CAS: 65550-78-9; 2-Bromo-5-Iodo-3-Methylpyridine

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3430-17-9 942206-07-7 1805025-71-1

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CAS号3430-18-0 2,5-二溴-3-甲基吡啶 | CAS号166266-19-9 2-氨基-3-甲基-5-碘吡啶 | CAS号1603-40-3 2-氨基-3-甲基吡啶 | CAS号234107-95-0 5-iodo-2-methox... | CAS号65550-80-3 2-溴-5-碘烟酸

2,5-二溴-3-甲基吡啶置于异丙基氯化镁,碘体系中,用 四氢呋喃 作为反应溶剂,化学反应 25.0H,以55%的收率获得产物2-溴-5-碘-3-甲基吡啶
参考文献:Design,Synthesis,And Structure−activity Relationship Of A Novel Series Of 2-Aryl 5-(4-Oxo-3-Phenethyl-2-Thioxothiazolidinylidenemethyl)Furans As Hiv-1 Entry Inhibitors
标题:Design,Synthesis,And Structure−activity Relationship Of A Novel Series Of 2-Aryl 5-(4-Oxo-3-Phenethyl-2-Thioxothiazolidinylidenemethyl)Furans As Hiv-1 Entry Inhibitors
摘要:We Previously Identified Two Small Molecules Targeting The Hiv-1 Gp41,N-(4-Carboxy-3-Hydroxy)Phenyl-2,5-Dimethylpyrrole 12 (Nb-2) And N-(3-Carboxy-4-Chloro)Phenylpyrrole 13 (Nb-64),That Inhibit Hiv-1 Infection At Low Micromolar Levels. Oil The Basis Of Molecular Docking Analysis,We Designed A Series Of 2-Aryl 5-(4-Oxo-3-Phenethyl-2-Thioxothiazolidinylidenemethyl)Furans. Compared With 12 And 13,These Compounds Have Bigger Molecular Size (437-515 Da) And Could occupy More Space In The Deep Hydrophobic Pocket Oil The Gp41 Nhr Trimer. Fifteen 2-Aryl 5-(4-Oxo-3-Phenethyl-2-Thioxothiazolidinylidenemethyl)Furans (11A-O) Were Synthesized By Suzuki-Miyaura Cross-Coupling Followed By A Knoevenagel Condensation And Tested For Their Anti-Hiv-1 Activity And Cytotoxicity On Mt-2 Cells. We Found That All 15 Compounds Had Improved Anti-Hiv-1 Activity And 3 Of Them (11A,11B,And 11D) Exhibited Inhibitory Activity Against Replication Of Hib-1(Iiib) And 94Ug103 At < 100 Nm Range,More Than 20-Fold More Potent Than 12 And 13,Suggesting That These Compounds Can Serve As Leads For Development Of Novel Small Molecule Hiv Fusion Inhibitors.
DOI:10.1021/jm900450N

专利信息

专利号:US-9795613-B2
优先权日:2014-12-10
标题 :GLP-1 receptor modulators
发明人：BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK
权利人:CELGENE INT II SÀRL
摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

专利号:US-9598430-B2
优先权日:2013-06-11
标 题 :GLP-1 receptor modulators
发明人：BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
权利人:RECEPTOS INC; CELGENE INT II SÀRL
摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.