CAS: 394730-60-0; Boceprevir

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CAS号394735-28-5 (1R,2S,5S)-N-(4... | CAS号816444-90-3 (1R,2S,5S)-3-[(... | CAS号817169-86-1 2-羰基-3-氨基-4环丁烷丁酰胺盐酸盐 | CAS号394735-19-4 (1-环丁基-3-氧代丙烷-2... | CAS号394735-20-7 1-氰基-3-环丁基-1-羟基... | CAS号565456-75-9 B°C-DL-环丁基丙氨酸 | CAS号394735-18-3 (3-环丁基-1-(甲氧基(甲... | CAS号394735-17-2 2-氨基-3-环丁基丙酸乙酯 | CAS号816430-02-1 ETHYL 2-((TERT-...

1-氰基-3-环丁基-1-羟基丙烷-2-氨基甲酸叔丁酯置于n-甲基吗啉 N-甲基吗啉,盐酸,二氯乙酸,Lithium Hydroxide,氯化铵,二甲基亚砜,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,3-羟基-1,2,3-苯并三嗪-4(3H)-酮体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,水,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 152.0H,反应生成 博赛泼维
参考文献:Discovery Of (1R,5S)-N-[3-Amino-1-(Cyclobutylmethyl)-2,3-Dioxopropyl]-3-[2(S)-[[[(1,1-Dimethylethyl)Amino]Carbonyl]Amino]-3,3-Dimethyl-1-Oxobutyl]-6,6-Dimethyl-3-Azabicyclo[3.1.0]Hexan-2(S)-Carboxamide (Sch 503034),A Selective,Potent,Orally Bioavailable Hepatitis C Virus Ns3 Protease Inhibitor: A Potential Therapeutic Agent For The Treatment Of Hepatitis C Infection
标题:Discovery Of (1R,5S)-N-[3-Amino-1-(Cyclobutylmethyl)-2,3-Dioxopropyl]-3-[2(S)-[[[(1,1-Dimethylethyl)Amino]Carbonyl]Amino]-3,3-Dimethyl-1-Oxobutyl]-6,6-Dimethyl-3-Azabicyclo[3.1.0]Hexan-2(S)-Carboxamide (Sch 503034),A Selective,Potent,Orally Bioavailable Hepatitis C Virus Ns3 Protease Inhibitor: A Potential Therapeutic Agent For The Treatment Of Hepatitis C Infection
摘要:Hepatitis C Virus (Hcv) Infection Is The Major Cause Of Chronic Liver Disease,Leading To Cirrhosis And Hepatocellular Carcinoma,Which Affects More Than 170 Million People Worldwide. Currently The Only Therapeutic Regimens Are Subcutaneous Interferon-Alpha Or Polyethylene Glycol (Peg)-Interferon-Alpha Alone Or In Combination With Oral Ribavirin. Although Combination Therapy Is Reasonably Successful With The Majority Of Genotypes,Its Efficacy Against The Predominant Genotype (Genotype 1) Is Moderate At Best,With Only About 40% Of The Patients Showing Sustained Virological Response. Herein,The Sar Leading To The Discovery Of 70 (Sch 503034),A Novel,Potent,Selective,Orally Bioavailable Ns3 Protease Inhibitor That Has Been Advanced To Clinical Trials In Human Beings For The Treatment Of Hepatitis C Viral Infections Is Described. X-Ray Structure Of Inhibitor 70 Complexed With The Ns3 Protease And Biological Data Are Also Discussed.
DOI:10.1021/jm060325B

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-8987493-B2
优先权日:2010-05-20
标题 :Process for synthesis of silane dipeptide analogs
发明人：SIEBURTH SCOTT MCNEILL; BO YINGJIAN
权利人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN; Temple University—Of the Commonwealth System of Higher Education
摘要:The invention provides a method of preparing silane dipeptide analogs, comprising the steps of treating a solution of a substituted 1,2-oxasilolane with lithium metal to form a solution of the dilithium salt of a substituted 3-hydroxypropylsilanol, and reacting the solution of the dilithium salt of the substituted 3-hydroxypropylsilanol with a substituted enamine.

专利号:US-8686145-B2
优先权日:2010-02-25
标 题 :Process for the preparation of α-acyloxy β-formamido amides
发明人：RUIJTER EELCO; ORRU ROMANO; ZNABET ANASS; POLAK MARLOES; TURNER NICHOLAS
权利人:RUIJTER EELCO; ORRU ROMANO; ZNABET ANASS; POLAK MARLOES; TURNER NICHOLAS; VERENIGING VOOR CHRISTELIJK HOGER ONDERWIJS WETENSCHAPPELIJK ONDERZOEK EN PATIENTENZORG C O TECHNOLO
摘要:The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R 2 COOH and a compound of the general Formula IV R 3 NC under such conditions that compound I is formed, wherein R 1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R 2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R 3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.

专利号:US-2018148745-A1
优先权日:2015-05-26
标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor
发明人：ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN
权利人:CALIFORNIA INST OF TECHN; PROVIVI INC
摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.

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-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.