Process for the preparation of 3-glutamido bile ester derivatives using n-prtotected methyl proglutamate
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United States of America Patent
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Issued Date -
Jul 15, 2004
app pub date -
Mar 12, 2004
filing date -
Feb 5, 2001
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Abandoned
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Abstract
The present invention relates to a novel process for the preparation of bile esters derivatives of general formula (1), in which R.sub.0 is H or OH; R.sub.1 is H, .alpha.-OH or .beta.-OH; R.sub.2 and R.sub.3 are independently hydrogen, straight or branched (C.sub.1-C.sub.20) alkyl optionally substituted with aryl; R.sub.5 is a straight or branched (C.sub.1-C.sub.4) alkyl and R.sub.6 is a straight or branched (C.sub.1-C.sub.4) alkyl or a benzyl group, via transamidation of the amine (V) with the 5-ocoproline derivative (II), wherein R.sub.4 is selected from the group consisting of tertbutoxycarbonyl, methoxycarbonyl, ethoxycarbonyl, 2-trimethylsilylethoxycarbonyl, cyclobutoxycarbonyl and 1-methylcyclobutoxy carbonyl, followed by the selective cleavage of the protecting group R.sub.4 under acidic conditions.
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