CAS: 17518-98-8; 7-Bromo-6-Chloroquinazolin-4(3H)-One

3-氯甲苯置于吡啶,Copper(I) Oxide,Iron(III) Chloride,Potassium Permanganate,氨,溴,Potassium Hydroxide,Sodium Hydroxide体系中,用 二氯甲烷,水 用作溶剂,化学反应 6.5H,反应生成7-溴-6-氯-4(3H)-喹唑啉酮
参考文献:高效抗球虫药物卤夫酮氢溴酸盐的新合成
标题:高效抗球虫药物卤夫酮氢溴酸盐的新合成
摘要:背景:Halofuginone Hydrobromide (1) 被认为是一种有效的药物,可以对抗家禽中的几种艾美球虫 (E.).在本文中,我们描述了一种方便且低成本的化合物制备方法,以及对其活性的初步验证.方法:首先以间氯甲苯为原料,采用常规工艺制备7-溴-6-氯喹唑啉-4(3H)-一(2),然后创造性地分两步引入氯丙酮.最后,由7-Bromo-6-Chloro-3-(3-Cholroacetonyl) Quinazolin-4(3H)-One(4)通过缩合,环化,脱保护和脱保护等四步反应得到卤夫酮氢溴酸盐(1).异构化.相关中间体和目标化合物的结构经熔点,红外,质谱和1H-NMR表征.除了,分别通过降低死亡率,体重减轻,粪便卵囊排泄和肠道病理,评估了添加化合物 1 的鸡日粮以 6,3 和 1.5 Mg/1 Kg 的剂量对感染 E.Tenella 的鸡的保护作用.结果:在传统研究的基础上
Doi:10.3390/molecules22071086

专利信息

专利号:US-12410131-B2
优先权日:2021-10-21
标题:Method for preparation of trans-n-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as intermediate of halofuginone
发明人：FENG YU; XU HONG; WU JIAXUAN; SONG DANHUI; ZHONG WEIHUI; LING FEI; XU CHAO
权利人:CHENGDA PHARMACEUTICALS CO LTD
摘要:The present disclosure relates to the field of drug synthesis, and discloses a method for the preparation of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as an intermediate of halofuginone. In the preparation method according to the present disclosure, for the first time, trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as shown in Formula I is obtained from amino-substituted pentanal and a thiazolyl sulfoxide compound as raw materials by Mislow-Evans rearrangement reaction and subsequent Lewis acid catalysis. The method for the preparation of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as an intermediate of halofuginone according to the present disclosure has high yields and stable qualities, provides a new reference route for the synthesis of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone, avoids the reduction of pyridine, and overcomes the disadvantage of requiring the use of an expensive metal catalyst Rh/Al2O3.

专利号:CN-119409646-A
优先权日:2024-11-01
标题 :New compound, synthesis method thereof and application of new compound in preparation of anticoccidial drugs