CAS: 164650-44-6; (2R,3R)-2-(2,4-Difluorophenyl)-3-(4-Methylenepiperidin-1-yl)-1-(1H-1,2,4-Triazol-1-yl)Butan-2-Ol

上下游产品

4-methylene piperidine oxirane(2S,3R)-2-(2,4-difluorophenyl)-3-methyl-2-(1H-1,2,4-triazol-1-yl)methyloxirane (4-(chloromethyl)piperidin-1-yl)(phenyl)methanone N-benzoyl-4-methylenepiperidine

3-Chloro-2-(2,4-Difluorophenyl)-2-(Trimethylsilanyloxy)Propionaldehyde置于四丁基氟化铵,甲基磺酰氯,三乙胺体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应 35.0H,反应生成艾氟康唑
参考文献:三唑类抗真菌剂关键中间体的对映选择性合成;Efinaconazole(jublia)在催化不对称合成中的应用
标题:三唑类抗真菌剂关键中间体的对映选择性合成;Efinaconazole(jublia)在催化不对称合成中的应用
摘要:开发了一种新的合成路线,该路线是迄今为止报道的最短路线,可通往合成各种三唑抗真菌剂的关键中间体.通过高级酮的催化不对称氰基硅烷化反应构建了在高级三唑抗真菌剂中必不可少的难以捉摸的四取代立体异构中心.随后的转化以两个一锅操作进行,从而提高了中间体的整体合成效率.这种简化的合成方法已成功地应用于依非那康唑(jublia)和拉伏康唑的有效对映选择性合成.
Doi:10.1021/jo500369Y

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-10626102-B2
优先权日:2015-12-30
标题 :Process for the synthesis of efinaconazol
发明人：VERONESE MARTINO; BETTONI PIERGIORGIO; ROLETTO JACOPO; PAISSONI PAOLO
权利人:PROCOS SPA
摘要:Disclosed is a process for the synthesis of efinaconazole (I), starting from 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole and 4-methylenepiperidine, as free base or hydrochloride, in an organic solvent, under anhydrous conditions and in the presence of neutralising agents and reaction-promoting metal species. (1) The process is particularly advantageous because it gives rise to efinaconazole in high yields and purity, and uses little more than the stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.

专利号:EP-3091007-A1
优先权日:2015-05-08
标 题 :Process for the preparation of piperidine compounds
发明人：ATTOLINO EMANUELE; RIZZO ELISABETH; ROSSI DAVIDE
权利人:DIPHARMA FRANCIS SRL
摘要:The present invention relates to a process for the preparation of intermediates useful in the synthesis of efinaconazole and their use in the synthesis of efinaconazole.

专利号:US-2023364251-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

专利号:ES-2785157-T3
优先权日:2016-04-13
标 题 :Procedure for the preparation of useful intermediates in the synthesis of antifungal drugs

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