Imperial Chemical Industries Limited

Zeneca Limited

Stanley A Lee

Andrew Peter Thomas

Lyn Powell

David M Martin

Gregory D Harris

The invention provides a novel chemical process for the manufacture of quinoline, pyridine and imidazole derivatives of the formula IV wherein Q, Y.sup.1 and Y.sup.2 have the various meanings defined herein, and their non-toxic salts, which are angiotensin II inhibitors. The process involves the removal of an electron-deficient phenyl group or a pyridyl or pyrimidyl group from a compound of the formula VI as defined herein. Certain of the intermediates are novel and are provided as a further feature of the invention.

Biphenyl-tetrazole intermediate compounds

The invention provides a novel chemical process for the manufacture of certain imidazo[4,5-b]pyridine derivatives of the formula I wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the various meanings defined herein, and their non-toxic salts, which are angiotensin II inhibitors. The process involves the removal of an electron-deficient phenyl group or a pyridyl or pyrimidyl group from a compound of the formula II as defined herein. Certain of the intermediates are novel and are provided as a further feature of the invention.

Chemical process and intermediates used therein

The invention provides a novel chemical process for the manufacture of quinoline, pyridine and imidazole derivatives of the formula IV wherein Q, Y.sup.1 and Y.sup.2 have the various meanings defined herein, and their non-toxic salts, which are angiotensin II inhibitors. The process involves the removal of an electron-deficient phenyl group or a pyridyl or pyrimidyl group from a compound of the formula VI as defined herein.

Chemical process for making angiotesin II antagonist compounds

A process for the manufacture of trifluoroacetaldehyde, or a hydrate or hemiacetal thereof, which comprises reduction of an ester of trifluoroacetic acid with a borohydride reducing agent in a hydroxylic solvent to form trifluoroacetaldehyde hydrate or hemiacetal; whereafter if the free aldehyde is required, water or alcohol is removed from the hydrate or hemiacetal respectively using conventional procedures.

Chemical process for manufacturing trifluoroacetaldehyde hydrate or

The invention concerns novel boron compounds of the formula IV, in which Q, Y.sup.1, G.sup.1 and G.sup.2 have the various meanings defined herein, and their acid and base addition salts. The said compounds are useful in the manufacture of certain quinoline, pyridine and imidazole derivatives which have angiotensin II inhibitory activity. The invention also provides novel processes for the production of the quinoline, pyridine and imidazole derivatives. ##STR1##

Heterocyclic boron compounds as intermediates for angiotensin II

The invention concerns a novel process for the manufacture of various aryloxyaliphatic aldehydes and related arylthio analogues, which are useful as chemical intermediates. The process involves reacting a dihalogenohydroxyalkane of the formula: HO.C(R.sup.2).sub.2.CHX.sub.2 wherein R.sup.2 is alkyl and X is chloro or bromo with a phenol or thiophenol in the presence of base and is applicable to large scale use.

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Macclesfield, United Kingdom

Stanley A Lee