Process for the preparation of a tetrazole derivative in two cry

Details Process for the preparation of a tetrazole derivative in two cry Process for the preparation of a tetrazole derivative in two cry

1995-10-17

1997-05-13

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548253, 5483007, A61K 31415, C07D40310

Patent

active

056293313

ABSTRACT:
The present invention relates to a process for the preparation of the 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro [4.4]-non-1-en-4-one by reaction of the corresponding nitrile with an alkaline azide and triethylamine hydrochloride, recovering the 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4]n on-1-en-4-one in form of one of its alkaline salts in aqueous solution, by neutralization of said alkaline salt and crystallization of the 2-n.butyl-3-[[2'-(tetrazol-5-yl)-biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4] non-1-en-4-one thus precipitated either in a solvent containing less than 10% of water or in a solvent containing more than 10% of water in order to obtain two differents crystalline forms. Furthermore a novel crystalline form of 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4] non-1-en-4-one and pharmaceutical compositions containing it are described.

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