53017-34-8Relevant academic research and scientific papers
Novel method for preparing drotaverine hydrochloride intermediate
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Paragraph 0052-0058, (2020/06/16)
The invention discloses a novel method for preparing a drotaverine hydrochloride intermediate, belonging to the technical field of medicine synthesis. The preparation method comprises the following steps: preparing an intermediate 3,4-diethoxyphenylacetic acid with 1,2-diethoxybenzene as a raw material, and preparing the intermediate 3,4-diethoxyphenylacetamide with 3,4-diethoxyphenylacetic acid as a raw material. According to the novel process for preparing the drotaverine hydrochloride intermediate, a method for directly preparing 3,4-diethoxyphenylacetic acid and 3,4-diethoxyphenylethylamine is adopted, and a process for preparing 3,4-diethoxyphenylacetonitrile is avoided, so a reaction step of using sodium cyanide is avoided.
Design, synthesis and acaricidal/insecticidal activities of etoxazole analogues
Liu, Yu-Xiu,Wei, Xing-Cun,Li, Yong-Qiang,Yang, Na,Wang, Qing-Min
, p. 1803 - 1810 (2013/06/27)
Based on the structure-activity relationship of etoxazole analogues and benzoylphenylureas, a series of 2-(2,6-difluorophenyl)-4-(4-substitutedphenyl)- 1,3-oxazolines 4a-y were designed and synthesized. It was found that most of these compounds showed excellent acaricidal activities. They gave above 85% mortality at a concentration of 2.5 mg L-1, both for the eggs and larvae of spider mites. Some compounds also showed excellent insecticidal activities. The position and type of the substituents on the 4-phenyl of 2,4-diphenyl-1,3-oxazoline have a great influence on the activities. 2-(2,6-Difluorophenyl)-4-(2-Cl-4-(4-Cl-phenoxy)phenyl)-1,3-oxazoline (4r) exhibited 100% acaricidal mortality at 2.5 mg L-1, with 65% and 93% mortality against beet armyworm and diamondback moth, respectively, at 12.5 mg L-1, which is almost the same level as etoxazole. The newly found structure-activity relationship may also benefit further acaricide/insecticide development.
