CAS: 69056-38-8; (R)-2-Amino-6-((1R,2S)-1,2-Dihydroxypropyl)-5,6,7,8-Tetrahydropteridin-4(1H)-One Dihydrochloride
该化合物是一种合成的自然生成的共生四氢生物素(BH4)的合成形式,主要用于苯丙酮尿(PKU)的治疗,一种代谢性紊乱,其特点是不能对苯丙烯酸盐进行代谢,该化合物作为药理学护身,加强了苯丙烯丙烯基羟基酶的活动,该酶是负责将苯丙烯转化为苯丙烯酸的酶.二氢氯酸盐是一种白的脱白晶状粉,可溶于水,适合口服.其化学配方反映二氢氯酸盐的形式,有助于其稳定性和溶性.该物质一般都具有良好的燃烧作用,包括头痛,胃肠扰动和过敏反应.作为治疗剂,它在管理血液苯丙酸盐水平方面发挥着至关重要的作用,从而防止与PKU相关的...
- 英文名称(R)-2-Amino-6-((1R,2S)-1,2-Dihydroxypropyl)-5,6,7,8-Tetrahydropteridin-4(1H)-One Dihydrochloride
- 中文名称(6R)-5,6,7,8-四氢生物蝶呤二盐酸盐
- IUPAC名称(R)-2-amino-6-((1R,2S)-1,2-dihydroxypropyl)-5,6,7,8-tetrahydropteridin-4(1H)-one dihydrochloride
- 其它别名Biopten (Tn); 4-Fluoro-Beta-Nitrostyrene, >=98.5% (Sum Of Isomers, Gc); Sapropterin Dihydrochloride (Usan); (6R)-2-Amino-6-[(1R,2S)-1,2-Dihydroxypropyl]-5,6,7,8-Tetrahydro-1H-Pteridin-4-One; Dihydrochloride; Sapropterin Hcl
- CAS编号69056-38-8
- MFCD编号:MFCD00891665
- EINECS号:663-669-3
- FDA UNII编号:RG277LF5B3
- 分子式:C9H17Cl2N5O3分子量:314.17
- 产品CID: 1685476
- 同类组份化合物CAS62989-33-7 (free base)69056-38-8 (HCl)90366-07-7 (sesqui HCl)17528-72-2 (free base)
- 产品分类Chemistry → Organic Building Blocks → Amines | Chemistry → Asymmetric Synthesis → Chiral Building Blocks | Amides | Alcohols | Inhibitors/Agonists → Metabolic Enzyme → Hydroxylase | Aliphatic Heterocycles
物理性质
- 熔点245-246° (dec)
- 沸点506.6±60.0 °C at 760 mmHg
- 闪点260.2±32.9 °C
- 密度1.9±0.1 g/cm3
- PH:D25 -6.81° (c = 0.665 in 0.1 M HCl)
- PSA:136.29
- LogP:-4.22
- 折射率1.822
- 蒸汽压0.0±3.0 mmHg at 25°C
- 溶解性Water, Oxygen Free: Soluble19.60 - 20.40mg/mL, Clear To Slightly Hazy, Colorless To Faintly Yellow
- 敏感性常温常压下稳定，远离氧化剂。
- 外观形态白色至类白色白色至类白色粉末
- 储存条件-20°C
- 产品应用该化合物用作4岁及4岁以上的成人和儿童,作为苯丙烯羟基酶,苯丙胺羟基苯基乙烯,乙酰羟基酰酶,三氯苯基羟基醚和硝氧化合成酶的天然共生物,并充当苯丙烷基羟乙烯的活体.
MSDS等安全信息
欧盟法规
C&L通报上下游产品
CAS号22150-76-1 L-生物喋呤合成工艺路线路线简述
海关参考信息
- 2905122000-异丙醇
2905310000-1,2-乙二醇
2905320000-1,2-丙二醇
2921211000-乙二胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:WO-2016101211-A1
优先权日:2014-12-25
标题 :Preparation method for sapropterin hydrochloride
发明人：WU FUJIAN
权利人:BEIJING CAVIR BIO PHARM CO LTD; SUZHOU ZHIYU BIOTECHNOLOGY CO LTD
摘要:The present invention belongs to the technical field of pharmaceutical synthesis, and specially relates to a preparation method for sapropterin hydrochloride. The method comprises glycosylation of L-arabinose, iodination of 5-hydroxy, reduction and deiodination, hydrolyzation of glycosidic bond and removal of alkyl to obtain 5-deoxy-L-ribose, further reaction to obtain L-erythrobiopterin, and reduction of L-erythrobiopterin to obtain sapropterin hydrochloride. The reaction condition in each step of the preparation method is mild, and the operation is simple and easy. The material is cheap and easily available, so the cost is reduced.
专利号:CN-110872293-A
优先权日:2018-09-04
标题:A kind of chemical synthesis and purification method of biopterin
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
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主要参考文献
1: Doyle S, O'Regan M, Stenson C, Bracken J, Hendroff U, Agasarova A, Deverell D, Treacy EP. Extended Experience of Lower Dose Sapropterin in Irish Adults with Mild Phenylketonuria. JIMD Rep. 2017 Oct 14. doi: 10.1007/8904_2017_63. [Epub ahead of print] doi: 10.1515/jpem-2016-0461. doi: 10.1186/s13023-017-0600-x.
4: Hawks Z, Shimony J, Rutlin J, Grange DK, Christ SE, White DA. Pretreatment cognitive and neural differences between sapropterin dihydrochloride responders and non-responders with phenylketonuria. Mol Genet Metab Rep. 2017 Feb 23;12:8-13. doi: 10.1016/j.ymgmr.2017.01.013. eCollection 2017 Sep.
5: Feldmann R, Wolfgart E, Weglage J, Rutsch F. Sapropterin treatment does not enhance the health-related quality of life of patients with phenylketonuria and their parents. Acta Paediatr. 2017 Jun;106(6):953-959. doi: 10.1111/apa.13799. Epub 2017 Mar 19. doi: 10.1080/09513590.2016.1247796. Epub 2016 Nov 29. doi: 10.1038/tp.2016.24.
合成参考文献
摘要:Yakkyoku. Pharmacy., 43(1191), 1992
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2022)
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