CAS: 2628280-40-8; Nirmatrelvir

(1R,2S,5S)-6,6-Dimethyl-3-(3-Methyl-L-Valyl)-3-Azabicyclo[3.1.0]Hexane-2-Carboxylic Acid Hydrochloride Salt置于伯吉斯试剂,三乙胺,N,N-二异丙基乙胺,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-)体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 3.0H,反应生成帕罗韦德
参考文献:冠状病毒主要蛋白酶抑制剂nirmatrelvir的弹头替代研究
标题:冠状病毒主要蛋白酶抑制剂nirmatrelvir的弹头替代研究
摘要:自 2019 年 12 月出现以来,Sars-Cov-2 大流行目前正在引起前所未有的全球卫生紧急情况.2021 年 12 月,Fda 授予 Sars-Cov-2 主要蛋白酶抑制剂 Nirmatrelvir 紧急使用授权,用于治疗感染患者.这种肽模拟物设计有一个腈弹头,它与病毒蛋白酶形成共价键.在此,我们研究了具有不同弹头的 Nirmatrelvir 类似物及其抑制活性.此外,还研究了针对人类甲型冠状病毒 229E 的抗病毒活性以及基于细胞的测定.我们发现羟甲基酮和酮苯并噻唑弹头与腈弹头等效,这表明这些类似物也可用于治疗冠状病毒感染.
Doi:10.1021/acsmedchemlett.2C00260

专利信息

专利号:WO-2023083926-A1
优先权日:2021-11-12
标题 :Synthesis of (1r,2s,5s)-n-((s)-1-cyano-2-((s)-2-oxopyrrolidin-3-yl)ethyl)-3-((s)-3,3-dimethyl-2- (2,2,2-trifluoroacetamido)butanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
发明人：ZUPANCIC SILVO; RUZIC MILOS; SENICAR TANJA; BEZENSEK JURE
权利人:KRKA D D NOVO MESTO
摘要:The invention relates to a process for the synthesis of (1R,2S,5S)-N-((S)-1-cyano-2-((S)-2-oxopyrroli- din-3-yl)ethyl)-3-((S)-3,3-dimethyl-2-(2,2,2-trifluoroacetamido)butanoyl)-6,6-dimethyl-3-azabicy- clo[3.1.0]hexane-2-carboxamide.

专利号:WO-2023151188-A1
优先权日:2022-02-08
标题 :Green synthesis method of antiviral drug intermediate
发明人：XIA BIN; WANG JIAMING; ZHANG XIANSHU; CAI LINGLI; WANG ZIKUN; CAO MING; YANG SHAOBO; GAO QIANG; ZHENG BAOFU
权利人:SHANGHAI HAOYUAN CHEMEXPRESS CO LTD
摘要:The present application provides a green synthesis method of an antiviral drug intermediate. The method comprises: in the presence of a catalyst, adding zinc powder into a compound as represented by a formula II and performing a cyclization reaction with dihaloalkane to generate a compound as represented by a formula I, zinc halide being not required to be added to the cyclization reaction, wherein R1 is selected from H or an amino-protecting group, and R2 is selected from substituted or unsubstituted C1-C10 alkyl, substituted or unsubstituted C6-C14 aryl or substituted or unsubstituted C7-C14 aralkyl; R3 and R4 are each independently selected from hydrogen, substituted or unsubstituted C1-C10 alkyl, and R3 and R4 can be connected to form a fatty ring containing 3-10 carbon atoms. The synthesis method is short in steps, dangerous and expensive materials are not used, a reaction conversion rate is high, reaction time is short, and operation is easy and convenient. Production costs and post-treatment costs are reduced, and a cost advantage is obvious. The method can be widely used for preparing antiviral drugs of nirmatrelvir, boceprevir or narlaprevir, and has good market prospects.

专利号:WO-2025076406-A1
优先权日:2023-10-05
标题:Synthesis and evaluation of 9-aminoacridines with sars-cov-2 antiviral activity
发明人：JONES THANE; LANE THOMAS; MAKAROV VADIM; EKLINS SEAN
权利人:COLLABORATIONS PHARMACEUTICALS INC
摘要:The synthesis and characterization of a series of derivatives and analogs based on the 9-aminoacridine scaffold shared by antimalarial drugs quinacrine and pyronaridine are described. Also described is the structure-activity relationship of these compounds against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus that causes the coronavirus disease of 2019 (COVID-19). Several compounds displayed potent in vitro activity, with 50% inhibitory concentrations below 1 micromolar.

专利号:WO-2024131056-A1
优先权日:2022-12-20
标 题:Synthesis method for intermediate of paxlovid and of boceprevir
发明人：YANG XIAOLONG; PEI PIBING; CHEN QIAN; YANG TIEBO; Yang Kaimike
权利人:HUANGGANG LUBAN PHARMACEUTICAL CO LTD
摘要:Disclosed in the present invention is a novel method for synthesizing a compound represented by formula 1. The method comprises: reacting diphenyl sulfide with 2-bromopropane to obtain a compound represented by formula 5; reacting a compound represented by formula 4 with the compound represented by formula 5 to obtain a compound represented by formula 6; and subjecting the compound represented by formula 6 to deprotection and salt forming under the effect of hydrogen chloride, so as to obtain the compound represented by formula 1. The method of the present invention can be carried out under mild conditions, thereby facilitating industrial production and further improving the reaction yield.

专利号:US-2025270523-A1
优先权日:2023-03-01
标题 :Rna polymerase variant, and preparation method therefor and use thereof in rna synthesis
发明人：XU XIAOYU; Jin Qiuheng; HE WEI; WANG CHONG; HU HUIXUE
权利人:NANJING VAZYME BIOTECH CO LTD
摘要:Provided are an RNA polymerase variant and a preparation method therefor. When the RNA polymerase variant is used in in-vitro transcription, an RNA product with low dsRNA contamination and a high integrity can be obtained, the utilization efficiency of cap analogs in the co-transcriptional capping reaction system can also be improved, and costs are saved. In addition, further provided is a method for generating RNA by means of in-vitro transcription.

专利号:CN-119506238-A
优先权日:2023-08-22
标题:Mutant monoamine oxidase and application thereof in synthesis of chiral amine compound