General and mild preparation of 2-aminopyridines.
A general and facile one-pot amination procedure for the synthesis of 2-aminopyridines from the corresponding pyridine-N-oxides is presented as a mild alternative to S(N)Ar chemistry. A variety of amines and heterocyclic-N-oxides participate effectively in this transformation which uses the phosphonium salt, PyBroP, as a means of substrate activation.
CVMED Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, Connecticut 06340, United States. allyn.t.londregan@pfizer.com
Allyn T
AT
Londregan
Sandra
S
Jennings
Liuqing
L
Wei
D000586:Amination; D000588:Amines / Q000737:chemistry*; D000631:Aminopyridines / Q000138:chemical synthesis* / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques; D015394:Molecular Structure; D009943:Organophosphorus Compounds / Q000737:chemistry; D011725:Pyridines / Q000737:chemistry*
D000588:Amines; D000631:Aminopyridines; D009943:Organophosphorus Compounds; D011725:Pyridines; C013229:pyridine N-oxide; C032439:alpha-aminopyridine