83709-59-5

Upstream product

• 22150-76-1 biopterin 
• 858127-57-8 (3S,4S)-1-amino-3,4-dihydroxy-2-pentanone 

Downstream Products

• 102340-67-0 p-quinonoid (6R)-dihydrobiopterin hydrochloride 
• 1041007-05-9 (R)-2-amino-6-((1R,2S)-1,2-dihydroxypropyl)-4-oxo-4,6,7,8-tetrahydro-3H-pteridine-5-carboxylic acid benzyl ester 

Relevant academic research and scientific papers

Chemical synthesis and purification method of biopterin (by machine translation)

The method, uses diacetyl biopterin as a raw material, to hydrolyze, with diacetyl biopterin to obtain the salpterin crude, obtained by extracting,hydrogenated,acid after the hydrolysis reaction time is short. and obtaining the methotrexate crude product, according to the method . The method is short in production cycle, cost, and suitable for industrial production. after recrystallization of the mixed solution . The method is simple,efficient, % by weight of the methotrexate aqueous solution obtained by. the method. (by machine translation)

METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE

Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.

METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE

Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.

METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE

Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.

METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE

Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.

PROCESSES FOR PREPARING TETRAHYDROBIOPTERIN, AND ANALOGS OF TETRAHYDROBIOPTERIN

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.

Pterins. VIII. The Absolute Configuration at C 6 of Natural 2-Amino-6--5,6,7,8-tetrahydropteridin-4(3H)-one (L-erythro-5,6,7,8-tetrahydrobiopterin)

The conformation of the side chain of 5,6,7,8-tetrahydrobiopterin (6) in 0.5 M DCl/D2O is predominantly quasi-equatorial (deduced from 3J (13C 4a, 1H 6) 1.1 Hz), and is the same as that of the methyl group in 2-methyl-1,2,3,4-tetrahydroquinoxaline and in 2-amino-6-methyl-5,6,7,8-tetrahydropteridin-4(3H)-one in the same solvent.Because (-)-2S)-2-methyl-1,2,3,4-tetrahydroquinoxaline (4) and (-)-(6S)-2-amino-6-methyl-5,6,7,8-tetrahydropteridin-4(3H)-one (5) have the same conformation and negative c.d. spectra (Θ 248 nm and 263 nm respectively) as does the natural 5,6,7,8-tetrahydrobiopterin (Θ minimum at 265 nm) in 0.1 M hydrochloric acid, then the absolute conformations of the tetrahydropyrazine rings and the absolute configurations at the chiral crntres C2, C6, and C6 of compounds (4),(5) and (6) respectively are the same.Hence the absolute configuration at C6 in natural 5,6,7,8-tetrahydrobiopterin is R.A convenient synthesis of biopterrin on a gram scale is described.