2-AMINO-7-(1-SUBSTITUTED-2-HYDROXYETHYL)-3,5-DIHYDRO-PYRROLO 3,2-D PYRIMIDIN-4-ONES

The compounds of formula I wherein Ar represents biaryl, carbocyclic or heterocyclic aryl, are prepared, as substantially pure enantiomers, by (a) condensing a compound of the formula as a substantially pure enantiomer, wherein Ar has meaning as defined above and R6 is on O-protecting group with a l...

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Bibliographic Details
Main Authors MUGRAGE, BENJAMIN, BIRO, VAN DUZER, JOHN, HENRY, MCQUIRE, LESLIE, WIGHTON
Format Patent
LanguageEnglish
French
German
Published 22.03.2000
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The compounds of formula I wherein Ar represents biaryl, carbocyclic or heterocyclic aryl, are prepared, as substantially pure enantiomers, by (a) condensing a compound of the formula as a substantially pure enantiomer, wherein Ar has meaning as defined above and R6 is on O-protecting group with a lower alkyl ester of formic acid; (b) then condensing the compound so obtained with a compound of the formula wherein R8 is hydrogen or COOR3and R3 is lower alkyl; (c) then cyclizing the compound so obtained to a compound of the formula as a substantially pure enantiomer; (d) and then condensing the compound so obtained (1) with a carbocyclic aroyl isothiocyanate and treatment of the product so obtained with an alkyl halide followed by anhydrous ammonia; or (2) with cyanamide in acid, optionally followed by treatment with a base.
Bibliography:Application Number: EP19980932088