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