Process for the preparation of new phenol derivatives

Details Process for the preparation of new phenol derivatives Process for the preparation of new phenol derivatives

C - Chemistry, Metallurgy

07

C

167/179, 260/559

C07C 65/00 (2006.01) A61K 31/00 (2006.01) C07C 39/18 (2006.01) C07C 39/19 (2006.01) C07C 39/23 (2006.01) C07C 43/23 (2006.01) C07C 65/01 (2006.01) C07C 69/84 (2006.01) C07F 7/18 (2006.01) C07F 9/54 (2006.01)

Patent

CA 1272723

ABSTRACT A process for the preparation of new phenol derivatives of the general formula Image wherein A and B have the same or different meanings and each represents one of the groups -C?C-, cis-CH=CH- or trans-CH=CH-, R1 is hydrogen, an optionally substituted alkyl or phenyl radical or a cycloalkyl group, R2 is hydrogen, methyl or ethyl, R3 represents hydrogen, acetyl or propionyl, R4 has the same meaning as R3 or represents an alkyl group, R5 is a carboxylic or a hydroxy group or a functional derivative of such groups or R5 is a nitril group and R6 is hydrogen, an alkyl group or the group OR4 is disclosed. These compounds are prepared by reacting suitable acety- lene compounds or metal derivatives thereof with e.g. alkyl or aryl halides, optionally in presence of palladium and copper(I)catalysts or by means of Wittig reactions followed, for instance, by transforming the member R5 in an other carboxylic acid derivative, if desired. By hydrogenation A and B may be varied within the scope of the definition. The compounds of formula I specifically inhibit 5-lipoxygenase and thus are valuable ingredients of pharmaceutical compositions for pro- phylaxis and treatment of diseases due to the action of leukotrienes.

505690

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