公开(公告)号：EP1476407A2

公开(公告)日：2004-11-17

申请号：EP03713665.2

申请日：2003-02-24

申请人： Honeywell International Inc.

发明人： WERNER, Christian ,  NERENZ, Franc ,  KANSCHIK-CONRADSEN, Andreas

IPC分类号： C07B47/00 ,  C07F9/24 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00

CPC分类号： C07H19/10 ,  C07H19/20

摘要： Provided are methods of producing phosphitylated compounds, including 3'-O­phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of (1) acid-base complexes derived from an amine base of Formula (I) wherein R, R1, and R2 are independently C1-C10 alkyl, C1-C10 cycloalkyl, C1-Cl0 aryl, Cl-C10 aralkyl, Cl-C10 heteroalkyl, or Cl-CIO heteroaryl; (2) acid-base complexes derived from an amine base of Formula (II) wherein R3, R4, R5, R6, and are independently hydrogen, C1-C10 alkyl, Cl-C10 cycloalkyl, Cl-C10 aryl, Cl-CIO aralkyl, Cl-CIO heteroalkyl, or C1-C10 heteroaryl, and at least one of R3, R4, R5, R6, and R7 is not hydrogen.; (3) acid-base complexes derived from a diazabicyclo amine base; (4) zwitterionic amine complexes; and (5) combinations of two or more thereof, to produce a phosphitylated compound.