CAS: 55985-32-5; Methyl 2-(Benzyl-Methyl-Amino)Ethyl2,6-Dimethyl-4-(3-Nitrophenyl)-1,4-Dihydropyridine-3,5-Dicarboxylate

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2,6-Dimethyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-methyl ester 5-[2-(toluene-4-sulfonyloxy)-ethyl] ester benzyl-methyl-amine 2-(N-benzyl-N-methyl)amino-1-ethanol (R)-2,6-Dimethyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-((S)-1-benzyl-piperidin-3-yl) ester 5-methyl ester3-{2-[benzyl(methyl)amino]ethyl} 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylate 2,6-Dimethyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-(2-benzylamino-ethyl) ester 5-methyl ester nisoldipine 26H23(2)H6N3O6C26H23(2)H6N3O6

📜2-Hydroxyethyl Methyl 1,4-Dihydro-2,6-Dimethyl-4-(3-Nitrophenyl)-3,5-Pyridinedicarboxylate置于水,三乙胺体系中,用 四氢呋喃 作为反应溶剂,化学反应 9.5H,反应生成 尼卡地平
参考文献:Synthesis Of Asymmetric 4-Aryl-1,4-Dihydro-2,6-Dimethyl-3,5-Pyridinedicarboxylates With Vasodilating And Antihypertensive Activities.
标题:Synthesis Of Asymmetric 4-Aryl-1,4-Dihydro-2,6-Dimethyl-3,5-Pyridinedicarboxylates With Vasodilating And Antihypertensive Activities.
摘要:合成了非对称的4-芳基-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸酯,其中含有2-乙烯二氧丙基,2-氧丙基或环丙基甲基作为酯基,以及相关衍生物,并进行了在麻醉开放胸腔犬中的扩血管活性及在意识清醒的自发性高血压大鼠中的抗高血压活性测试.环丙基甲基甲基1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸酯(5F,Mpc-2101)和甲基2-氧丙基1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸酯(8I,Mpc-1304)分别表现出强效的脑扩血管和抗高血压活性.在3.0 μg/kg的静脉给药后,5F对脊椎血流的最大增加为221.4%,而硝苯地平和尼卡地平氯化物分别为187.0%和166.3%.8I在0.3和1.0 Mg/kg口服给药后的收缩压最大下降分别为42.2和54.0 Mmhg,而硝苯地平,尼卡地平和肼苯噻啶氯化物在3.0 Mg/kg时的最大下降分别为23.3,16.8和24.5 Mmhg.5F和8I的显著扩血管和抗高血压效果持续时间比硝苯地平和尼卡地平更长.
DOI:10.1248/cpb.34.1589

专利信息

专利号:US-9199913-B2
优先权日:2011-04-25
标 题:Process for continous flow synthesis of beta-amino crotonate
发明人：KULKARNI ARVIND A; JOSHI ANNA R; JOSHI RAMESH R
权利人:KULKARNI ARVIND A; JOSHI ANNA R; JOSHI RAMESH R; COUNCIL SCIENT IND RES
摘要:Beta aminocrotonates are important intermediates for the synthesis of Ca channel blockers. The processes available in the art are batch processes with yields about 85%. There are no continuous processes available for the synthesis of such compounds. This gap in the art is addressed by the invention by disclosing a continuous process resulting in high yields of beta amino crotonates.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-2017348280-A1
优先权日:2016-06-06
标题 :Counteracting the inhibition of collagen synthesis by select calcium and sodium channel blockers using ascorbic acid and ascorbyl palmitate
发明人：RATH MATTHIAS W; NIEDZWIECKI ALEKSANDRA; IVANOV VADIM O; IVANOVA SVETLANA V
权利人:RATH MATTHIAS W; NIEDZWIECKI ALEKSANDRA; IVANOV VADIM O; IVANOVA SVETLANA V
摘要:A therapeutic use of ascorbyl palmitate, ascorbic acid and/or derivatives thereof to reverse or counter the adverse effects of channel blockers in the medical management of cardiovascular disease in a subject is presented. Effects of select Na- and Ca-channel blockers on collagen synthesis and deposition were evaluated in cultured human dermal fibroblasts and aortic smooth muscle cells by immunoassay. Ca and Na-channel blockers inhibited the synthesis of collagen type I and collagen type IV, the basic molecules of vascular wall stability. The inhibitory effects of the calcium and sodium channel blockers on collagen synthesis was reversed by introducing ascorbic acid and/or ascorbyl palmitate. It can be concluded that calcium and sodium channel blockers have a direct inhibitory effect on collagen synthesis, favoring the instability of the vascular wall and the progression of cardiovascular disease, an effect that is mitigated by treatment with, ascorbyl palmitate, ascorbic acid and or derivatives thereof.