Intermediates in the synthesis of novel (1-phenyl-1-heterocyclyl) methanol and (1-phenyl-1-heterocyclyl)methylamine derivatives
AssigneeAstra Aktiebolag
InventorsRobin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
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Abstract
Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo1,2-a!pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo1,2-a!pyridin-2-yl)-ben zimidazol-1-yl)-methyl!-biphenyl-2-carboxylic acid.
Claims1
A compound of formula (6) ##STR9## wherein X is O, S or Se;
- R.sub.1 is H, lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkyl or CF.sub.3 ;
- R.sub.2 is H, lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkyl or CF.sub.3 ;
- Ar is phenyl, furyl, thienyl, naphthyl, pyridyl or pyrrolyl, optionally substituted by R.sub.6 ;
- and
- R.sub.6 is one or more groups selected from lower alkyl, lower acyl, halogen, lower alkoxy, CF.sub.3, OH, NO.sub.2 or NR.sub.4 R.sub.5, wherein R.sub.4 and R.sub.5 independently are H, lower alkyl or lower acyl,
- with the provisos that when R.sub.1 and R.sub.2 are both hydrogen and Ar represents phenyl, then Ar is substituted by R.sub.6 ;
- and that the following five compounds are excluded:
- 2-methyl-5-thiazolyl phenyl ketone;
- phenyl 2-phenylmethyl-4-oxazolyl ketone;
- 4-bromophenyl 5-thiazolyl ketone;
- 4-methyl-5-thiazolyl phenyl ketone;
- and
- 4-methoxyphenyl 4-methyl-5-thiazolyl ketone.
Dependencies are inferred from the claim text.