Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Stanley H Wright

Charles G Caldwell

Milton L Hammond

Ihor E Kopka

Robert A Zambias

Peter G Houghton

Ramon John Alabaster

Compounds of formula III: ##STR1## wherein R.sup.1 is a 5- or 6-membered aromatic heterocyclic group; and R.sup.4 and R.sup.5 each idependently signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl; are useful intermediates in a novel process for the preparation of a class of pharmacologically active compounds of formula I: ##STR2## wherein R.sup.1, R.sup.4 and R.sup.5 are as defined above; and R.sup.3 represents hydrogen or lower alkyl.

Benzoxazepinone process

Novel position-4 and/or position-6 substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs of the following general structural formula (I) are disclosed: ##STR1## These compounds are found to be potent inhibitors of leukotriene biosynthesis.

6-substituted 5-hydroxy-2,3-dihydrobenzofurans as inhibitors of

Resolution of the .alpha. and .beta. isomers of .alpha.-pivaloyloxyethyl-(S)-3-(3,6-dihydroxyphenyl)-2-methylalaninate is accomplished by; (a) forming the (+) hydrogen tartrate salt of the mixture; (b) fractionally crystallizing the .beta.-isomer salt; and (c) recovering the .alpha.-isomer from the mother liquor by treatment with first a base and second a mineral acid.

Resolution of

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Sawbridgeworth, United Kingdom

Stanley H Wright