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US 6,143,900 AGranted
Stereoselective synthesis of oxazoline derivative
AssigneeDong Kook Pharmaceutical Co., Ltd.
InventorsWon Hun Ham, Kyung Seok Choi, Han Won Lee, Sung Ki Seo, Jin Kyu Park, Ki Young Lee, Yong Hyun Kim
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Abstract
The present invention relates to stereoselective synthetic method of oxazoline derivative. More particularly, it relates to a synthetic method of oxazoline derivative having the structure of formula I. ##STR1## wherein R represents phenyl, benzyl, methyl, ethyl, isopropyl, isobutyl, cyclohexyl or cyclohexylmethyl.
Claims4
A stereoselective synthetic method of oxazoline derivative comprising the steps of;
- i) cyclizing the compound of formula II in the presence of 0.02.about.0.1 mole % of palladium (Pd) catalyst at 20.about.50.degree. C. by separating the leaving group X to obtain the compound of formula III;
- and
- ii) oxidizing the compound of formula III by adding the oxidizing agent in the mixed solvent (acetonitrile/carbontetrachloride/water) in the presence of ruthenium catalyst to obtain the compound of formula I ##STR7## wherein R represents phenyl, benzyl, methyl, ethyl, isopropyl, isobutyl, cyclohexyl or cyclohexylmethyl;
- X represents acetyl, benzoyl or carbonate as leaving group.
1 more element
Dependencies are inferred from the claim text.