CAS: 103129-81-3; (R)-3-Ethyl 5-Methyl 2-((2-Aminoethoxy)Methyl)-4-(2-Chlorophenyl)-6-Methyl-1,4-Dihydropyridine-3,5-Dicarboxylate

上下游产品

-4(R)-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-1,4-dihydropyridine2-(2-azidoethoxy)methyl-4(R)-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-1,4-dihydropyridine -4-(2-chlorophenyl)-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine2-(2-azidoethoxy)methyl-4-(2-chlorophenyl)-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine -4-(2-chlorophenyl)-5-(methoxycarbonyl)-3--6-methyl-1,4-dihydropyridine(-)-2-(2-azidoethoxy)methyl-4-(2-chlorophenyl)-5-(methoxycarbonyl)-3-(2(S)-methoxy-2-phenethoxy)carbonyl-6-methyl-1,4-dihydropyridine 2-cyanoethyl 4-(2-azidoethoxy)-3-oxobutanoateramipril-amlodipine salt 2-(2-Amino-ethoxymethyl)-4-(2-chloro-phenyl)-6-methyl-pyridine-3,5-dicarboxylic acid 3-ethyl ester 5-methyl ester 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine amlodipine

2-<(2-Azidoethoxy)Methyl>-4-(2-Chlorophenyl)-5-Methoxycarbonyl-6-Methyl-1,4-Dihydropyridine置于lindlar'S Catalyst 氢气,Sodium Ethanolate,N,N'-羰基二咪唑体系中,用 乙醇,二乙二醇二甲醚 用作溶剂,25.0 °C,103.42 Kpa 条件下,反应 2.0H,反应生成3-乙基5-甲基2-[(2-氨基乙氧基)甲基]-4-(2-氯苯基)-6-甲基-1,4-二氢-3,5-吡啶二羧酸酯
参考文献:长效二氢吡啶类钙拮抗剂.1.结合有碱性取代基的2-烷氧基甲基衍生物.
标题:长效二氢吡啶类钙拮抗剂.1.结合有碱性取代基的2-烷氧基甲基衍生物.
摘要:描述了一系列在2-位被碱性侧链取代的二氢吡啶,并列出了其作为钙拮抗剂的效力.发现一种化合物2-[((2-氨基乙氧基)甲基]-4-(2-氯苯基)-3-乙氧基羰基-5-甲氧基羰基-6-甲基-1,4-二氢吡啶(17,氨氯地平)具有可比性.对硝苯地平有效,并具有30 H的消除半衰期.口服生物利用度接近100%,血液动力学反应起效缓慢,效果持久.已经制备了两种对映异构体,并且发现大部分活性与(-)异构体18有关.对17的相似类似物进行的x射线晶体学研究表明,两者之间存在弱氢键侧链氧和质子在环氮上.
Doi:10.1021/jm00159A022

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:CN-114989072-B
优先权日:2022-05-27
标 题 :Method for asymmetric catalytic synthesis of chiral 1, 4-dihydropyridine compound and application thereof

专利号:CA-2551859-C
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:EP-2250143-A2
优先权日:2008-01-25
标题 :Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:WO-2005066122-A2
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof