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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 5
BKCSDE 29(5)
May 20, 2008 

Effective Amidation of Carboxylic Acids Using
(4,5-Dichloro-6-oxo-6H-pyridazin-1-yl)phosphoric Acid Diethyl Ester
Seung-Beom Kang, Heung-Seop Yim, Ju-Eun Won, Min-Jung Kim, Jeum-Jong Kim, Ho-Kyun Kim, Sang-Gyeong Lee*, Yong-Jin Yoon*
(4,5-Dichloro-6-oxo-6H-pyridazin-1-yl)phosphoric acid diethyl ester, Coupling agent, Pyridazinone,
Amidation, Dipeptide
(4,5-Dichloro-6-oxo-6H-pyridazin-1-yl)phosphoric acid diethyl ester (3a) are efficient and selective coupling agents for the amidation of carboxylic acids. Amidation of aliphatic and aromatic carboxylic acids with aliphatic and aromatic amines using 3a under mild condition gave chemoselectively the corresponding amides in good to excellent yield. Three protected-dipeptides were also synthesized from N-BOC-Phe and O-Meamino acid hydrochlorides using 3a under mild condition.
1025 - 1032
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