Preparation of ethambutol-diisoniazide methane sulfonic acid sal

Details Preparation of ethambutol-diisoniazide methane sulfonic acid sal Preparation of ethambutol-diisoniazide methane sulfonic acid sal

1982-06-10

1984-05-22

Jiles, Henry R.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546324, C07D40112

Patent

active

044502745

ABSTRACT:
This invention pertains to a new process for preparing an ethambutol-sulfonic acid derivative which is widely used as an antituberculosis agent. In the known process, there are many defects which include: side reactions, impurities, low yield, high cost production inefficiency and pollution hazard.
For the purpose of preparing an ethambutol-sulfonic acid derivative of a higher purity and higher yield than the known process, ethambutol or its hydrogen chloride salt is reacted with chloromethane sulfonic acid or its sodium salt in the lower alcoholic solvent such as methanol, ethanol, propanol, or isopropanol, at a temperature between room temperature and boiling point of the solvent, for about an hour, to produce ethambutol-chloromethane-sulfonate which is then reacted with isoniazid to produce the ethambutol-sulfonic acid derivative of the present invention.

REFERENCES:
patent: 3718655 (1973-02-01), Ferrer-Salat et al.

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