Microcrystalline 3-(alpha-acetonylbenzyl)-4-hydroxycoumarin (war

Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal

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424281, C07D31120

Patent

active

041137442

ABSTRACT:
Microcrystalline 3-(alpha-acetonylbenzyl)-4-hydroxy coumarin (warfarin), having a crystal size not greater than 4.0 microns, is stable for long periods of time, is advantageous in that it is rapidly absorbed from the gastrointestinal tract and thus provides a highly desirable level of bioavailability not previously possible. It is crystallized from a buffered alkaline solution of warfarin by acidification thereof. Compositions thereof are useful for anticoagulant and rodenticide purposes, and methods of making such compositions and of using the new microcrystalline form of warfarin for such purposes are disclosed.

REFERENCES:
patent: 2666064 (1954-01-01), Starr et al.
patent: 2752360 (1956-06-01), Starr et al.
patent: 2777859 (1957-01-01), Link
patent: 2932652 (1960-04-01), Molnar
United States Pharmacopeia, XVIII, p. 675-676, (1970).
The Van Nostrand Chemist's Dictionary, (1953), p. 105.
Pauling, College Chemistry, 3rd Ed., (1964), pp. 537-539.

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