Phenylbutanol derivatives and compositions containing them

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...

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260140, 2604299, 260465F, 260469, 2605011, 26050118, 2605012, 260520B, 260544D, 260559D, 260599, 260613R, 260613B, 560 59, 560 61, 560255, 560 62, C07C 6976

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040498239

ABSTRACT:
Phenylbutanol derivatives of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --Y wherein Z is 4-biphenyl or 4-phenoxyphenyl wherein the phenoxy group is unsubstituted or substituted by F, Cl or Br and Y is COOR.sup.2 or CH.sub.2 OR.sup.3 wherein R.sup.2 is H or alkyl of 1 to 6 carbon atoms and R.sup.3 is H or alkanoyl of 1 to 6 carbon atoms, and their physiologically acceptable salts, possess anti-inflammatory activity and are produced by (a) treating with a solvolyzing agent a compound of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --W or Z--CX(CH.sub.3)--CH.sub.2 --Y wherein W is a functionally modified carboxy or methylol group different from Y and X is Cl, Br or I or a functionally modified hydroxyl group; or (b) reducing a compound otherwise corresponding to a desired final product but having instead of one of the hydrogen atoms a group which can be reduced or replaced by a hydrogen atom; or (c) oxidizing a compound otherwise corresponding to a desired final product but lacking the tertiary hydroxyl group; or (d) converting a compound otherwise corresponding to a desired final product wherein Z is a 4-phenoxyphenyl group but having instead a 4--OH--, Cl--, Br-- or I-substituted phenyl group into a desired final product; or (e) diazotizing a compound otherwise corresponding to a desired final product wherein Z is a halogen-substituted 4-phenoxyphenyl group but having an --NH.sub.2 -substituted phenoxy group and reacting the resulting diazonium salt with a halogenating agent.

REFERENCES:
Barron, J. D. et al., J. Med. Chem. 1968, 11(6) 1139-1144.

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