- METHOD FOR PRODUCING FLUORINATED PROLINE DERIVATIVE
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Disclosed is a method for efficiently producing a high-purity fluorinated proline derivative with high yield. Specifically disclosed is a method for producing a compound represented by the general formula (2) below wherein a compound represented by the formula (1) below is reacted with a fluorination agent, and then chlorine, bromine, iodine, hypochlorous acid, hypochlorite, hypobromous acid, hypobromite or N-halogenosuccinimide is caused to act on the reaction product obtained by the preceding reaction and containing the compound represented by the general formula (2) below and a by-product for chemically changing the by-product. (1) (In the formula (1), R1 represents an unsubstituted or substituted alkyl group having 1-6 carbon atoms or the like; R2 represents an unsubstituted or substituted alkyl group having 1-6 carbon atoms or the like; and R3 represents a hydroxyl group or the like.) (2) (In the formula (2), R1 and R2 are as defined above.)
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Page/Page column 36-38
(2008/06/13)
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- Synthetic studies toward astins A, B and C. Efficient syntheses of cis- 3,4-dihydroxyprolines and (-)-(3S,4R)-dichloroproline esters
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Efficient syntheses of the esters of cis-3,4-dihydroxyprolines and the first synthesis of the ester of the rare amino acid (-)-(3S,4R)- dichloroproline from trans-4-hydroxy-L-proline are presented. The synthetic route provides easy access to several substituted prolines and cis- hydroxylated proline esters. Various types of biological activities have been associated with these substituted prolines. The role of (-)-(3S,4R)- dichloroproline in astins A, B and C is under investigation.
- Schumacher, Kelly K.,Jiang, Jianjun,Joullie, Madeleine M.
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