
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- Compound and its as L-type calcium channel blocker or/and application of acetylcholine esterase inhibitors
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Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.
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Paragraph 0214; 0216
(2016/10/07)
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- PROCESS FOR PREPARATION OF CLEVIDIPINE AND ITS INTERMEDIATE
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The present invention relates to a process for the removal of t-butyl group from t-butyl methyl 4-(2',3'-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate to provide-1,4-dihydro-2,6-dimethyl-4-(2',3'-dichorophenyl)-5-methoxycarbonyl-3-pyr
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Page/Page column 5
(2012/06/15)
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- PREPARATION OF INTERMEDIATES FOR THE SYNTHESIS OF DIHYDROPYRIDINE CALCIUM CHANNEL BLOCKERS
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4- (2,3- dichlorophenyl) -1,4- dihydro- 2,6- dimethyl- 5- methoxycarbonyl- 3- pyridinecarboxylic acid, a key intermediate in the synthesis of the cardiovascular calcium channel blocker drug 3-butanoyloxymethoxycarbonyl-5- methoxycarbonyl-4- (2,3-dichlorop
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Page/Page column 6
(2011/11/06)
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- Mild and facile cleavage of 2-cyanoethyl ester using sodium sulfide or tetrabutylammonium fluoride. Synthesis of 1,4-dihydropyridine monocarboxylic acids and unsymmetrical 1,4-dihydropyridine dicarboxylates
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Several 3-(2-cyanoethyl)-1,4-dihydropyridine carboxylates (16) were prepared in moderate to good yields by means of the Hantzsch reaction. Treatment of these carboxylates with a weak base such as sodium sulfide or tetrabutylammonium fluoride at room temperature afforded smoothly the corresponding 1,4-dihydropyridine monocarboxylic acids (18) in good yields. The monocarboxylic acids 18n and 18o were esterified with 2-nitrooxypropanol or N-(2-hydroxyethyl)nicotinamide p-toluenesulfonic acid salt to afford the selective coronary vasodilators CD-349 (5) and CD-832 (6), respectively.
- Ogawa,Hatayama,Maeda,Kita
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p. 1579 - 1589
(2007/10/02)
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- Synthesis and antihypertensive activities of new 1,4-dihydropyridine derivatives containing a nitrooxy moiety at the 3-ester position
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The synthesis of a new series of dihydropyridines containing a nitrooxy moiety at the 3-ester position is described. The antihypertensive activity of the compounds was examined and compared with that of nifedipine; some of them were relatively potent. The structure-activity relationship is also discussed.
- Ogawa,Nakato,Tsuchida,Hatayama
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p. 108 - 116
(2007/10/02)
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- Acyloxymethyl as an activating group in lipase-catalyzed enantioselective hydrolysis. A versatile approach to chiral 4-aryl-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylates
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The first practical syntheses of chiral 4-aryl-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylates, which are attractive compounds as new calcium antagonists, were realized by lipase-catalyzed enantioselective hydrolysis of the acyloxymethyl esters. The monoesters obtained were revealed to have high optical purity and demonstrated to be useful chiral synthons.
- Ebiike,Terao,Achiwa
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p. 5805 - 5808
(2007/10/02)
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- Resolution of 1,4-dihydropyridine derivatives
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Optically active compounds of formula 1 STR1 wherein R1 is H or lower alkyl; R2 and R6 are each independently lower alkyl, aryl, or arylalkyl; R3 is CN, NO2, CO2 R5, CONHR5, SO2 R5, or P(O)(OR5)2, where R5 is lower alkyl, lower alkoxyalkyl, aryl, or arylalkyl; R4 is aryl, heterocyclyl, or fused-ring heterocyclyl, optionally substituted with one, two, or three halo, NO2, CN, lower alkyl, lower alkoxy, lower alkylamino, CF3, OCH2 F, or OCF3 ; are prepared by fractional crystallization from hot organic solvent and water in the presence of a suitable optically active amine base.
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