Synthesis of 7-benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine and novel derivatives free of positional isomers. Potent inhibitors of cAMP-specific …
…, D Marko, T Regiert, G Reiss, W Frank…
文献索引:Merz, Karl-Heinz; Marko, Doris; Regiert, Thomas; Reiss, Guido; Frank, Walter; Eisenbrand, Gerhard Journal of Medicinal Chemistry, 1998 , vol. 41, # 24 p. 4733 - 4743
7-Benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine (7a) is a potent inhibitor of the cAMP-specific phosphodiesterase isoenzyme family PDE4 and induces growth inhibition in a panel of tumor cell lines. In this study, we describe a synthesis that yields 7a and novel derivatives free of positional isomers. The synthesis of alkylamino substituted pteridines is based on the successive nucleophilic aromatic substitution of the chlorine atoms of 2, 4, 6, ...