[EN] BIPHENYL-SUBSTITUED 4-AMINO-BUTYRIC ACID DERIVATIVES AND THEIR USE IN THE SYNTHESIS OF NEP INHIBITORS<br/>[FR] DÉRIVÉS D'ACIDE 4-AMINÉ-BUTYRIQUE SUBSTITUÉS PAR LE BIPHÉNYLE, ET LEUR UTILISATION DANS LA SYNTHÈSE D'INHIBITEURS DE NEP
申请人:NOVARTIS AG
公开号:WO2017033128A1
公开(公告)日:2017-03-02
The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.
A cascade process for the straightforward one-pot conversion of β-ketonitriles into β-hydroxyamides is presented. The process, that proceeds in water employing the arene-ruthenium(II) complex [RuCl2(η6-p-cymene)P(4-C6H4F)2Cl}] as catalyst in combination with sodium formate, involves the initial hydration of the β-ketonitrile substrates to generate the corresponding β-ketoamide intermediates, which
提出了一种简单的一锅法将β-乙腈转化为β-羟酰胺的级联方法。的过程中,在水中进行采用芳烃-钌(II)络合物将[RuCl 2(η 6 - p -cymene)P(4-C 6 H ^ 4 F)2氯}]如甲酸钠催化剂组合该方法涉及β-酮腈底物的初始水合反应,以生成相应的β-酮酰胺中间体,然后对其进行羰基的转移氢化(TH)。雇用40个不同的β族-乙腈具有不同的取代模式,已经确定了该方法的范围和局限性。
Ruthenium-Catalyzed Synthesis of β-Hydroxyamides from β-Ketonitriles in Water
An unprecedented hydration/transfer hydrogenation tandem process for the catalytic conversion of β-ketonitriles into synthetically useful β-hydroxyamides in water has been developed, making use of the ruthenium(II) complex [RuCl2(η6-p-cymene)P(4-C6H4F)2Cl}] in combination with sodium formate.
对于β酮腈的催化转化成在水中合成有用β羟基酰胺前所未有的水合/转移氢化串联过程已经被开发,利用钌(II)络合物将[RuCl 2(η 6 - p -cymene)P (4-C 6 H 4 F)2 Cl}]与甲酸钠组合。
Diastereoselective β-Hydroxyalkylation
and β-Hydroxycarboxylation of Amides by a Diels-Alder
Strategy
作者:Léon Ghosez、Deogratias Ntirampebura
DOI:10.1055/s-2002-34367
日期:——
Acid chlorides readily condensed with N-silylated imines in the presence of a base to generate 2-azadienes. These underwent Diels-Alder cycloadditions with a wide variety of aldehydes.. In most cases the cycloadditions were diastereoselective in favor of the 3,4-cis-oxazinone adducts. Ethanolysis stereoselectively yielded products of hydroxyalkylation or hydroxycarboxylation of the primary amides derived
Antipicornaviral compounds, compositions containing them, and methods for their use
申请人:——
公开号:US20040072907A1
公开(公告)日:2004-04-15
A magnetic circuit component having a plurality of claws arranged in a plurality of rows, with the base of each claw connected to a common yoke. A plurality of non-interlaced coils constituting a multi-phase winding are included, with the coils being wound around the bases of corresponding claws, and being distributed uniformly in the direction of motion.