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US 7,732,599 B2Granted
Process for preparing tetrahydrobiopterin and analogs of tetrahydrobiopterin
AssigneesBiomarin Pharmaceutical Inc., Merck Eprova AG
InventorsRudolf Moser, Viola Groehn, Andreas Schumacher, Pierre Martin, Dirk Spielvogel
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Abstract
Process for the preparation of tetrahydrobiopterin from neopterin and/or 6-substituted pterins with an improved yield and a high stereoselectivity. Also disclosed herein are novel individual intermediates prepared in the preparation of tetrahydrobiopterin, such as selectively protected neopterin useful for the preparation of tetrahydrobiopterin.
Claims7
A process for forming enantiomerically-enriched tetrahydrobiopterin (BH4) or a salt thereof from neopterin, comprising the steps of:
- (a) protecting the primary amine group at C-2 of neopterin with an amino protecting group;
- (b) converting the primary hydroxyl group of neopterin to a thioether;
- and
- (c) reducing the thioether of step (b) to a methyl group.
1 more element
Dependencies are inferred from the claim text.