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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 23, Number 2
BKCSDE 23(2)
February 20, 2002 

A Convergent Synthesis of Bis-2-oxo Amide Triacylglycerol Analogues as Potent Lipase Inhibitors Using Acyl Cyanophosphorane Methodology
Kieseung Lee
Lipase inhibitors, Bis-2-oxo amide triacylglycerol, a-Keto amide, Cyano triphenylphosphorane.
A number of bis-2-oxo amide triacylglycerol analogues, a recently reported potent human gastric lipase inhibitor and its new analogues, have been prepared starting from 1,3-dibromo-2-propanol utilizing acyl cyanophosphorane methodology as a key step in a convergent manner. The key coupling reaction has been accomplished at -78℃ between 1,3-diamino-2-propanol derivative and the labile diketo nitriles, derived from acyl cyanotriphenylphosphoranes upon oxidizing with O3, under mild condition in moderate yields.
351 - 354
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