CAS: 75907-82-3; 2-Fluorobenzothioamide

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CAS号394-47-8 2-氟苯甲腈 | CAS号445-28-3 2-氟苯甲酰胺 | CAS号75907-83-4 2-FLUORO-N-HYDR...

📜2-氟苯腈置于magnesium(II) Chloride Hexahydrate,Sodium Hydrogen Sulfide Monohydrate体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 2-氟苯甲酰硫胺
参考文献:一些含有酰腙部分的新型苯基噻唑衍生物的设计,合成和抗真菌活性
标题:一些含有酰腙部分的新型苯基噻唑衍生物的设计,合成和抗真菌活性
摘要:农作物真菌病害对全球农作物生产和质量构成严重威胁.开发新型高效杀菌剂是防治作物病害的重要措施.我们前期对天然产物噻孢菌素a的结构优化和生物活性研究发现,苯基噻唑是一种优异的抗真菌骨架.为了寻找新的杀菌剂,利用活性子结构原理设计合成了45种含有酰腙结构的苯基噻唑衍生物.拼接.除了化合物 E1,E14 和 E33 之外,45 种化合物中有 42 种是新化合物.它们的结构通过 1H NMR,13C NMR 和 Hrms 进行了结构表征.目标化合物在 25 μg/ml 浓度下对稻瘟病菌,山茶炭疽菌,玉米双极菌和核盘菌的抗真菌活性进行了评估.生物测定结果表明,大多数化合物在 25 μg/ml 浓度下对米霉和茶霉表现出优异的抗真菌活性.其中,化合物e4,E10,E14,E17,E23,E26和e27对米霉的抑制率超过80%,Ec50值为1.66,2.01,2.26,1.45,1.50,1.29和2.65.
DOI:10.3390/molecules28207084

专利信息

专利号:US-8552175-B2
优先权日:2009-04-23
标题:Sulfur transfer reagents for oligonucleotide synthesis
发明人：GUZAEV ANDREI P
权利人:GUZAEV ANDREI P; A M CHEMICALS INC
摘要:The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones, 5-phenyl-3H-1,2,4-dithiazole-3-thiones, and derivatives thereof as novel, efficient sulfur-transfer reagents is disclosed. Sulfur transfer from these reagents to compounds containing a P(III) atom (e.g., triphenylphosphine, 5′-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5′-O-DMT-3′-O-levulinyl dithymidilyl 2-cyanoethyl phosphite), was studied in solution by 31 P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2′-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods. As opposed to many sulfur transfer reagents known in the prior art such as 1,2-benzodithiol-3-one-1,1-dioxide (Beaucage reagent) and 5-ethoxy-3H-1,2,4-dithiazole-2-one (EDIT), the sulfurizing agents disclosed herein are highly stable in solution, which increases their practical and commercial value.