Process and intermediates for preparing trans-4-substituted-S-prolines.

摘要

4-Substituted proline derivatives having the formula
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can be prepared by reacting the compound having the formula
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with a compound having the formula
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to obtain a compound having the formula
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<Chemistry id="chema05" num="0005"><Image id="ia05" he="26" wi="41" file="IMGA0005.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry></ListItem><ListItem>(a novel intermediate), converting that compound to a compound having the formula
<Chemistry id="chema06" num="0006"><Image id="ia06" he="17" wi="36" file="IMGA0006.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry></ListItem><ListItem>(a novel intermediate), and oxidizing that compound to yield the desired proline having the formula
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wherein R, is alkyl, cycloalkyl, aryl or arylalkyl, R<Sub>1</Sub>' is alkyl, cycloalkenyl, aryl or arylalkyl, R<Sub>2</Sub> is alkyl, aryl, arylalkyl or cycloalkyl and R<Sub>3</Sub> is hydrogen, alkyl, aryl, arylalkyl or cycloalkyl.