1006376-63-1Relevant articles and documents
Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity
Casandra, Debora R.,Chakrabarti, Debopam,Iyamu, Iredia D.,Kyle, Dennis E.,Manetsch, Roman,Parvatkar, Prakash T.,Roberts, Bracken F.,Wojtas, Lukasz,Zhao, Yingzhao
, (2022/01/28)
Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.
Method for preparing (S)-2-(3,4-difluorophenyl)ethylene oxide
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Paragraph 0019; 0042-0044; 0047-0066, (2019/07/16)
The invention relates to a method for preparing (S)-2-(3,4-difluorophenyl)ethylene oxide. The invention relates to the technical field of pharmaceutical and chemical synthesis, and discloses a methodfor producing the (S)-2-(3,4-difluorophenyl)ethylene oxi
Preparation process for (1R,2S)-1-cyano-2-(3,4-difluoro-phenyl)cyclopropane
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Paragraph 0025-0027; 0028-0030; 0031-0033, (2017/08/29)
The invention discloses a preparation process for (1R,2S)-1-cyano-2-(3,4-difluoro-phenyl)cyclopropane. The preparation process comprises the following steps: 1) in the presence of (S)-(+)-1,1'-binaphthyl-2,2'-diyl hydrogenphosphate, performing a contact reaction on 3,4-difluorostyrene and hydrogen peroxide to obtain (2S)-2-(3,4-diflurophenyl)-ethylene oxide; 2) in the presence of alkali, making the (2S)-2-(3,4-diflurophenyl)-ethylene oxide react with diethyl cyanomethylphosphonate in 1,4-dioxane to obtain a target product. By adopting the preparation process, the use of chiral raw materials is avoided, and the reaction cost is lowered; moreover, the (1R,2S)-1-cyano-2-(3,4-difluoro-phenyl)cyclopropane is synthesized conveniently through the diethyl cyanomethylphosphonate, so that high overall yield and three-dimensional selectivity are achieved; furthermore, the method is easy and convenient to operate, and is suitable for industrial expandable production.