C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/242.01
C07D 471/04 (2006.01)
Patent
CA 1140124
A b s t r a c t The invention concerns a new process for the preparation of nitrogen bridgehead condensed pyrimidine compounds of the general formula Image I (wherein R represents hydrogen or lower alkyl; R1 represents hydrogen, lower alkyl, carboxy or a derivative thereof or styryl; R2 represents hydrogen, optionally substituted lower alkyl; R3 represents hydrogen, optionally substituted substituted lower alkyl, aryl, aralkyl, halogen, carboxy or a derivative thereof, the group -(CH2)m-COOH (in which m is the integer 1, 2 or 3) or a carboxy derivative thereof, formyl, lower alkanoyl or a condensed derivative thereof; R4 represents hydrogen, optionally substituted alkyl, aryl optionally substituted by one or more substituents, optionally substituted aralkyl, a heterocyclic group optionally substituted by one or more substituents, the group -(CH2)m-Het (m is the integer 1, 2 or 3) Het is an optionally substituted heterocyclic group); R5 represents hydrogen C1-6 alkyl, aryl optionally substituted by one or more substituents, formyl, lower alkanoyl, optionally substituted aroyl or hetero- aroyl; or R4 and R5 together with the nitrogen therebetween represent an optionally substituted mono- or bicyclic heterocyclic ring, optionally containing further heteroatom) and pharmaceutically acceptable salts, hydrates, stereoisomers, optically active and geometric isomers and tautomers thereof, which comprises reacting a racemic or optically active compound of the general formula Image II (wherein R, R1, R2 and R3 are as defined above and X represents halogen) with a compound of the general formula Image III wherein R4 and R5 are as hereinbefore defined) or an acid addition salt thereof. Compounds of the general formula I wherein a) R3 represents aralkyl or halogen and R, R1 , R2 , R4 and R5 have the same meaning as defined above or b) R4 represents the group -(CH2)m-Het (m is the integer 1, 2 or 3 and Het represents an optionally substituted heterocyclic group) and R, R1, R2 , R3 and R5 have the same meaning as defined above) and pharmaceutically acceptable salts, hydrates, stereoisomers, optically active and geometric isomers and tautomers thereof are also included. The compounds of formula I possess interesting physiological properties, part- icularly antiallergic and/or antiasthmatic activity.
351664
Breining Tibor
Hermecz Istvan
Horvath Agnes
Kokosi Jozsef
Vasvari Lelle (nee Debreczy)
Chinoin Gyogyszer - Es Vegyeszeti Termekek Gyara Rt.
Fetherstonhaugh & Co.
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