CAS: 188416-47-9; 4-(1-Bromoethyl)-5-Fluoropyrimidine

上下游产品

4-乙基-5-氟嘧啶 4-Ethyl-5-Fluoropyrimidine 137234-88-9

📜2,4-二氯-6-乙基-5-氟嘧啶置于n-溴代丁二酰亚胺(Nbs),偶氮二异丁腈,5%-Palladium/activated Carbon,氢气,Sodium Acetate体系中,用 甲醇,二氯甲烷 用作溶剂,50.0 °C,344.75 Kpa 条件下,反应 11.0H,反应生成4-(1-溴乙基)-5-氟嘧啶
参考文献:Process Development Of Voriconazole: A Novel Broad-Spectrum Triazole Antifungal Agent
标题:Process Development Of Voriconazole: A Novel Broad-Spectrum Triazole Antifungal Agent
摘要:In The Synthesis Of (2R,3S)-2-(2,4-Difluorophenyl)-3-(5-Fluoro-4-Pyrimidinyl)-1-(1H-1,2,4-Triazol-1-yl)-2-Butanol (Voriconazole),The Relative Stereochemistry Is Set In The Addition Of A 4-(1-Metalloethyl)-5-Fluoropyrimidine Derivative To 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-Triazol-1-yl)-1-Ethanone,The Diastereo-Control Of This Reaction Has Been Examined By Variation Of Pyrimidine Substitution Pattern And By Changes In The Metalation And Reaction Conditions. Excellent Diastereoselection (12: Ii Is Obtained Using An Organozinc Derivative Of 6-(1-Bromoethyl)-4-Chloro-5-Fluoropyriminidine. Lifter Removal Cf The Chlorine From The Pyrimidine Ring The Absolute Stereochemistry Of Voriconazole Is Established Via A Diastereomeric Salt Resolution Process Using (1R)-10 Camphorsulfonic Acid. Synthetic Routes To The Pyrimidine Partner Have Also Been Evaluated. The Initial Six-Step Development Route From 5-Fluorouracil Has Been Superseded By A Four-Step Synthesis Involving Fluorination Of Methyl 3-Oxopentanoate And Cyclisation With Formamidine Acetate.
Doi:10.1021/op0000879

专利信息

专利号:RU-2156760-C2
优先权日:1995-08-05
标 题 :Method of synthesis of triazoles, ultimate and intermediate compounds of method

专利号:CN-1076019-C
优先权日:1995-08-05
标 题:Synthesis of triazoles via addition of organometallic compounds to ketones and their intermediates

专利号:CN-113354625-B
优先权日:2021-06-16
标 题:Synthesis process of voriconazole

专利号:CN-113354625-A
优先权日:2021-06-16
标题:The synthesis process of voriconazole