CAS: 127000-90-2; 1-{[(2R,3S)-2-(2,4-Difluorophenyl)-3-Methyloxiran-2-Yl]Methyl}-1H-1,2,4-Triazole

相似化合物

86386-77-8 135270-07-4 135270-13-2

上下游产品

(2R,3R)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)丁烷-2,3-二醇 (2R,3R)-2-(2,4-Difluorophenyl)-1-(1H-1,2,4-Triazol-1-yl)Butane-2,3-Diol 133775-25-4
(2R,3S)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)-2,3-丁二醇 (2R,3S)-2-(2,4-Difluorophenyl)-1-(1H-1,2,4-Triazol-1-yl)-2,3-Butanediol 135270-11-0
(2R,3R)-3-(2,4-二氟苯基)-3-羟基-4-(1H-1,2,4-三唑-1-基)丁烷-2-基甲磺酸酯 (2R,3R)-2-(2,4-Difluorophenyl)-3-Methanesulfonyloxy-1-(1H-1,2,4-Triazol-1-yl)-2-Butanol 133775-26-5
(R)-2-(2,4-二氟苯基)-3-[1H-1,2,4]三唑-1-基丙烷-1,2-二醇 (R)-2-(2,4-Difluorophenyl)-3-(1H-1,2,4-Triazol-1-yl)Propane-1,2-Diol 141113-41-9
(3R)-2-(2,4-Difluorophenyl)-3-(3,4,5,6-Tetrahydro-2H-Pyran-2-Yloxy)-1-(1H-1,2,4-Triazol-1-yl)2-Butanol 844879-56-7
(2R,3R)-2-(2,4-二氟苯基)-3-((四氢-2H-吡喃-2-基)氧基)-1-(1H-1,2,4-三唑-1-基)丁烷-2-醇 (3R)-2-(2,4-Difluorophenyl)-3-(Tetrahydropyran-2-Yloxy)-1-[1,2,4]Triazol-1-Yl-Butan-2-Ol 135133-23-2
(R)-2-(2,4-Difluorophenyl)-2-Hydroxy-3-(1H-1,2,4-Triazol-1-yl)Propanal
[(2R,3S)-2-(2,4-二氟苯基)-3-甲基-2-环氧乙烷基]甲醇 (2R,3S)-2-(2,4-Difluorophenyl)-2,3-Epoxy-1-Butanol 126918-27-2 (1R)-1-<(2R)-2-(2,4-Difluorophenyl)-2-Oxiranyl>Ethanol 126918-35-2 (1S)-1-<(2R)-2-(2,4-Difluorophenyl)-2-Oxiranyl>Ethanol 126918-33-0

(2R,3R)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)丁烷-2,3-二醇置于sodium Methylate,三乙胺体系中,用 甲醇,二氯甲烷,乙酸乙酯 用作溶剂,化学反应 1.0H,反应生成1-(((2R,3S),2-(2,4-二氟苯基)-3-甲基环氧乙烷-2-基)甲基)-1H-1,2,4-三唑
参考文献:光学活性抗真菌唑类.I.(2R,3R)-2-(2,4-二氟苯基)-3-巯基-1-(1H-1,2,4-三唑-1-基)-2-丁二醇的合成及抗真菌活性它的立体异构体.
标题:光学活性抗真菌唑类.I.(2R,3R)-2-(2,4-二氟苯基)-3-巯基-1-(1H-1,2,4-三唑-1-基)-2-丁二醇的合成及抗真菌活性它的立体异构体.
摘要:(2R,3R)-2-(2,4-二氟苯基)-3-巯基-1-(1H-1,2,4-三唑-1-基)-2-丁醇[(2R,3R)-7 ]和其立体异构体[(2S,3R)-,(2S,3S)-和(2R,3S)-7]是通过新开发的开环反应由旋光环氧乙烷6制备的,并评价其抗真菌活性.硫醇(2R,3R)-7在体外和体内均显示出极强的抗真菌活性.旋光性环氧乙烷(2R,3S)-6,一种用于合成含硫抗真菌唑5的有用中间体,是通过(R)-乳酸甲酯[(R)-8]经八步立体控制合成的.合成的关键步骤是(R)-乳酸的酰胺衍生物[(R)-12A]与2,4-二氟苯基-溴化镁(13)的grignard反应.
Doi:10.1248/cpb.41.1035

专利信息

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:EP-3397628-A1
优先权日:2015-12-30
标题 :Process for the synthesis of efinaconazol

专利号:EP-3397628-B1
优先权日:2015-12-30
标题:Process for the synthesis of efinaconazol

专利号:IT-UB20159795-A1
优先权日:2015-12-30
标题 :PROCESS FOR THE SYNTHESIS OF EFINACONAZOLE

专利号:WO-2017114743-A1
优先权日:2015-12-30
标题:Process for the synthesis of efinaconazol