Patents Examined by Robert W. Ramjuer
  • Patent number: 5919947
    Abstract: The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps:(1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage;(2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation;(3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and(4) isolation of the desired indole derivative thereby obtained.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: July 6, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Adrian Leonard Smith