An efficient and regioselective ruthenium-catalyzed hydroaminomethlyation of olefins is reported. Key to success is the use of specific 2-phosphino-substituted imidazole ligands and triruthenium dodecacarbonyl as catalyst. Both industrially important aliphatic as well as various functionalized olefins react with primary and secondary amines to give the corresponding secondary and tertiary amines generally in high yields (up to 96%) and excellent regioselectivities (n/iso up to 99:1).
Amines Made Easily: A Highly Selective Hydroaminomethylation of Olefins
A highly chemo- and regioselective hydroaminomethylation of simple as well as functionalized alpha-olefins using a cationic rhodium precatalyst together with Xantphos as ligand is reported. Studies of the influence of ligands and reaction conditions led to an unprecedented selective hydroaminomethylation procedure. The novel procedure constitutes an economically attractive and environmentally favorable synthesis of secondary and tertiary aliphatic amines.
KAFKA, S.;KYTNER, J.;SILHANKOVA, A., COLLECT. CZECHOSL. CHEM. COMMUN., 52,(1987) N 8, 2035-2046
作者:KAFKA, S.、KYTNER, J.、SILHANKOVA, A.
DOI:——
日期:——
PHOSPHOR-LIGANDEN UND VERFAHREN ZUR SELEKTIVEN RUTHENIUM-KATALYSIERTEN HYDROAMINOMETHYLIERUNG VON OLEFINEN
申请人:Evonik Degussa GmbH
公开号:EP2951188A1
公开(公告)日:2015-12-09
[EN] BENZOTHIOPHENES<br/>[FR] BENZOTHIOPHENES
申请人:ELI LILLY AND COMPANY
公开号:WO1999015521A1
公开(公告)日:1999-04-01
(EN) This invention is related to novel benzothiophene compounds of formula (I) which are useful for the inhibition of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula (I) and processes for their preparation.(FR) La présente invention concerne de nouveaux composés de benzothiophène répondant à la formule (I) qui sont utilisés pour inhiber différents états pathologiques associés au syndrome postménopausique et à des maladies dépendant des oestrogènes, y compris le cancer du sein, de l'utérus et du col utérin. La présente invention concerne en outre des formulations pharmaceutiques de composés de la formule (I) et leurs procédés de préparation.