CAS: 102195-79-9; (2S,4S)-1-Tert-Butyl 2-Methyl 4-Hydroxypyrrolidine-1,2-Dicarboxylate

上下游产品

(2S,4S)-1-t-butoxycarbonyl-4-formyloxy-2-methoxycarbonylpyrrolidine B°C-(2S,4S)-p-nitrobenzoate-4-hydroxyproline methyl ester tert-butyl dicarbonatedi-tert-butyl dicarbonate cis-L-hydroxyproline methyl ester(S)-1-tert-butyl 2-methyl 4-oxopyrrolidine-1,2-dicarboxylate phenoxy>)-OMeN-B°C-L-trans-Pro(4-4-(E)-2-(4-cyanophenyl)-1-diazenylphenoxy)-OMe 1-tert-butyl 2-methyl (2S,4R)-4-azido-1,2-pyrrolidinedicarboxylate 1-tert-butyl 2-methyl (2S,4S)-4-{[(4-bromo-phenyl)sulfonyl]oxy}-pyrrolidine-1,2-dicarboxylate

L-羟基脯氨酸置于甲醇,Sodium Azide,偶氮二甲酸二异丙酯,Potassium Carbonate,三苯基膦,Sodium Hydroxide体系中,用 1,4-二氧六环,二氯甲烷,水,丙酮 用作溶剂,化学反应 29.0H,反应生成N-Boc-顺式-4-羟基-L-脯氨酸甲酯
参考文献:4R-和4S-碘苯基羟脯氨酸,4R-戊酰羟脯氨酸和s-炔丙基-4-硫醇苯丙氨酸:用于生物正交反应的构象偏向和可调氨基酸†
标题:4R-和4S-碘苯基羟脯氨酸,4R-戊酰羟脯氨酸和s-炔丙基-4-硫醇苯丙氨酸:用于生物正交反应的构象偏向和可调氨基酸†
摘要:生物正交反应允许将新功能引入肽,蛋白质和其他生物分子中.用于生物正交反应的最容易获得的氨基酸具有适度的构象偏好或分子相互作用的基础.在此,我们描述了用于生物正交反应的 4 种含有官能团的新型氨基酸的合成.羟脯氨酸的( 2S,4R )-和( 2S,4S )-碘苯醚能够在水中通过快速,特异性的suzuki和sonogashira反应进行修饰.这些氨基酸(如 Boc-,Fmoc-和游离氨基酸)的合成是通过简洁的序列实现的.这些氨基酸表现出明确的构象偏好,其中 4 S-碘苯基羟脯氨酸在晶体学上表现出 β 转角 ( Phi,ψ ∼-80°,0°) 或相对延伸 ( Phi,ψ ∼-80°,+170°)构象,而 4 R-非对映异构体更喜欢更紧凑的构象 ( Phi ∼-60°).芳氧基脯氨酸非对映体以高度不同的方式呈现芳基,表明它们在分子设计,药物化学和催化中的立体定向用途.因此,
Doi:10.1039/c5Ob02473K

专利信息

专利号:US-2011104057-A1
优先权日:2008-05-20
标题:Novel [F-18]-labelled L-glutamic acid and L-glutamine derivatives (II), their use and processes for their preparation
发明人：DINKELBORG LUDGER; GRAHAM KEITH; BERNDT MATHIAS; KOGLIN NORMAN; SCHMITT-WILLICH HERIBERT; FRIEBE MATTHIAS; LEHMANN LUTZ
权利人:BAYER SCHERING PHARMA AG
摘要:What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

专利号:US-9308282-B2
优先权日:2008-05-20
标 题:[F-18]-labelled L-glutamic acid and L-glutamine derivatives (I), their use and processes for their preparation
发明人：FRIEBE MATTHIAS; SCHMITT-WILLICH HERIBERT; BERNDT MATTHIAS; DINKELBORG LUDGER; KOGLIN NORMAN; GRAHAM KEITH
权利人:PIRAMAL IMAGING SA
摘要:What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

专利号:US-8591878-B2
优先权日:2008-02-25
标 题:Therapeutic compounds
发明人：MCCAULEY JOHN A; LIVERTON NIGEL J; HARPER STEVEN; MCINTYRE CHARLES J; RUDD MICHAEL T
权利人:MCCAULEY JOHN A; LIVERTON NIGEL J; HARPER STEVEN; MCINTYRE CHARLES J; RUDD MICHAEL T; MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO
摘要:A class of macrocyclic compounds of formula (I), wherein R 1 , R 3 , R 4 , R a , R b , A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.

专利号:US-8309540-B2
优先权日:2006-10-24
标 题:HCV NS3 protease inhibitors
发明人：LIVERTON NIGEL J; VACCA JOSEPH P; MCCAULEY JOHN A; ROMANO JOSEPH J; RUDD MICHAEL T
权利人:LIVERTON NIGEL J; VACCA JOSEPH P; MCCAULEY JOHN A; ROMANO JOSEPH J; RUDD MICHAEL T; MERCK SHARP & DOHME
摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. (I)

专利号:US-8518952-B2
优先权日:2008-08-06
标题 :6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors
发明人：BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER
权利人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER; PFIZER
摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.

专利号:US-7879797-B2
优先权日:2005-05-02
标 题 :HCV NS3 protease inhibitors
发明人：HOLLOWAY M KATHARINE; LIVERTON NIGEL J; LUDMERER STEVEN W; MCCAULEY JOHN A; OLSEN DAVID; RUDD MICHAEL T; VACCA JOSEPH P
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.