Method of synthesizing tetrahydrobiopterin

The present disclosure provides a method that efficiently produces (6R)-tetrahydrobiopterin in high yield and purity. The method includes the step of hydrolyzing diacetylbiopterin to biopterin under basic conditions in a biphasic mixture comprising an organic phase and an aqueous phase. After substa...

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Main Authors ROIDL, GABRIELE, BAFFI, ROBERT, MUELLER, CHRISTIAN, KAISER, STEFAN, HENDERSON, MARK, JUNGLES, STEVEN, INDOLESE, ADRIANO, SCHMIDT, PHILIPP
Format Patent
LanguageChinese
English
Published 16.10.2009
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The present disclosure provides a method that efficiently produces (6R)-tetrahydrobiopterin in high yield and purity. The method includes the step of hydrolyzing diacetylbiopterin to biopterin under basic conditions in a biphasic mixture comprising an organic phase and an aqueous phase. After substantially complete hydrolysis of diacetylbiopterin, the aqueous phase containing biopterin can be separated from the organic phase containing most of the organic impurities, which avoids the time-consuming step of isolating biopterin as a solid. The aqueous solution containing biopterin is stereoselectively hydrogenated to (6R)-tetrahydrobiopterin under basic conditions and high hydrogen pressure in the presence of a metal catalyst (e. g., a platinum catalyst). To improve the purification of an acid addition salt of (6R)-tetrahydrobiopterin (e. g., (6R)-tetrahydrobiopterin dihydrochloride), any residual salts (e. g., sodium salts) in the aqueous solution after the hydrogenation reaction can be removed by contacting t
Bibliography:Application Number: TW200998100222