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J Org Chem ; 76(20): 8262-9, 2011 Oct 21.
Article in English | MEDLINE | ID: mdl-21899258

ABSTRACT

A POCl(3)-mediated, direct amination reaction of heterocyclic amides/ureas with NH-heterocycles or N-substituted anilines is described. Compared to the existing methods, this operationally simple protocol provides unique reactivity and functional group compatibility because of the metal-free, acidic reaction conditions. The yields are generally excellent.


Subject(s)
Amides/chemistry , Chemistry, Pharmaceutical/methods , Heterocyclic Compounds/chemical synthesis , Prescription Drugs/chemical synthesis , Urea/chemistry , Amination , Aniline Compounds/chemistry , Anticholesteremic Agents/analysis , Anticholesteremic Agents/chemistry , Azabicyclo Compounds/analysis , Azabicyclo Compounds/chemistry , Benzamides , Catalysis , Erlotinib Hydrochloride , Eszopiclone , Fluorobenzenes/analysis , Fluorobenzenes/chemistry , Heterocyclic Compounds/analysis , Humans , Hydrogen-Ion Concentration , Hypnotics and Sedatives/analysis , Hypnotics and Sedatives/chemistry , Hypoglycemic Agents/analysis , Hypoglycemic Agents/chemistry , Imatinib Mesylate , Molecular Structure , Phosphorus Compounds/chemistry , Piperazines/analysis , Piperazines/chemistry , Prescription Drugs/analysis , Protein Kinase Inhibitors/analysis , Protein Kinase Inhibitors/chemistry , Pyrimidines/analysis , Pyrimidines/chemistry , Quinazolines/analysis , Quinazolines/chemistry , Rosiglitazone , Rosuvastatin Calcium , Sulfonamides/analysis , Sulfonamides/chemistry , Thiazolidinediones/analysis , Thiazolidinediones/chemistry , Urea/analogs & derivatives
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