vinyl-terminated allyl chlorides via alkene hydroboration with 9-BBN-H followed by Cu-catalyzed asymmetric intramolecular allylicalkylation with a new chiral phosphoramidite ligand produced six-membered ring compounds with a tertiary or quaternary stereogenic center in the ring with high enantioselectivity.
通过烯烃与 9-BBN-H 的硼氢化反应,然后用新的手性亚磷酰胺配体进行 Cu 催化的不对称分子内烯丙基烷基化,乙烯基封端的烯丙基氯的还原性 C-C-键形成环化产生具有叔或环中的四元立体中心具有高对映选择性。
BREHM, RENATE;OHNHAUSER, DIETER;GERLACH, HANS, HELV. CHIM. ACTA, 70,(1987) N 8, 1981-1987
作者:BREHM, RENATE、OHNHAUSER, DIETER、GERLACH, HANS
DOI:——
日期:——
[EN] METHODS FOR THE STEREOSELECTIVE SYNTHESIS OF SUBSTITUTED PIPERIDINES<br/>[FR] PROCEDES DE SYNTHESE STEREOSELECTIVE DE PIPERIDINES SUBSTITUEES
申请人:SEPRACOR INC
公开号:WO2002046157A2
公开(公告)日:2002-06-13
One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invnetion relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that affict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
Synthese und Bestimmung des Chiralitätssinns von (+)-(<i>R</i>)-1-Azabicylo[3.3.1]nonan-2-on
作者:Renate Brehm、Dieter Ohnhäuser、Hans Gerlach
DOI:10.1002/hlca.19870700802
日期:1987.12.16
Synthesis and Determination of the Chirality Sense of (+)-(R)-1-Azabicyclo[3.3.1]nonan-2-one