CAS: 65193-87-5; 2-Cyanoethyl 3-Oxobutyrate

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54527-68-3 5459-58-5 1779-60-8

上下游产品

乙酰乙酸甲酯 Acetoacetic Acid Methyl Ester 105-45-3

乙酰乙酸甲酯,3-羟基丙腈置于candida Antarctica Lipase B体系中,40.0 °C,1.33 Kpa 条件下,以88%的收率获得产物2-氰基乙酰乙酸乙酯
参考文献:新型高亲脂性1,4-二氢吡啶的合成与结构研究
标题:新型高亲脂性1,4-二氢吡啶的合成与结构研究
摘要:由相应的β-酮制备了一系列新的1,4-二氢吡啶(1,4-Dhps),这些酯在氮环的c3和c5位上带有带有长且官能化的烷氧基链的酯基 酯类依次由脂肪酶催化的酯交换反应制备.结构研究已经由x射线晶体学和在半经验(am1),从头算 (hf / 6-31G *)和b3Lyp / 6-31G *级别的理论计算,发现烷基链对生物活性所需的1,4-Dhp几何形状没有任何影响.但是,这些链对亲脂性有很大影响,因此,它们可用于更好地控制药理作用的持续时间.
DOI:10.1039/b506018D

专利信息

专利号:WO-2011130852-A1
优先权日:2010-04-21
标题:Preparation of intermediates for the synthesis of dihydropyridine calcium channel blockers
发明人：SOUZA FABIO; PAN MING
权利人:ALPHORA RES INC; SOUZA FABIO; PAN MING
摘要: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-dichlorophenyl) -2,6- dimethyl-1,4- dihydropyridine, of purity greater than 97% and essentially free of the corresponding diacid, is prepared by a process involving selective precipitation of its carboxylate via addition of concentrated solutions of alkali metal salts. Similar intermediate mono-carboxylic acids useful in the synthesis of other unsymmetrically substituted dihydropyrine drugs such as nisoldipine, nitrendipine and nimodipine can be similarly prepared and purified.

专利号:CA-2701272-A1
优先权日:2010-04-21
标 题 :Preparation of intermediates for the synthesis of dihydropyridine calcium channel blockers

专利号:CN-119751447-A
优先权日:2024-12-23
标 题 :Method for asymmetric catalytic synthesis of naphthyridine carboxamide drugs

专利号:US-5767131-A
优先权日:1993-04-05
标 题 :Dihydropyridines and new uses thereof
发明人：GLUCHOWSKI CHARLES; WETZEL JOHN M; CHIU GEORGE; MARZABADI MOHAMMED R; WONG WAI C; NAGARATHNAM DHANAPALAN
权利人:SYNAPTIC PHARMA CORP
摘要:The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the structure: ##STR1## wherein Y is --(CH 2 ) n --, where n is 1, 2, 3, 4 or 5; --(CH 2 ) h --O--(CH 2 ) k --, where h and k are independently the same or different and are 2, 3 or 4; --(CH 2 ) h --CHâ• CH--(CH 2 ) k --; or --(CH 2 ) h --C.tbd.C--(CH 2 ) k --, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH 2 ; wherein R 1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R 2 and R 4 are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R 3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R 5 and R 6 are independently the same or different and are H, OH, Cl, Br, F, NO 2 , CN, CF 3 , or NH 2 , or a linear or branched chain alkyl, alkoxy, alkoxycarbonyl, acyl, alkylsulfoxide, alkylsulfone, or mono- or dialkylamino group. Other active compounds containing one, two or three rings are also disclosed as well as pharmaceutical compositions prepared therefrom and methods of use in the treatment of BPH, inhibition of cholesterol synthesis, and reduction of intraocular pressue.

专利号:US-6608086-B2
优先权日:1993-04-05
标 题:Dihydropyridines and new uses thereof
发明人：GLUCHOWSKI CHARLES; WETZEL JOHN M; CHIU GEORGE; MARZABADI MOHAMMED R; WONG WAI C; NAGARATHNAM DHANAPALAN
权利人:SYNAPTIC PHARMA CORP
摘要:This invention provides dihydropyridines useful for treatment of prostatic hyperplasia, inhibition of cholesterol synthesis, and/or reduction of intraocular pressure.

专利号:RU-2124006-C1
优先权日:1992-10-20
标 题 :Quinolone and acridine compounds, methods of their synthesis and pharmaceutical composition based on thereof