Robinson, Henry; Oatley, Steven A.; Rowedder, James E.; Slade, Pawel; Macdonald, Simon J. F.; Argent, Stephen P.; Hirst, Jonathan D.; McInally, Thomas; Moody, Christopher J. published the artcile< Late-Stage Functionalization by Chan-Lam Amination: Rapid Access to Potent and Selective Integrin Inhibitors>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is naphthyridinylpentanamide arylpropanoic acid boronate Chan Lam amination; aminophenylpropanoic tetrahydro naphthyridinylpentanamide preparation integrin inhibitor idiopathic pulmonary fibrosis; C−N coupling; integrin antagonists; late-stage functionalization; medicinal chemistry; β-amino acids.
A late-stage functionalization of the aromatic ring in amino acid derivatives was described. The key step was a copper-catalyzed diversification of a boronate ester I (X = 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl; R1 = Boc; R2 = t-Bu) by amination (Chan-Lam reaction) that can be carried out on a complex β-aryl-β-amino acid scaffold. This not only considerably extended the substrate scope of amination partners, but also delivered an array of potent and selective integrin inhibitors I (X = 1-pyrazolyl, 4-chloro-1-imidazolyl, 1-piperidinyl, 1,4-oxazepan-4-yl, etc.; R1 = R2 = H) as potential treatment agents of idiopathic pulmonary fibrosis (IPF). This versatile chem. strategy, which was amenable to high-throughput-array protocols, allows the installation of pharmaceutically valuable heteroaromatic fragments at a late stage by direct coupling to NH heterocycles, leading to compounds with drug-like attributed.
Chemistry – A European Journal published new progress about Amination. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics