📜5-甲基-2-(2H-1,2,3-三唑-2-基)苯甲酰氯置于palladium 10% On Activated Carbon,氢气,三乙胺体系中,用 甲醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,20.0 °C,482.64 Kpa 条件下,反应 16.0H,反应生成(7R)-7-甲基-1-[5-甲基-2-(2H-1,2,3-三唑-2-基)苯甲酰基]-1,4-二氮杂环庚烷 参考文献:Process For The Preparation Of Suvorexant And Intermediates Useful In The Synthesis Of Suvorexant 标题:Process For The Preparation Of Suvorexant And Intermediates Useful In The Synthesis Of Suvorexant 摘要:一种用于制备苏维瑞昔安(化学式i),其相关化合物和中间体的新工艺,简单,经济且具有商业可行性. (I)
专利信息
专利号:US-2016168138-A1 优先权日:2013-07-15 标题:Process for the preparation of suvorexant and intermediates useful in the synthesis of suvorexant 发明人:IQBAL JAVED; DAHANUKAR VILAS HARESHWAR; ORUGANTI SRINIVAS; KANDAGATLA BHASKAR 权利人:REDDY S LAB LIMTED DR 摘要:A novel processes for the preparation of suvorexant (formula I), its related compounds and its intermediates that are simple, economical and commercially viable. (I)
专利号:US-10030010-B2 优先权日:2014-08-04 标题:Route of synthesis for the preparation of suvorexant 发明人:BARTH ROLAND; HÖFERL-PRANTZ KATHRIN; RICHTER FRANK; WIDSCHWENTER GERHARD 权利人:SANDOZ AG 摘要:The present invention relates to a process for the preparation of a compound of formula (A), Further, the present invention relates to the respective compound (A) as such and to its use in the preparation of antifungal agent.
专利号:EP-3021851-A2 优先权日:2013-07-15 标 题 :Process for the preparation of suvorexant and intermediates useful in the synthesis of suvorexant
专利号:EP-3177616-A1 优先权日:2014-08-04 标题 :Novel routes of synthesis for the preparation of suvorexant
专利号:US-2017217947-A1 优先权日:2014-08-04 标 题:Novel Route of Synthesis for the Preparation of Suvorexant
专利号:US-10618891-B2 优先权日:2016-02-01 标 题 :Suvorexant intermediate and preparation method thereof 发明人:LIN JIANPING; GUO XIAOWEN; GAO XIAOFEI; HUANG CHAO; GUO YUANBING; TAO ANPING; HUANG LUNING; GU HONG 权利人:ZHEJIANG HUAHAI PHARM CO LTD; SHANGHAI AOBO PHARMTECH INC LTD 摘要:The present invention relates to a synthesis process of suvorexant, novel compounds represented by formulas II, III, IV or V, or salts thereof for preparing suvorexant, and a method for preparing the intermediates. The preparation method uses a chiral starting material to synthesize chiral compounds represented by formulas II, III, IV or V, the compounds obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy to purify, high yield, high ee value for the product, and easy to industrialize. In the reaction route shown, R represents benzyl, allyl or 1-phenethyl, or optionally substituted benzyl at the 2 position to 6 position, such as 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl.