1-Aminopyridinium Ylides as Monodentate Directing Groups for sp<sup>3</sup> C–H Bond Functionalization
作者:Ky Khac Anh Le、Hanh Nguyen、Olafs Daugulis
DOI:10.1021/jacs.9b06643
日期:2019.9.18
1-Aminopyridinium ylides are efficientdirecting groups for palladium-catalyzed β-arylation and alkylation of sp3 C-H bonds in carboxylic acid derivatives. The efficiency of these directing groups depends on the substitution at the pyridine moiety. The unsubstituted pyridine-derived ylides allow functionalization of primary C-H bonds, while methylene groups are unreactive in the absence of external
[EN] NOVEL PROCESS FOR THE PREPARATION OF AMINO ACID DERIVATIVES<br/>[FR] PROCÉDÉ INÉDIT DE FABRICATION DE DÉRIVÉS D'ACIDES AMINÉS
申请人:UCB PHARMA SA
公开号:WO2010052011A1
公开(公告)日:2010-05-14
The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).