CAS: 182230-43-9; 2-(2,4-Difluorophenyl)-3-(5-Fluoropyrimidin-4-yl)-1-(1H-1,2,4-Triazol-1-yl)Butan-2-Ol

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CAS号188416-35-5 外消旋-6-氯 伏立康唑 | CAS号86404-63-9 2,4-二氟-α-(1H-1,... | CAS号1289559-65-4 1-(2,6-dichloro... | CAS号51336-94-8 2-氯-2,4-二氟苯乙酮 | CAS号137234-87-8 6-乙基-5-氟嘧啶-4(3H)-酮 | CAS号1237496-99-9 6-ethyl-5-fluor... | CAS号137234-62-9 伏立康唑

3-(6-氯-5-氟嘧啶-4-基)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇盐酸盐置于palladium 10% On Activated Carbon,氢气,Sodium Carbonate体系中,用 乙醇 用作溶剂,20.0~25.0 °C,101.33 Kpa 条件下,以82%的收率获得(2R,3S/2S,3R)-2-(2,4-二氟苯基)-3-(5-氟嘧啶-4-基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇
参考文献:一种制备伏立康唑关键中间体的新方法
标题:一种制备伏立康唑关键中间体的新方法
摘要:本发明公开一种制备伏立康唑关键中间体的新方法.本发明采用高立体选择性的手性氨基醇催化剂和锌铜偶联合催化1‑(4‑氯‑5‑氟嘧啶‑6基)卤代乙烷与1‑(2,4‑二氟苯基)‑2‑(1H‑1,2,4‑三唑‑1‑基)乙酮进行不对称加成反应,得到(2R,3S/2S,3R)‑2‑(2,4‑二氟苯基)‑3‑(4‑氯‑5‑氟嘧啶‑4‑基)‑1‑(1H‑1,2,4‑三唑‑1‑基)‑2‑丁醇,经过氢化脱卤制得伏立康唑关键中间体(2R,3S/2S,3R)‑2‑(2,4‑二氟苯基)‑3‑(5‑氟嘧啶‑4‑基)‑1‑(1H‑1,2,4‑三唑‑1‑基)‑2‑丁醇,拆分得到伏立康唑.本发明使用了更经济和环境友好的天然手性氨基醇催化剂;采用卤代烃与酮进行高立体选择性不对称加成反应,省掉将卤代烃和活性锌制备成有机锌金属化合物后再与酮进行不对称加成反应,简化操作,降低生产成本,利于产业化.

专利信息

专利号:US-10633368-B2
优先权日:2015-12-23
标 题 :Voriconazole intermediate and voriconazole synthesis method
发明人：HUANG HU; HUANG WENFENG; TU GUOLIANG; LIU JIEGEN; XU ZHONGMING; WU QIANGHUI; MENG ZHAOYANG; FANG YULING
权利人:ZHEJIANG HUAHAI PHARM CO LTD
摘要:Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula 1, the product is prepared via compounds III and IV. The synthesis method adjusts the feeding means, and the reaction conditions are mild and controllable, thereby reducing the production of impurity A, avoiding the use of highly toxic metal lead, and eliminating the risk of highly toxic metal remaining in a drug. The product has a higher purity and significant industrial application value.

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-118164968-A
优先权日:2024-01-26
标 题:Synthesis method of triazole antifungal drug voriconazole

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