CAS: 73821-95-1; Boc-Asp(Ochx)-Oh

相似化合物

130304-80-2 73821-97-3 112259-66-2

上下游产品

CAS号24424-99-5 二碳酸二叔丁酯 | CAS号112259-66-2 L-天冬氨酸-4-环己酯 | CAS号73821-94-0 B°C-Asp(°CHex)-OBzl | CAS号30925-18-9 B°C-L-天冬氨酸1-苄酯 | CAS号108-93-0 环己醇 | CAS号30750-74-4 B°C-L-天冬氨酸酐 | CAS号141261-62-3 cyclo-RGDPhg | CAS号112259-66-2 L-天冬氨酸-4-环己酯 | CAS号13726-67-5 B°C-L-天冬氨酸

Boc-L-天冬氨酸 1-苄酯置于palladium On Activated Charcoal 4-二甲氨基吡啶,氢气,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 二氯甲烷,乙酸乙酯 作为反应溶剂,化学反应生成 Boc-L-天冬氨酸-4-环己酯
参考文献:基于l氨基酸的n型钙通道阻滞剂的结构活性研究.
标题:基于l氨基酸的n型钙通道阻滞剂的结构活性研究.
摘要:描述了基于l-氨基酸的n型钙通道阻滞剂的合成及其构效关系(sar).评价合成的化合物对n型和l型钙通道的抑制活性,重点是降低由于阻断l型钙通道而引起的心血管副作用的选择性.在筛选我们的化合物库的过程中,N-(叔丁氧羰基)-L-天冬氨酸衍生物1A被确定为一系列新的n型钙通道阻滞剂的初始铅化合物,该抑制剂可抑制钙流入imr-32个人类神经母细胞瘤细胞,Ic(50)为3.4 Microm.在使用imr-32细胞的电生理实验中,化合物1A也显示出n型钙通道电流的阻滞作用(在10 Microm处抑制34%,N = 3).作为1A氨基酸残基转化的结果,发现包含n-(叔丁氧羰基)-L-半胱氨酸的化合物12A是有效的n型钙通道阻滞剂,Ic(50)为0.61 Microm .因此,选择l-半胱氨酸作为进一步修饰的潜在结构基序.以s-环己基甲基-L-半胱氨酸为中心支架优化l-半胱氨酸的c和n端可产生有效和选
DOI:10.1016/s0968-0896(02)00558-8

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-2007179279-A1
优先权日:2005-12-30
标题:Methods for the synthesis of arginine-containing peptides
发明人：CHEN LIN; ROBERTS CHRISTOPHER R
权利人:CHEN LIN; ROBERTS CHRISTOPHER R
摘要:Methods for the synthesis of arginine-containing peptides are provided. The methods include a step that minimizes contact of side chain protected arginine with base prior to the coupling step.

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:WO-0018790-A1
优先权日:1998-09-25
标 题 :Synthesis of cyclic peptides

专利号:EP-0566824-A1
优先权日:1992-01-28
标题 :Enzymatic peptide synthesis
发明人：FELIX ARTHUR MARTIN; HEIMER EDGAR PHILIP
权利人:HOFFMANN LA ROCHE
摘要:This invention relates to a process for coupling an N-terminal amino acid residue or an N-terminal peptide fragment, each of which can be optionally substituted, to a C-terminal amino acid residue or a C-terminal peptide fragment, each of which can be optionally substituted, to form a compound having the formula n n n n        Y N -Q-X C    I n n n nwhere Y N is H or is an N-terminal amino acid residue or an N-terminal peptide fragment, each of which can be optionally substituted, Q is an acidic amino acid residue and X C is a C-terminal amino acid residue or a C-terminal peptide fragment, each of which can be optionally substituted, comprising: n   reacting a substrate component having the formula n n n n        Y N -Q-OR   II n n n nwhere R is hydrogen, alkyl, haloalkyl, aryl, aralkyl, or a 5- or 6-membered heterocyclic ring having at least one heteroatom, nwith X C in the presence of an endopeptidase in an aqueous solution or dispersion having a pH of from about 5 to about 10.5, to form the compound of formula I.

专利号:EP-0193910-A2
优先权日:1985-03-06
标题:Synthesis of a derivative of GRF and intermediate peptides