CAS: 135270-13-2; 1-(((2R,3R)-2-(2,4-Difluorophenyl)-3-Methyloxiran-2-yl)Methyl)-1H-1,2,4-Triazole
该化合物是一种具有二氟苯基组和1,27997-三氮基混合物的手性乙氧衍生物,其结构为1,24,4-三氮基混合物,其立体特性(2R,3R)使其在非对称合成中成为有价值的中间体,特别是用于研制生物活性化合物;氟原子的存在可增强代谢稳定性和结合性,而三硝酸化合物组则有助于其在医药化学应用中的用途;由于其结构僵化性和功能组的兼容性,这种复合物很适合用于合成抗排剂和药剂;高纯度和定义的立体化学确保研究和工业过程中的再生性.
- 英文名称1-(((2R,3R)-2-(2,4-Difluorophenyl)-3-Methyloxiran-2-yl)Methyl)-1H-1,2,4-Triazole
- 中文名称1-[[(2R,3R)-2-(2,4-二氟苯基)-3-甲基-2-环氧乙烷基]甲基]-1H-1,2,4-三唑
- IUPAC名称1-(((2R,3R)-2-(2,4-difluorophenyl)-3-methyloxiran-2-yl)methyl)-1H-1,2,4-triazole
- 其它别名1-(((2R,3R)-2-(2,4-Difluorophenyl)-3-Methyloxiran-2-yl)Methyl)-1H-1,2,4-Triazole; Efinaconazole Related Impurity 6; 1-[[(2R,3R)-2-(2,4-Difluorophenyl)-3-Methyl-2-Oxiranyl]Methyl]-1H-1,2,4-Triazole; Efinaconazole Epoxy Impurity; Efinaconazole Impurity 2; Efinaconazole Related Impurity; 1H-1,2,4-Triazole, 1-[[(2R,3R)-2-(2,4-Difluorophenyl)-3-Methyl-2-Oxiranyl]Methyl]-; 1-(((2R,3R)-2-(2,4-Difluorophenyl)-3-Methyloxiran-2-yl)Methyl)-1H-1,2,4-Triazole (Efinaconazole Impurity)
- CAS编号135270-13-2
- MFCD编号:MFCD30343831
- FDA UNII编号:X7MPV5WL2Y
- 分子式:C12H11F2N3O分子量:251.24
- 产品CID: 540652
- 产品分类分析化学 → 标准品 → 药典标准品和杂质标准品
MSDS等安全信息
上下游产品
CAS号86404-63-9 2,4-二氟-α-(1H-1,... | CAS号170863-34-0 (2R,3R)-3-(2,4-... | CAS号170862-36-9 (αS,βR)-β-(2,4-...合成工艺路线路线简述
📜艾氟康唑中间体置于bis(Acetylacetonate)Oxovanadium 叔丁基过氧化氢,Sodium Hydride,三乙胺体系中,用 二氯甲烷,苯 用作溶剂,化学反应 3.17H,反应生成1-[[(2R,3R)-2-(2,4-二氟苯基)-3-甲基-2-环氧乙烷基]甲基]-1H-1,2,4-三唑
参考文献:Triazole Antifungals. Iii. Stereocontrolled Synthesis Of An Optically Active Triazolylmethyloxirane Precursor To Antifungal Oxazolidine Derivatives.
标题:Triazole Antifungals. Iii. Stereocontrolled Synthesis Of An Optically Active Triazolylmethyloxirane Precursor To Antifungal Oxazolidine Derivatives.
摘要:以l-乳酸为起始原料,通过两种方法实现了光学活性三唑甲基环氧乙烷2的立体控制合成,三唑甲基环氧乙烷2是制备真菌恶唑烷化合物1的重要中间体.该过程中使用的关键中间体酮 6 也用于合成 2 的对映体和相应的非对映体环氧化物.
Doi:10.1248/cpb.39.2241
海关参考信息
- 2902600000-乙苯
2902700000-异丙基苯
2905122000-异丙醇
2906210000-苄醇 - 💡 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-10487070-B2
优先权日:2016-04-13
标 题:Process for preparing intermediates useful in the synthesis of antifungal drugs
发明人：BERTOLINI GIORGIO; COLLI CORRADO; SADA MARA; COLOMBO FEDERICA
权利人:OLON SPA; OLSON S P A
摘要:Subject-matter of the invention is a process for preparing intermediates useful in the synthesis of drugs, for example antifungal drugs, such as efinaconazole. Subject-matter of the invention are also such novel synthesis intermediates and the use thereof.
专利号:US-2019119244-A1
优先权日:2016-04-13
标 题 :Process for preparing intermediates useful in the synthesis of antifungal drugs
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主要参考文献
参考标题:An Enantioselective Synthesis Of The Key Intermediate For Triazole Antifungal Agents; Application To The Catalytic Asymmetric Synthesis Of Efinaconazole (Jublia)作者:Keiji Tamura,Naoya Kumagai,Masakatsu Shibasaki |发布日期:2014.4.4
摘要:A New Synthetic Route, The Shortest Reported To Date, To Access A Key Intermediate For The Synthesis Of Various Triazole Antifungal Agents Was Developed. The Elusive Tetrasubstituted Stereogenic Center That Is Essential In Advanced Triazole Antifungal Agents Was Constructed Via The Catalytic Asymmetric Cyanosilylation Of A Ketone. The Subsequent Transformations Were Performed In Two One-Pot Operations
合成参考文献
参考DOI号:10.1021/acs.orglett.1c02588
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