Cholesterol-lowering bile acid-binding agents: novel lipophilic polyamines
摘要:
A series of novel lipophilic polyamines was synthesized by the sodium cyanoborohydride-mediated reductive amination of various ketones and aldehydes with the polyamine tris(2-aminoethyl)amine. Two of these compounds, N,N-bis[2-(cyclododecylamino)ethyl]-N'-benzyl-1,2-ethanediamine trihydrochloride (36.3HCl) and N,N-bis[2-(cyclododecylmethylamino)ethyl]-N',N'-dimethyl-1,2-ethaediamine (23), are 29 and 24 times more potent than colestipol hydrochloride, respectively, for lowering animal serum cholesterol levels.
Highly Active Palladium Catalysts Supported by Bulky Proazaphosphatrane Ligands for Stille Cross-Coupling: Coupling of Aryl and Vinyl Chlorides, Room Temperature Coupling of Aryl Bromides, Coupling of Aryl Triflates, and Synthesis of Sterically Hindered Biaryls
作者:Weiping Su、Sameer Urgaonkar、Patrick A. McLaughlin、John G. Verkade
DOI:10.1021/ja0450096
日期:2004.12.1
R' = i-Bu, 1; R = Bz, R' = i-Bu, 3; R = R' = Bz, 4] for palladium-catalyzed Stille reactions of aryl chlorides is described. Catalysts derived from ligands 1 and 4 efficiently catalyze the coupling of electronically diverse aryl chlorides with an array of organotin reagents. The catalyst system based on the ligand 3 is active for the synthesis of sterically hindered biaryls (di-, tri-, and tetra-ortho
LIPOPHILIC POLYAMINES USEFUL FOR TREATING HYPERCHOLESTEROLEMIA
申请人:THE UPJOHN COMPANY
公开号:EP0424385A1
公开(公告)日:1991-05-02
US5192798A
申请人:——
公开号:US5192798A
公开(公告)日:1993-03-09
[EN] LIPOPHILIC POLYAMINES USEFUL FOR TREATING HYPERCHOLESTEROLEMIA
申请人:THE UPJOHN COMPANY
公开号:WO1989008098A2
公开(公告)日:1989-09-08
(EN) This invention relates to novel lipophilic polyamides of the formula Z1-(CH2)n-Y1-X1-R1, the method of using these compounds to treat hypercholesterolemia, and intermediates thereto.(FR) Cette invention concerne de nouvelles polyamines lipophiles de la formule Z1-(CH2)n-Y1-X1-R1, le procédé d'utilisation de ces composés afin de traiter l'hypercholestérolémie, ainsi que des intermédiaires de ceux-ci.