1,2-Diphenyl-3,5-ditrifluoroacetyloxy-4-butyl-5-hydroxy-3-pyrazo

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

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C07D23108

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active

041397096

ABSTRACT:
The compound 1,2-Diphenyl-3,5-ditrifluoroacetyloxy-4-butyl-5-hydroxy-3-pyrazoline is disclosed as an intermediate useful in the preparation of selected pro-phenylbutazone derivatives.
Such selected pro-phenylbutazone derivatives are novel, transient, pro-drug forms of phenylbutazone and oxyphenbutazone having the following formulae wherein R, R.sub.2, R.sub.4, R.sub.5, X and Y are as defined herein: ##STR1## The above-identified compounds exhibit anti-inflammatory activity in warm-blooded animals. Upon administration to warm-blooded animals, these compounds pass through the gastrointenstinal tract and cleave in the bloodstream, thus releasing phenylbutazone or oxyphenbutazone in an anti-inflammatory effective amount at their therapeutic site or sites of activity.

REFERENCES:
patent: 3847936 (1974-11-01), Adolphi et al.
Sloan et al., J. Org. Chem., 1976, vol. 41, pp. 165-166.
Sala et al., Chimie Therapeutique, 1967, No. 4, 272-276.
Sloan et al., Chem. Absts., vol. 84, 1976, 43929m.
Chem. Absts., vol. 84, 1976, p. 44336, col. 2.

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