CAS: 45170-31-8; N-(Tert-Butoxycarbonyl)-N-Methyl-L-Valine

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CAS号13734-41-3 B°C-L-缬氨酸 | CAS号74-88-4 碘甲烷 | CAS号77-78-1 硫酸二甲酯 | CAS号172096-96-7 (4S)-N-tert-but... | CAS号2480-23-1 N-甲基-L-缬氨酸 | CAS号41840-28-2 S-B°C-2-巯基-4,6-二甲基嘧啶 | CAS号72-18-4 l-缬氨酸 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1070-19-5 Carbonazidic ac... | CAS号3339-44-4 N-甲基-L-缬氨酸甲酯盐酸盐 | CAS号24164-06-5 (S)-2-((叔丁氧基羰基)...

L-缬氨酸置于sodium Hydride,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,水 作为反应溶剂,化学反应 28.0H,反应生成 Boc-N-甲基-L-缬氨酸
参考文献:设计,合成和体外抗疟原虫活性的4-氨基喹啉含有修饰的氨基酸缀合物.
标题:设计,合成和体外抗疟原虫活性的4-氨基喹啉含有修饰的氨基酸缀合物.
摘要:摘要合成了一系列新的侧链修饰的4-氨基喹啉,并筛选了针对恶性疟原虫的氯喹敏感(3D7)和耐氯喹(k1)菌株的体外抗血浆活性.间的系列中,化合物30和31表现出对的k1株寄生虫生长的抑制显著恶性疟原虫与ic 50个值0.28和0.31μm,分别,而化合物34,35,和38显示出优异的活性针对k1菌株的ic 50值分别为0.18,0.22和0.17 µm,而氯喹(cq)的值为0.255 µm.所有化合物在1.54至> 34.48之间均显示出非常好的抗性因子,而cq为51.0.发现所有这些类似物均与血红素形成强复合物,并在体外抑制β-血红素的形成,表明这类化合物可作用于血红素聚合目标.总体结果表明,本系列化合物似乎有望用于进一步的铅优化以获得对耐药性寄生虫具有活性的化合物. 图形概要
DOI:10.1007/s00044-016-1555-5

专利信息

专利号:US-7312343-B2
优先权日:2004-06-02
标 题:Synthesis of α-amino-β-alkoxy-carboxylic acid esters
发明人：SCHMID RUDOLF; ZUTTER ULRICH
权利人:HOFFMANN LA ROCHE
摘要:Compounds of formula I n nand a process for the preparation of such compounds are disclosed.

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-2005192265-A1
优先权日:2003-03-20
标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-6906056-B2
优先权日:1998-06-22
标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J
权利人:LILLY CO ELI
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-8633224-B2
优先权日:2002-03-22
标题 :Hemiasterlin derivatives and uses thereof in the treatment of cancer
发明人：KOWALCZYK JAMES J; KUZNETSOV GALINA; SCHILLER SHAWN; SELETSKY BORIS M; SPYVEE MARK; YANG HU
权利人:KOWALCZYK JAMES J; KUZNETSOV GALINA; SCHILLER SHAWN; SELETSKY BORIS M; SPYVEE MARK; YANG HU; EISAI CO LTD
摘要:The present invention provides compounds having formula (I): n n n n n n n n n n n n and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R 1 -R 7 , X 1 , X 2 , R, Q, and n are as defined herein.

专利号:US-7579323-B1
优先权日:1997-12-19
标 题:Hemiasterlin analogs
发明人：ANDERSEN RAYMOND; PIERS EDWARD; NIEMAN JAMES; COLEMAN JOHN; ROBERGE MICHEL
权利人:UNIV BRITISH COLUMBIA
摘要:This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as cytotoxic and anti-mitotic agents.