专利号:US-8809553-B2 优先权日:2010-06-15 标题:Process for the preparation of pteridine derivatives 发明人:ATTOLINO EMANUELE; MICHIELETTI MARIO; ROSSI DAVIDE; ALLEGRINI PIETRO 权利人:ATTOLINO EMANUELE; MICHIELETTI MARIO; ROSSI DAVIDE; ALLEGRINI PIETRO; DIPHARMA FRANCIS SRL 摘要:The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.
专利号:US-3505329-A 优先权日:1968-02-06 标题 :Process for the synthesis of biopterin 发明人:WEINSTOCK JOSEPH 权利人:SMITHKLINE CORP
专利号:US-9365573-B2 优先权日:2012-04-10 标题:Method for synthesizing sapropterin dihydrochloride 发明人:HONG HAO; GAGE JAMES; CHEN CHAOYONG; LU JIANGPING; ZHOU YAN; LIU SHUANGYONG 权利人:ASYMCHEM LAB TIANJIN CO LTD; ASYMCHEM LIFE SCIENCE TIANJIN CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LAB FUXIN CO LTD; JILIN ASYMCHEM LAB CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD 摘要: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.
专利号:US-9371326-B2 优先权日:2012-04-10 标题 :Method for synthesizing sapropterin dihydrochloride 发明人:HONG HAO; GAGE JAMES; CHEN CHAOYONG; LU JIANGPING; ZHOU YAN; LIU SHUANGYONG 权利人:ASYMCHEM LAB TIANJIN CO LTD; ASYMCHEM LIFE SCIENCE TIANJIN CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LAB FUXIN CO LTD; JILIN ASYMCHEM LAB CO LTD; JILIN ASYMCHEM LAB CO LTD 摘要: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.