CAS: 158257-40-0; (3S,4S)-4-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-Hydroxy-6-Methylheptanoic Acid

相似化合物

58521-49-6 940301-35-9 66967-01-9

上下游产品

CAS号82911-69-1 9-芴甲基-N-琥珀酰亚胺碳酸酯 | CAS号67010-44-0 (3R,4S)-(t-buty... | CAS号125814-21-3 NALPHA-9-Fluore...

📜Boc-(3R,4S)-Statine Ethyl Ester置于lithium Hydroxide,甲基磺酰氯,三乙胺体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 4.75H,反应生成(3S,4S)-4-[(芴甲氧羰基)氨基]-3-羟基-6-甲基庚酸
参考文献:Total Synthesis Of Miraziridine A And Identification Of Its Major Reaction Site For Cathepsin B
标题:Total Synthesis Of Miraziridine A And Identification Of Its Major Reaction Site For Cathepsin B
摘要:The Synthesis Of Miraziridine A,A Pentapeptide Derivative Isolated From Marine Sponge,And Its Truncated Analogs Has Been Achieved. To Construct The Backbone Of Miraziridine A,A Side-Chain-Unprotected Vinylogous Arginine Was Condensed With An Aziridine-Containing Fragment Prepared By A Conventional Solid-Phase Procedure. An Analog Lacking The Vinylogous Arginine Site Showed Comparable Inhibitory Activity With Miraziridine A,Whereas An Analog Lacking The Aziridine Site Showed Remarkably Weak Inhibitory Activity For Cathepsin B. (C) 2007 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Tet.2007.06.082

专利信息

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-5847150-A
优先权日:1996-04-24
标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
发明人：DORWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-8598089-B2
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries
发明人：MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A
权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC
摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.

专利号:US-8410028-B2
优先权日:2003-12-17
标 题:Methods for synthesis of encoded libraries
发明人：MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A
权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC
摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.

专利号:US-2007042401-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries

专利号:US-2012245040-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries