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新型IDO1抑制剂HS-10319的合成工艺研究
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作者 孙平 游军辉 +2 位作者 韦唯 吴成军 孙铁民 《中国药物化学杂志》 CAS 2024年第1期67-74,共8页
目的优化新型IDO1抑制剂HS-10319的合成工艺。方法以丙二腈为起始原料,经硝化、重排、肟化、脱水缩合、重氮化反应得到4-氨基-N′-羟基-1,2,5-噁二唑-3-亚甲酰氯(4);另以二甲基二硫醚为起始原料,经氧化反应后与二丙酮-D-葡萄糖在碱性条... 目的优化新型IDO1抑制剂HS-10319的合成工艺。方法以丙二腈为起始原料,经硝化、重排、肟化、脱水缩合、重氮化反应得到4-氨基-N′-羟基-1,2,5-噁二唑-3-亚甲酰氯(4);另以二甲基二硫醚为起始原料,经氧化反应后与二丙酮-D-葡萄糖在碱性条件下反应得到高立体选择性的S构型甲基亚砜化合物(7),7经取代、胺化反应后与中间体4发生取代反应,然后经重排、重氮化、取代、环合、缩合和水解反应得到目标化合物HS-10319。结果与结论目标化合物及其关键中间体的结构经1H-NMR、13C-NMR和MS谱确证,总收率为8.06%(以丙二腈计),纯度为98.9%(HPLC法)。优化后的工艺参数设置合理、工艺稳定性好、产品质量稳定且易于控制,适合工业化生产。 展开更多
关键词 IDO1抑制剂 合成工艺 创新药 硫亚胺化 不对称合成
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Grafting polysulfides into a functional N-halo compound for high-performance lithium—sulfur battery 被引量:1
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作者 Junfeng Wu Bohai Zhang +4 位作者 Sheng Liu Yihua Song Shihai Ye Tianying Yan Xueping Gao 《Science China Materials》 SCIE EI CSCD 2020年第10期2002-2012,共11页
Due to its high energy density,lithium-sulfur(Li-S)battery is considered as the most promising candidate for the energy storage systems,but its practical application is hindered by the dissolution of lithium polysulfi... Due to its high energy density,lithium-sulfur(Li-S)battery is considered as the most promising candidate for the energy storage systems,but its practical application is hindered by the dissolution of lithium polysulfides in the electrolyte.In this work,N-bromophthalimide(C8H4NO2Br,NBP),an aromatic molecule with carbophilic,sulfiphilic,lithiophilic,and solvophilic nature,is introduced into active graphene(AG)to fabricate the sulfur composite cathode.The carbophilic NBP is anchored readily on the AG surface viaπ−πstacking interaction.During discharging,the dissolved lithium polysulfide anion(LiS−n)is grafted into the sulfiphilic NBP spontaneously via SN2 substitution reaction to form C8H4NO2SnLi,which brings the dissolved LiS−n back to the AG surface in the composite cathode.Moreover,the lithiophilic and solvophilic nature of NBP improve the wettability of the porous composite cathode,and the electrolyte molecule is easily penetrated into the micro-mesopores of AG to facilitate the diffusion of the electrolyte.Thus,NBP,as a multi-functional compound in Li-S battery,can immobilize LiS−n and enhance the diffusion of the electrolyte.The above features of NBP endow the sulfur composite cathode with improved electrochemical performance in the cycling stability. 展开更多
关键词 Li-S battery sulfur cathode multi-functional materials N-bromophthalimide POLYSULFIDES ab initio calculation
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