CAS: 923604-59-5; (2R,3Ar,11As,12Ar,14Ar,Z)-N-(Cyclopropylsulfonyl)-2-((2-(4-Isopropylthiazol-2-yl)-7-Methoxy-8-Methylquinolin-4-yl)Oxy)-5-Methyl-4,14-Dioxo-2,3,3A,4,5,6,7,8,9,11A,12,13,14,14A-Tetradecahydrocyclopenta[c]Cyclopropa[g][1,6]Diazacyclotetradecine-12A(1H)-Carbo

上下游产品

(2R,3Ar,11As,12Ar,14Ar,Z)-2-((2-(4-异丙基吡啶-2-基)-7-甲氧基-8-甲基喹啉-4-基)氧基)-5-甲基-4,14-二氧代-2,3,3A,4,5,6,7,8,9,11A,12,13,14,14A-十四氢环戊[c]环丙并[g][1,6]二氮杂环四氢萘-12A(1H)-羧酸 (2R,3Ar,10Z,11As,12Ar,14Ar)-2-({7-Methoxy-8-Methyl-2-[4-(Propan-2-yl)-1,3-Thiazol-2-Yl]Quinolin-4-Yl}Oxy)-5-Methyl-4,14-Dioxo-2,3,3A,4,5,6,7,8,9,11A,12,13,14,14A-Tetradecahydrocyclopenta[c]Cyclopropa[g][1,6]Diazacyclotetradecine-12A(1H)-Carboxylic Acid 923604-58-4
(2R,3Ar,11As,12Ar,14Ar,Z)-2-(2-(4-异丙基噻唑-2-基)-7-甲氧基-8-甲基-4-喹啉氧基)-5-甲基-4,14-二氧-1,2,3,3A,4,5,6,7,8,9,11A,12,12A,13,14,14A-16氢环戊烷并[c]环丙基并[g][1,6]双氮杂十四烷-12A-羧酸乙酯 2,3,3A,4,5,6,7,8,9,11A,12,13,14,14A-Tetradecahydro-2-[[7-Methoxy-8-Methyl-2-[4-10(1-Methylethyl)-2-Thiazolyl]-4-Quinolinyl]Oxy]-5-Methyl-4,14-Dioxo-(2R,3Ar,10Z,11As,2Ar,14Ar)-Cyclopenta[c]Cyclopropa[g][1,6]Diazacyclotetradecine-12A(1H)-Carboxylic Acid Ethyl Ester 923604-57-3
(1R,2S)-2-乙烯基-1-[[[(1R,2R,4R)-2-[(5-己烯-1-基甲基氨基)羰基]-4-[[7-甲氧基-8-甲基-2-[4-异丙基-2-噻唑基]-4-喹啉基]氧基]环戊基]羰基]氨基]环丙烷羧酸乙酯 Ethyl (1R,2S)-2-Ethenyl-1-({[(1R,2R,4R)-2-[hex-5-En-1-Yl-(Methyl)Carbamoyl]-4-({7-Methoxy-8-Methyl-2-[4-(Propan-2-yl)-1,3-Thiazol-2-Yl]Quinolin-4-Yl}Oxy)Cyclopentyl]Carbonyl}-Amino)Cyclopropanecarboxylate 923604-56-2
(1R,3S,4Z,12R,14R,16R)-14-[7-Methoxy-8-Methyl-2-(4-Propan-2-Yl-1,3-Thiazol-2-yl)Quinolin-4-Yl]Oxy-10-Methyl-18-Oxa-10,20-Diazatetracyclo[15.2.1.01,3.012,16]Icosa-4,17(20)-Diene-11,19-Dione 923604-55-1

(1R,4R,5R)-3-氧代-2-氧杂双环[2.2.1]庚烷-5-羧酸置于二氯(邻异丙氧基苯基亚甲基)(三环己基膦)钌,甲烷磺酸,Lithium Hydroxide Monohydrate,偶氮二甲酸二异丙酯,2-乙氧基-1-乙氧碳酰基-1,2-二氢喹啉,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三苯基膦,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,二氯甲烷,水,1,2-二氯乙烷,异丙醇,丙酮,甲苯 作为反应溶剂,化学反应 214.0H,反应生成 司美匹韦
参考文献:Ring-Closing Metathesis On Commercial Scale: Synthesis Of Hcv Protease Inhibitor Simeprevir
标题:Ring-Closing Metathesis On Commercial Scale: Synthesis Of Hcv Protease Inhibitor Simeprevir
摘要:The Key Macrocyclization Step In The Synthesis Of Simeprevir,A Hepatitis C Virus (Hcv) Antiviral Drug,Was Studied. N-Boc Substitution On The Diene Precursor Changes The Site Of Insertion Of The Metathesis Catalyst And,Consequently,The Kinetic Model Of The Ring Closing Metathesis (Rcm),Enabling A Further Increase In The Macrocyclization Efficiency Under Simulated High Dilution (Shd) Conditions. NMR Of The Inserted Species Of Both First And Second Generation Rcm Catalysts Are Reported And Discussed.
DOI:10.1021/acs.Joc.8B03124

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-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.

专利号:US-9227965-B2
优先权日:2011-09-22
标题 :Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV
发明人：HORVATH ANDRAS; DEPRÉ DOMINIQUE PAUL MICHEL; ORMEROD DOMINIC JOHN
权利人:JANSSEN PHARMACEUTICALS INC
摘要:Disclosed is a process for the preparation of a cinchonidine salt of formula (IV) via an aqueous solution of a racemic 4-hydroxy-1,2-cyclopentanedicarboxylic acid, which is subjected to cyclization without removing water, by the addition of a water-miscible organic solvent to the aqueous solution and, again without removing water, adding cinchonidine to the aqueous-organic solvent solution so as to obtain the cinchonidine salt of the lactone acid. The cinchonidine salt is allowd to crystallize so as to obtain the enantiomerically purified crystalline lactone acid cinchonidine salt (IV). The enantiomerically pure salt is an intermediate in the synthesis of HCV inhibitor compound of formula (I).

专利号:US-9364482-B2
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：DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; ZORN NICOLAS; DANG QUN; MCCOMAS CASEY C; PENG XUANJIA; LI PENG; SOLL RICHARD
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. (I)

专利号:US-9265773-B2
优先权日:2011-09-08
标题 :Tetracyclic heterocycle 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; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI
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; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI; 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.