Enantioselective synthesis of β-amino acids based on BINAP—ruthenium(II) catalyzed hydrogenation
摘要:
BINAP-Ru(II) catalyzed hydrogenation of beta-substituted (E)-beta-(acylamino)acrylic acids allows efficient enantioselective synthesis of beta-amino acids. The Z double bond isomers which possess an intramolecular hydrogen bond between amide and ester groups are more reactive but are hydrogenated with poor enantioselectivity. BINAP-Rh(I) complexes afford only moderate stereoselectivity with the opposite sense of enantioselection.
[EN] BICYCLIC PYRIMIDONE COMPOUNDS AS INHIBITORS OF LP-PLA2<br/>[FR] COMPOSÉS DE PYRIMIDONE BICYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE LP-PLA2
申请人:GLAXOSMITHKLINE IP DEV LTD
公开号:WO2014114249A1
公开(公告)日:2014-07-31
The present invention relates to novel pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
BICYCLIC PYRIMIDONE COMPOUNDS AS INHIBITORS OF LP-PLA2
申请人:GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
公开号:US20150344485A1
公开(公告)日:2015-12-03
The present invention relates to novel pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA
2
activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA
2
, for example atherosclerosis, Alzheimer's disease.
Enantioselective synthesis of β-amino acids based on BINAP—ruthenium(II) catalyzed hydrogenation
作者:William D. Lubell、Masato Kitamura、Ryoji Noyori
DOI:10.1016/s0957-4166(00)86107-8
日期:1991.1
BINAP-Ru(II) catalyzed hydrogenation of beta-substituted (E)-beta-(acylamino)acrylic acids allows efficient enantioselective synthesis of beta-amino acids. The Z double bond isomers which possess an intramolecular hydrogen bond between amide and ester groups are more reactive but are hydrogenated with poor enantioselectivity. BINAP-Rh(I) complexes afford only moderate stereoselectivity with the opposite sense of enantioselection.