申请人:Chirotech Technology, Ltd.
公开号:US06320068B1
公开(公告)日:2001-11-20
The present invention pertains to a process for the preparation of an arylphosphine of the formula R1OC—Ar—PR2R3 wherein Ar is aryl or heteroaryl; R1 is an alkoxy or amine group; and R2 and R3 are each any organic group; and each of the respective groups may optionally be substituted with any non-interfering group; which comprises the reaction of a sulfonyloxy compound of the formula R1OC—Ar—OSO2R4 wherein R4 is alkyl, haloalkyl, perhaloalkyl, aryl, aralkyl or alkaryl, with a phosphine of the formula HPR2R3, in a solvent and in the presence of a palladium catalyst and a base. The arylphosphine can then readily be converted to a chiral phosphine ligand.
本发明涉及一种制备式R1OC—Ar—PR2R3的芳基膦化合物的方法,其中Ar是芳基或杂环芳基;R1是烷氧基或胺基;R2和R3分别是任意的有机基;各自的基可以选择性地被任何非干扰基取代;所述方法包括将式R1OC—Ar—OSO2R4的磺酰氧化合物(其中R4是烷基、卤代烷基、全氟烷基、芳基、芳基烷基或烷基芳基)与式HPR2R3的膦化合物在溶剂中,在钯催化剂和碱的存在下反应。然后可以将芳基膦化合物轻松转化为手性膦配体。