Process for preparing N-9 substituted analogs of purine

摘要

Method for preparing N-9 substituted purine analogues of formula (III) wherein Z is H or amino, Q is amino, alkylamino C.sub.1-15.n., Dialkylamine C.sub.1-15.n., Heterocyclic amine, arylamine, diarylamine, hydroxy, alkoxy C.sub.1-15.n., thio. alkylthoskupina C.sub.1-15.n.nebo azido and Ri1 C.sub.1-15.n alkyl., alkenyl C.sub.1-15.n., alkynyl C. sub.1-15.n., cycloalkyl C.sub.3-10.n., cykloalenkyl C.sub.3-10.n., aryl or heteroaryl, wherein in a first step, a primary amine or diamine Ri1 is a substituent, as described above, or a salt thereof as the substrate allowed to react with the reagent, the pyrimidine precursor of formula I wherein Z is H or an amino group, in a suitable solvent in the presence of non-nucleophilic base, for heating, thus to the amino group of the substrate to the gradual construction purine base which is substituted 6-chloropurine of formula II wherein the substituents Z and R1 are as described above , wherein the nitrogen atom of such amino happens positions N-9 caused nucleobase; in a second step the reaction mixture without isolation of the intermediate chlorpurinového added nucleophilic reagent and the resulting substituted analogue chloropurine of formula III is subsequently separated. Reaction intermediate, 9-substituted-6-chloropurine, may also without performing a second reaction step directly obtained from the crude reaction mixture. Compounds of formula II are intermediates for the production of medicaments, compounds of formula III are useful as pharmaceuticals.