CAS: 4326-36-7; Boc-Tyr-Ome

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76757-90-9 1080-06-4 3417-91-2

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(Benzyloxy)Benzene置于二氯双(三邻甲苯膦)合钯(II),碘,Mercury(II) Oxide,锌体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基乙酰胺 作为反应溶剂,化学反应 50.0H,反应生成 Boc-L-酪氨酸甲酯
参考文献:An Efficient Synthesis Of [ring-14C]-L-Tyrosine From [u-14C]-Phenol
标题:An Efficient Synthesis Of [ring-14C]-L-Tyrosine From [u-14C]-Phenol
摘要:The Title Compound Was Prepared In Good Overall Yield And High Enantiopurity Via A Five Step Route Beginning With [u-C-14]-Phenol,4. Benzyl Ether 5 Was Prepared From 4 Under Standard Conditions And Underwent Selective Iodination At The 4-Position In The Presence Of Iodine And Mercuric Oxide. Palladium Catalysed Cross Coupling Of The Resulting Aryl Iodide 6 And The Organozinc Intermediate Derived From N-Tert-Butoxycarbonyl-3-Iodo-Alanine Methyl Ester,7,Proceeded Smoothly To Give 8. Debenzylation And Acid Hydrolysis Afforded The Deprotected Amino Acid As The Hydrochloride Salt. Purification (Flash Chromatography) Was Necessary In Only Two Of The Five Steps In The Synthesis.
DOI:10.1002/(Sici)1099-1344(200004)43:5<505::Aid-Jlcr336>3.0.Co;2-0

专利信息

专利号:US-2014309424-A1
优先权日:2011-06-30
标题:Direct synthesis of 18f-fluoromethoxy compounds for pet imaging and the provision of new precursors for direct radiosynthesis of protected derivatives of o-([18f] fluoromethyl) tyrosine
发明人：BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN
权利人:BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN; PIRAMAL IMAGING SA
摘要:The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18 F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([ 18 F]Fluoromethyl)tyrosines.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-8487108-B2
优先权日:2005-11-14
标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
发明人：BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

专利号:US-2010184989-A1
优先权日:2007-03-12
标 题 :De Novo Synthesis of Conjugates
发明人：RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J
权利人:NEKTAR THERAPEUTICS
摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.

专利号:KR-20140063577-A
优先权日:2011-06-30
标 题 :Direct synthesis of 18F-fluoromethoxy compounds for PET imaging and the provision of novel precursors for direct radiative synthesis of protected derivatives of O - ([18F] fluoromethyl) tyrosine

专利号:JP-2014523890-A
优先权日:2011-06-30
标题:Novel precursors for the direct synthesis of 18F-fluoromethoxy compounds for PET imaging and the direct radioactive synthesis of protected derivatives of O-([18F] fluoromethyl) tyrosine