Tandem α-Alkylation/Asymmetric Transfer Hydrogenation of Acetophenones with Primary Alcohols
作者:Oleksandr O. Kovalenko、Helena Lundberg、Dennis Hübner、Hans Adolfsson
DOI:10.1002/ejoc.201403032
日期:2014.10
A tandem -alkylation/asymmetric transferhydrogenation of acetophenones with primary alcohols, mediated by a single ruthenium catalyst, is described. Under optimized reaction conditions and with use of [Ru(p-cymene)Cl-2](2) in combination with an amino acid hydroxyamide ligand, the chiral secondary alcohol products were isolated in moderate yields and in moderate to good enantiomeric excess (up to
[EN] EP2 RECEPTOR AGONISTS<br/>[FR] AGONISTES DU RECEPTEUR EP2
申请人:PHARMAGENE LAB LTD
公开号:WO2005061449A1
公开(公告)日:2005-07-07
A compound selected from Formula (iv) or Formula (iii); (iv) (1R,2S)-2[4-1(S)-hydroxyhexyl)phenyl]-5-oxo-cyclopentaneheptanoic acid [RSS] or (iii) (1R,2S)-2[4-1(R)-hydroxyhexyl)phenyl]-5-oxo-cyclopentaneheptanoic acid [RSR] or a salt, solvate, chemically protected form or prodrug thereof, and its use in treating conditions alleviated by agonism of an EP2 receptor.
convert alkenes, unsaturated aliphatic alcohols, and aryl boronic acids into secondary benzylic alcohols with high stereoselectivities (typically >95:5 er) under sequential catalysis that integrates alkene cross-metathesis, isomerization, and nucleophilic addition. Prochiral allylic alcohols can be converted to any stereoisomer of the product with high stereoselectivity (>98:2 er, >20:1 dr).
A compound selected from one of the following:
or a salt, solvate, chemically protected form or prodrug thereof, and its use in treating conditions alleviated by agonism of an EP
2
receptor.
A compound selected from one of the following:
or a salt, solvate, chemically protected form or prodrug thereof, and its use in treating conditions alleviated by agonism of an EP
2
receptor.