Palladium catalyzed indolization

Details Palladium catalyzed indolization Palladium catalyzed indolization

1997-08-07

1999-03-02

Richter, Johann

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D20904

Patent

active

058773290

ABSTRACT:
Indoles of structural formula (III): ##STR1## are synthesized by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline and an alkyl ketone derivative. The process is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a facile leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride.

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