Method for sulfonation of 1,2-benzisoxazole-3-acetic acid

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

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11531364

ABSTRACT:
An efficient method for the preparation of 1,2-benzisoxazole-3-methanesulfonic acid involves a reaction of 1,2-benzisoxazole-3-acetic acid in toluene with chlorosulfonic acid optionally mixed with an inert solvent in the presence of a particular Lewis base (ester or a nitrile).

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Hitoshi Uno et al., “Studies of 3-substituted 1,2-benzisoxazole drivatives. 6. synthesis of 3-(sulfamoylmethyl)-1,2-benzisoxazole derivatives and their anticonvulsant activities,” Journal of Medicinal Chemistry, vol. 22, No. 2, pp. 180-183 (1979).
S. Patai and Z. Rappoport, “The chemistry of sulphonic acids, esters and their derivatives,” pp. 354-355 (1991), John Willy & Sons.
Hitoshi Uno et al., “Studies on 3-substituted 1,2-benzisoxazole derivatives. V. electrophilic substituions of 1,2-benzisoxazole-3-acetic acid,” Chem. Pharm. Bull., vol. 26, No. 11, pp. 3498-3503 (1978).

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