CAS: 70877-75-7; 4-((S)-Hydroxy((1S,2R,4S,5R)-5-Vinylquinuclidin-2-yl)Methyl)Quinolin-6-Ol

相似化合物

130-95-0 56-54-2 130-89-2

上下游产品

quinindine qunidine quinine quinine 9O-methanesulfonateQuinine (8α,9R)-10,11-dihydro-cinchonan-6',9-diol 6'-(methoxymethyl)-cupreidine 9-O-(4-(perfluoro-n-°Ctyl)benzyl) ether cupreidine 9-O-(4-(perfluoro-n-°Ctyl)benzyl) ether

📜9-Mesylquinine置于d-酒石酸,Sodium Hydride,乙硫醇体系中,用 水,N,N-二甲基甲酰胺,Mineral Oil 作为反应溶剂,化学反应 19.5H,反应生成 O-去甲基奎尼丁
参考文献:金鸡纳生物碱衍生物催化β-酮酯的对映选择性α-羟基化
标题:金鸡纳生物碱衍生物催化β-酮酯的对映选择性α-羟基化
摘要:在枯基氢过氧化物(chp)存在下,实现了由铜吡啶催化的β-酮酯的高效α-羟基化.该反应适用于多种 β-酮酯,以高产率(高达 95%)得到具有优异对映选择性(高达 97% Ee)的产物.该反应已成功放大到克级,并且 (S)-5-Chloro-2-Hydroxy-1-Oxo-2,3-Dihydro-1H-Indene-2-Carboxylate-茚虫威的重要中间体在96% 收率和 86% Ee.通过结晶可将对映体过量提高到99%,该方法具有对映选择性高,催化剂易于制备和催化剂回收等优点,具有工业应用前景.
DOI:10.1055/s-0034-1378548

专利信息

专利号:WO-2016173960-A1
优先权日:2015-04-29
标 题 :Optimized synthesis of pregabalin and 4-aminobutane acid using an improved method for producing conjugated nitroalkenes
发明人：STUMPF MARCUS
权利人:K H S PHARMA HOLDING GMBH
摘要:The invention relates to an optimized synthesis of pregabalin and additional 4-aminobutane acids using an improved method for producing conjugated nitroalkenes. This is achieved by a nitro-aldol reaction of an aliphatic aldehyde with a nitroalkane in the presence of a suitable diamine directly followed by an elimination of the conjugated nitroalkene by adding an acid, a subsequent catalyzed asymmetrical 1,4-Michael addition of a suitable nucleophile, and a subsequent retro-Claisen reaction or a hydrolosis and decarboxylation with a concluding reduction to 4-aminobutane acid.

专利号:EP-3088383-A1
优先权日:2015-04-29
标题:Optimized synthesis of pregabalin and 4-amino butanoic acid using an improved production method of conjugated nitroalkenes

专利号:US-11034695-B2
优先权日:2016-09-23
标 题:Dopamine-β-hydroxylase inhibitors
发明人：SOARES DA SILVA PATRÃ?CIO; ROSSI TINO; KISS LASZLO ERNO; BELIAEV ALEXANDER; LEAL PALMA PEDRO NUNO
权利人:BIAL—PORTELA & CA S A; BIAL—PORTELA & Cᵃ S A
摘要:This invention relates to: (a) compounds of Formula Ia (with R1, R4, R5, R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.