High-yielding two-step synthesis of 6,8-disubstituted N-9-unprotected purines.
We report herein a convenient method for the synthesis of libraries of 6,8-disubstituted-9-H-purines in two steps, including cyclization of 6-chloro-4,5-diaminopyrimidine with various arylcarboxylic acids or chlorides, followed by S(N)Ar with amines and alkoxides or Pd-catalyzed amidations at C-6. These reactions were highly efficient and allowed the synthesis of a 32-member library of 6,8-disubstituted purines.
Ibrahim
Nada
N
UMR 176, Institut Curie, Bâtiment 110-112, Centre Universitaire, Orsay, France.
Legraverend
Michel
M
D002384:Catalysis; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D003500:Cyclization; D010165:Palladium / Q000737:chemistry; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry
D011687:Purines; D010165:Palladium