CAS: 13734-36-6; N-(Tert-Butoxycarbonyl)-N-Methylglycine

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CAS号107-97-1 肌氨酸 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号4530-20-5 B°C-甘氨酸 | CAS号74-88-4 碘甲烷 | CAS号42492-57-9 N-B°C-N-甲基甘氨酸甲酯 | CAS号58632-95-4 2-(叔-丁氧基碳酰胺)-2-苯乙腈 | CAS号31954-27-5 B°C-甘氨酸甲酯 | CAS号89124-79-8 Glycine, N-carb... | CAS号1070-19-5 Carbonazidic ac... | CAS号16965-08-5 碳酸叔丁基-2,4,5-三氯苯酯 | CAS号37553-65-4 B°C-N-甲基-L-苯丙氨酸 | CAS号42492-57-9 N-B°C-N-甲基甘氨酸甲酯 | CAS号180976-09-4 (氰基甲基)(甲基)氨基甲酸叔丁酯 | CAS号57561-39-4 2-(N-B°C-N-甲基氨基)乙醇 | CAS号121492-06-6 N-B°C-N-甲基乙二胺 | CAS号123387-72-4 N-B°C-(甲氨基)乙醛 | CAS号65918-90-3 DIMETHYLCARBAMO... | CAS号80621-90-5 B°C-L-肌氨酸-羟基琥珀酰亚胺酯 | CAS号56612-14-7 2-(2-((叔丁氧基羰基)(... | CAS号5840-76-6 3-甲基恶唑烷-2,5-二酮

二碳酸二叔丁酯置于sodium Hydride,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,水 用作溶剂,化学反应 28.0H,反应生成叔丁氧羰酰基肌氨酸
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-7589170-B1
优先权日:1998-09-25
标题 :Synthesis of cyclic peptides
发明人：SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER
权利人:UNIV QUEENSLAND
摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

专利号:US-5446158-A
优先权日:1989-01-11
标题:Process for synthesis of FK-506 and tricarbonyl intermediates
发明人：JONES TODD K; MILLS SANDER G; ASKIN DAVID; REAMER ROBERT A; DESMOND RICHARD; TSCHAEN DAVID M; VOLANTE RALPH P; SHINKAI ICHIRO
权利人:MERCK & CO INC
摘要:A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.

专利号:US-10815194-B2
优先权日:2016-11-14
标题 :Process for the preparation of mono-protected α,ω-diamino alkanes
发明人：MENGE WIRO MICHAEL PETRUS BERNARDUS
权利人:BYONDIS BV
摘要:The present invention relates to a process for the synthesis of mono-protected α,ω-diamino alkanes, the use of said process in a process for the synthesis of a linker drug comprising an α,ω-diamino alkane moiety and the use of the process of the present invention in a process for preparing an antibody-drug conjugate comprising an α,ω-diamino alkane moiety.

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

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-2024392075-A1
优先权日:2021-10-14
标 题 :Solution phase polymer synthesis
发明人：GAFFNEY PIERS ROBERT JAMES; LIVINGSTON ANDREW GUY
权利人:EXACTMER LTD
摘要:A membrane-assisted process for the preparation of defined monomer sequence polymers, including oligonucleotides and peptides, in solution phase is described. The growing defined monomer sequence polymer is attached to a soluble synthesis support having properties that allow the polymer to be straightforwardly prepared in certain industry-favoured solvents with improved membrane flux and reduced fouling.