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Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines

Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines description/claims

This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.

Certain 4-anilino-benzo[g]quinoline-3-carbonitriles as protein kinase inhibitors are disclosed in PCT patent application WO0147892.

Certain 4-anilino-benzo[g]quinazolines as protein kinase inhibitors are disclosed in several patents and publications: WO9749688, U.S. Pat. No. 5,679,683, WO9519970, WO9713760 and J. Med. Chem. 1996, 39, 918-928. These references disclose that 4 anilino-benzo[g]quinazolines and 4-anilino-benzo[g]quinoline-3-carbonitriles possess potent activity as protein kinase inhibitors.

Throughout this patent application, the benzo[g]quinoline ring system will be numbered as indicated in the formula below:

Throughout this patent application, the benzo[g]quinazoline ring system will be numbered as indicated in the formula below:

The present invention relates to a process for the production of 6,7,8-substituted 3-amino-2-naphthoates or 3-amino-2-naphthonitriles of formula (A)

wherein

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Process for the synthesis of 9-hydroxy risperidone (paliperidone)
Industry Class:
Organic compounds -- part of the class 532-570 series

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