A palladium-catalyzed domino process for the quick assembly of tricyclic-fused heterocycles starting from aryl iodides and functionalized isocyanides containing a disubstituted terminal alkene has been developed. The process is triggered by intermolecular isocyanide insertion, followed by Heck-type carbopalladation of the intramolecular alkene moiety and subsequent C(sp2)–H activation. Moreover, an
Highly Enantioslective Synthesis of Multisubstituted Polyfunctional Dihydropyrrole via an Organocatalytic Tandem Michael/Cyclization Sequence
作者:Gen Zhang、Yaohu Zhang、Xianxing Jiang、Wenjin Yan、Rui Wang
DOI:10.1021/ol201299u
日期:2011.8.5
approach to asymmetric synthesis of various optically pure multisubstituted 2,3-dihydropyrroles catalyzed by a novel rosin-derived tertiary amine–thiourea via a tandem Michael/cyclization sequence with high yield (up to 97%) and good to excellent enantioselectivities (up to 97% ee) is present. This strategy provides an efficient and convenient method to access enantioenrich nitrogenheterocycles.
Ausgehend von L-Asparaginsäure (I), bzw. L-Asparagin (Ia) wurden über den L-Asparaginsäure-diäthylester (II) auf verschiedenen Wegen über die Zwischenprodukte III, VI, VIa, b, c, d, e, VII die racemischen Diastereomeren der Diamino-tricarbonsäure IX erhalten. Versuche zur präparativen Herstellung der Äthoxycarbonyl- und Methoxycarbonyl-anhydro-lycomarasminsäureester X, Xa aus den Chloracetyl-Derivaten
[EN] PROCESS FOR PREPARING 4-ARYL-PIPERIDINE DERIVATIVES<br/>[FR] PROCEDE DE PREPARATION DE DERIVES DE 4-ARYLPIPERIDINE
申请人:NOVO NORDISK A/S
公开号:WO1996036636A1
公开(公告)日:1996-11-21
(EN) A process for the preparation of a compound of formula (VIII), wherein R1 is C2-5-alkyl, phenyl-C1-5-alkyl, or substituted phenyl-C1-5-alkyl.(FR) L'invention concerne un procédé de préparation d'un composé de formule (VIII), dans laquelle R1 représente alkyle-C2-5, phényle-alkyle-C1-5, ou phényle-alkyle-C1-5 à substitution.