A new strategy for the synthesis of tetrahydroisoquinolines based on the Pd0‐catalyzed intramolecular α‐arylation of sulfones is reported. The combination of this Pd‐catalyzed reaction with intermolecular Michael and aza‐Michael reactions allows the development of two‐ and three‐step domino processes to synthesize diversely functionalized scaffolds from readily available starting materials.
[EN] THE NEW PREPARATION OF ALIPHATIC AMINES WITH SULPHONYL GROUP AND THEIR SALTS<br/>[FR] NOUVELLE PRÉPARATION D'AMINES ALIPHATIQUES AVEC UN GROUPE SULFONYLE ET LEURS SELS
申请人:KNOWA PHARMACEUTICAL SHANGHAI
公开号:WO2010130124A1
公开(公告)日:2010-11-18
A new preparation of aliphatic amines with sulphonyl group and their salts, using sulfonates with sulphonyl group as raw material and ammonia or amine as substituent reagent reacting with the raw material to obtain the product. A new kind of intermediates 2-(N,N-dibenzylamino)ethylmethylsulfones and their salts preparated by above new method and their use. A new use of preparation of 2-(amino) ethylmethylsulfone and its salts using 2-(N,N-dibenzylamino)ethylmethylsulfones and their salts. The invention not only avails to reduce the entironment pollution and can be used to prepare 2-(amino) ethylmethylsulfone and its salts on large scale, but also avails to prepare 2-(amino) ethylmethylsulfone hydrochloride of high purty.