1',2'-Diacyl-(6R,S)-5,6,7,8-tetrahydro-L-biopterin and process f

Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system


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C07D47504, A61K 31495




A novel compound, 1',2'-diacyl-(6R,S)-5,6,7,8-tetrahydro-L-biopterin which is prepared by catalytical hydrogenation of a 1',2'-diacyl-L-biopterin in a solvent in the presence of a catalyst. The 1',2'-diacyl-L-biopterin is prepared from a 1,1-dialkylsulfonyl-L-rhamnose through an acyl derivative of 5-deoxy-L-arabinose and a hydrazine derivative of tetrahydro-L-biopterin without isolating the intermediate products. The 1', 2'-diacyl-(6R,S)-5,6,7,8-tetrahydro-L-biopterin can be used for treatment of atypical phenylketonuria or dihydropterin-reductase deficiency and can readily cross the blood brain barrier without neurotransmitter precursors.

patent: 3505329 (1970-04-01), Weinstock
Helvetica Chimica Acta, 60(1), pp. 211-214 (1977) by Max Viscontini et al.
Helvetica Chimica Acta, 61(7), p. 2731 (1978) by Max Viscontini et al.
Bernhard Schircks, "Neue regiospezifische Synthese von L-Biopterin und von dessen Derivaten" (Dissertation-Zurich, 1978) pp. 34-37, 69-75.


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