CAS: 22432-95-7; 4-Amino-1-((2S,4S,5R)-4-Hydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-1,3,5-Triazin-2(1H)-One
该化合物是作为低甲基代谢剂的一种核素类比,主要用于治疗宫颈塑料综合症(MDS)和急性髓白血病(AML),通过将DNA纳入DNA并抑制DNA甲基转移酶,导致低甲基化并重新启动静默肿瘤抑制基因;这一机制恢复了恶性细胞的正常细胞分化和吸附;a-Decitabine因其纯度和稳定性很高而得到注意,确保了研究和临床应用的可靠性能;其精明的药用动力学特征和血解恶性疗法的既定功效使其成为了进行遗传学研究和治疗发展的宝贵工具;需要妥善处理和储存以保持其完整性.
- 英文名称4-Amino-1-((2S,4S,5R)-4-Hydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-1,3,5-Triazin-2(1H)-One
- 中文名称α-地西他滨
- IUPAC名称4-amino-1-((2S,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one
- 其它别名Decitabine Alpha-Isomer; Decitabine Impurity 4(Alpha-Isomer); Decitabine Alpha Isomer Impurity; 4-Amino-1-[4-Hydroxy-5-(Hydroxymethyl)Oxolan-2-Yl]-1,3,5-Triazin-2-One; Alpha-Decitabine; Decitabine Impurity 38; 1,3,5-Triazin-2(1H)-One, 4-Amino-1-(2-Deoxy-α-D-Erythro-Pentofuranosyl)-; 1-(2-Deoxy-A-D-Ribofuranosyl)-5-Azacytosine
- CAS编号22432-95-7
- MFCD编号:MFCD30738080
- EINECS号:815-973-4
- FDA UNII编号:Z8RX6X3ET8
- 分子式:C8H12N4O4分子量:228.21
- 产品CID: 1160408
- 产品分类分析化学 → 标准品 → 药典标准品和杂质标准品
物理性质
MSDS等安全信息
欧盟法规
C&L通报上下游产品
N-(formylamidino)-N'-β-D-2-deoxyribofuranosylurea decitabine monohydrate 5-azacytosine 3,5-O-bis(4-chlorobenzoyl)-2-deoxy-α-D-ribofuranosyl chloride2'-deoxy-3',5'-di-O-p-toluoyl-5-azacytidine 2'-deoxy-5'-O-p-toluoyl-5-azacytidine 2'-deoxy-β-D-5-azacytidine 5'-monophosphate Isobutyric acid 3-{(2R,4S,5R)-5-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-hydroxy-tetrahydro-furan-2-yl}-8-isobutyryl-7-isobutyryloxy-2-oxo-2,3,4,6,7,8-hexahydro-imidazo[1,2-a][1,3,5]triazin-6-yl ester合成工艺路线路线简述
📜[5-(4-Amino-2-Oxo-1,3,5-Triazin-1-yl)-2-(9H-Fluoren-9-Ylmethoxycarbonyloxymethyl)Oxolan-3-Yl] 9H-Fluoren-9-Ylmethyl Carbonate 以32的收率获得alpha-地西他滨
参考文献:一种地西他滨的合成与工业化生产方法
标题:一种地西他滨的合成与工业化生产方法
摘要:本发明涉及一种地西他滨的合成与工业化生产方法,即以2-脱氧-D-核糖为原料,与甲醇反应得到甲苷,3,5-二羟基用9-芴甲氧羰基保护,然后与氯化氢反应得到1-氯芴糖,1-氯芴糖再与硅烷化的5-氮杂胞嘧啶反应,然后脱保护基,精制后得到地西他滨.本发明的特点是1-氯芴糖与硅烷化的5-氮杂胞嘧啶缩合反应中不需要四氯化锡,避免原料药中重金属超标的问题;同时控制三氟甲磺酸三甲基硅酯的量和反应条件,使产物中β体含量增加.
海关参考信息
- 2905122000-异丙醇
2905310000-1,2-乙二醇
2905320000-1,2-丙二醇
2905399001-1,3-丙二醇 - 💡 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:US-9266863-B2
优先权日:2010-03-30
标题 :Process for the synthesis of azacitidine and decitabine
发明人：DE FERRA LORENZO; ZENONI MAURIZIO; TURCHETTA STEFANO; ANIBALDI MAURO; AMMIRATI ETTORE; BRANDI PAOLO; BERARDI GIORGIO
权利人:DE FERRA LORENZO; ZENONI MAURIZIO; TURCHETTA STEFANO; ANIBALDI MAURO; AMMIRATI ETTORE; BRANDI PAOLO; BERARDI GIORGIO; CHEMI SPA
摘要:Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.
专利号:WO-2011040984-A1
优先权日:2009-10-02
标 题:Synthesis of decitabine
专利号:US-2011245485-A1
优先权日:2010-03-30
标题 :Process for the synthesis of azacitidine and decitabine
