CAS: 1009119-64-5; Methyl ((S)-1-((S)-2-(5-(4'-(2-((S)-1-((Methoxycarbonyl)-L-Valyl)Pyrrolidin-2-yl)-1H-Imidazol-5-yl)-[1,1'-Biphenyl]-4-yl)-1H-Imidazol-2-yl)Pyrrolidin-1-yl)-3-Methyl-1-Oxobutan-2-yl)Carbamate

上下游产品

L-prolineL-proline

达卡他韦中间体置于盐酸,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺体系中,用 水,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 0.88H,反应生成达卡他韦
参考文献:用于偶联反应和抗病毒 Daclatasvir Api 合成的 Elements-Continuous-Flow 平台
标题:用于偶联反应和抗病毒 Daclatasvir Api 合成的 Elements-Continuous-Flow 平台
摘要:一种新型纳米纹理 Ni@cu 材料嵌入式电微流反应器具有最小的电极距离,已被用于通过构建新的 C-C 键来合成联苯.报告的协议不含贵金属,并涉及以快速方式合成取代/未取代联苯系统的无助还原剂/无氧化剂条件.电反应器体积针对克级联苯合成进行了优化,并进一步扩展为集成的总工艺系统,通过选择性去除不需要的化学品/溶剂来减少繁琐的下游工艺.Daclatasvir 的连续微流合成现已以非常好的收率完成.
Doi:10.1055/a-2022-2063

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2023364078-A1
优先权日:2022-05-12
标题:Method of preparing nanoparticles comprising poorly water soluble drugs for treating hepatitis
发明人：KIM HYUN CHUL; MOON BYOUNG YONG
权利人:EVEX TECH INC
摘要:The present invention provides nanoparticles which contain a poorly water-soluble drug for treating hepatitis, and a method of producing the nanoparticles. More particularly, the present invention provides a method of producing nanoparticles for treating hepatitis, which includes: a first step of preparing a precursor mixture solution for synthesis of nanoparticles which include a drug for treating hepatitis; a second step of extracting the compound under supercritical or subcritical conditions; and a third step of dispersing the same, as well as the nanoparticles including a poorly water-soluble drug for treating hepatitis with improved bioavailability and without organic solvent residue.

专利号:US-2022395555-A1
优先权日:2020-06-11
标题:Derivatives of antibiotics
发明人：FARBER BORIS; FARBER SOF'YA; MARTYNOV ARTUR VIKTOROVICH
权利人:FARBER BORIS; FARBER SOFYA; MARTYNOV ARTUR VIKTOROVICH
摘要:Field of application: The invention relates to chemistry, pharmacy and cosmetology, allows to synthesize of supramolecular structure on base antibiotics derivatives for use in pharmacy, cosmetology and pharmacy. n The essence of the invention: a new derivatives of antibiotics based on supramolecular structures and a method for their preparation, characterized in that the supramolecular structures are obtained by combinatorial synthesis of an antibiotic from one source molecule with two or more groups available in the reaction for covalent modification, at least with two different modifiers simultaneously, this creates a mixture of modified derivatives of the original molecule, with a maximum variety of derivatives with forming new supramolecular structure, and as biologically active substances to create pharmaceutical compositions use such supramolecular structure without separation into individual components, and in the reaction a combinatorial mixture of modified derivatives of the original molecule is formed antibiotic, the maximum number of combinations. n Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.

专利号:US-11485721-B2
优先权日:2017-11-21
标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses
发明人：KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN
权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST
摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

专利号:US-9573939-B2
优先权日:2011-09-08
标题:Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
发明人：MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN
权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN; MERCK SHARP & DOHME; MSD ITALIA SRL
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-2016130259-A1
优先权日:2013-06-24
标题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
发明人：LIU HONG; DAI XING; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; DANG QUN; PENG XUANJIA; LI PENG
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.