Background: Halofuginone hydrobromide (1) is recognized as an effective drug against several species of Eimeria (E.) in poultry. In this paper, we describe a convenient and low cost preparation method for the compound, as well as primary validation of its activity. Methods: First, 7-bromo-6-chloroquinazolin-4(3H)-one (2) was prepared from m-chlorotoluene by a conventional process, and then chloroacetone was creatively introduced in two steps. Finally, halofuginone hydrobromide (1) was obtained from 7-bromo-6-chloro-3-(3-cholroacetonyl) quinazolin-4(3H)-one (4) by a four-step reaction sequence including condensation, cyclization, deprotection and isomerization. The structures of the relative intermediates and target compound were characterized by melting point, IR, MS and 1H-NMR. Besides, the protective effect of compound 1-supplemented chicken diet at doses of 6, 3 and 1.5 mg per 1 kg were evaluated on chickens infected with E. tenella, by reduction in mortality, weight loss, fecal oocyst excretion and gut pathology, respectively. Results: Halofuginone hydrobromide (1) was prepared successfully by and improved and innovative method based on traditional research. Moreover, the synthesized halofuginone hydrobromide significantly exhibited an anti-coccidial property. Conclusions: The fruitful work described in this Communication has resulted in halofuginone hydrobromide, which has a good pharmaceutical development prospects, becoming more available for large-scale production.

中文翻译：

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高效抗球虫药物卤夫酮氢溴酸盐的新合成

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，采用改进创新的方法成功制备卤夫酮氢溴酸盐(1)。此外，合成的卤夫酮氢溴酸盐具有显着的抗球虫特性。结论：本通讯所描述的卓有成效的工作使得具有良好药物开发前景的卤夫酮氢溴酸盐更易于规模化生产。粪便卵囊排泄和肠道病理学，分别。结果：在传统研究的基础上，采用改进创新的方法成功制备卤夫酮氢溴酸盐(1)。此外，合成的卤夫酮氢溴酸盐具有显着的抗球虫特性。结论：本通讯所描述的卓有成效的工作使得具有良好药物开发前景的卤夫酮氢溴酸盐更易于规模化生产。粪便卵囊排泄和肠道病理学，分别。结果：在传统研究的基础上，采用改进创新的方法成功制备卤夫酮氢溴酸盐(1)。此外，合成的卤夫酮氢溴酸盐具有显着的抗球虫特性。结论：本通讯所描述的卓有成效的工作使得具有良好药物开发前景的卤夫酮氢溴酸盐更易于规模化生产。