CAS: 137234-74-3; 4-Chloro-6-Ethyl-5-Fluoropyrimidine

上下游产品

CAS号137234-87-8 6-乙基-5-氟嘧啶-4(3H)-酮 | CAS号137234-85-6 2,4-二氯-6-乙基-5-氟嘧啶 | CAS号759-67-1 氟代丙酰基乙酸乙酯 | CAS号1112937-23-1 4-(4-chlorophen... | CAS号188416-28-6 4-(1-溴代乙基)-5-氟-6-氯嘧啶 | CAS号188416-35-5 外消旋-6-氯 伏立康唑 | CAS号137234-62-9 伏立康唑

2-Chloro-6-Ethyl-5-Fluoro-4-Hydroxypyrimidine Ammonium Salt置于5%-Palladium/activated Carbon,氢气,三乙胺,三氯氧磷体系中,用 乙醇,二氯甲烷 用作溶剂,40.0~50.0 °C,344.75 Kpa 条件下,反应 8.0H,反应生成4-氯-6-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 The Initial Six-Step Development Route From 5-Fluorouracil Has Been Superseded By A Four-Step Synthesis Involving Fluorination Of Methyl 3-Oxopentanoate And Cyclisation With Formamidine Acetate.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-108059617-B
优先权日:2018-02-06
标 题:Impurity of voriconazole starting material 4-chloro-6-ethyl-5-fluoropyrimidine and synthesis method thereof

专利号:CN-118767991-A
优先权日:2023-03-30
标题:Catalyst, preparation method thereof and application of catalyst in cyclododecanone synthesis

专利号:CN-116751188-A
优先权日:2023-06-26
标 题:A synthesis method of process impurities produced by key intermediates of voriconazole

专利号:CN-1919846-A
优先权日:2006-09-14
标 题 :Novel oriented synthesis method of voriconazole, medicinal salt and intermediate thereof