Process for N5-formylating tetrahydropteridines

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United States of America Patent

PATENT NO 5198547
SERIAL NO

07851733

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Abstract

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Intermediates and a process for the synthesis of 6-monosubstituted tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolic acid. The intermediates are shown in their two enantiomeric forms as follows: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, methyl, hydroxy, amino, alkyl or dialkylamino, alkoxy, benzyloxy, or benzylthio; R.sub.3 represents an alkene, alkyne, cycloalkyl, benzyl, alkyl (substituted with hydroxy, acetoxy, benzyloxy, alkoxy, alkylthio, amino, carboxy, oxo, or phosphate), a protected aldehyde, or ##STR2## wherein n=1 or 2, R.sub.4 is hydrogen, formyl, methyl, or propargyl, and ZZ represents an amino acid or amino acid polymer. Also, a process for tetrahydropteridine N5-formylation for the preparation of, for example, N5-formyl-(6S)-tetrahydrofolic acid.

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Patent Owner(s)

Patent OwnerAddress
SOUTH ALABAMA MEDICAL SCIENCE FOUNDATION307 UNIVERSITY BLVD BOX U-1060 MOBILE AL 36527

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Ayling, June E Mobile, AL 14 193
Bailey, Steven W Mobile, AL 16 225

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