Process for regioselective substitution of trifluorobenzoate or

Details Process for regioselective substitution of trifluorobenzoate or Process for regioselective substitution of trifluorobenzoate or

1997-02-27

1998-07-07

Ivy, C. Warren

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

514327, 514331, 546230, 546238, C07D21144, A61K 31445

Patent

active

057771235

ABSTRACT:
The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

REFERENCES:
patent: 4684734 (1987-08-01), Kaieda et al.
patent: 5332851 (1994-07-01), Kumai et al.
Wells, K. M. et al.: Regioselective Nucleophilic Substitutions of Fluorobenzene Derivatives. Tetrahedron Letters. vol. 37, pp. 6439-6442, 1996.

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