邻氯苄醇置于sodium Hydroxide体系中,用 1,4-二氧六环,苯 作为反应溶剂,化学反应 60.0H,反应生成 N-叔丁氧羰基-N'-(2-氯苄氧羰基)-L-赖氨酸 参考文献:Salem,Ezzeldin M.; Schou,O.,Indian Journal Of Chemistry-Section B Organic And Medicinal Chemistry,1980,Vol. 19,# 1,P. 62-64 标题:Salem,Ezzeldin M.; Schou,O.,Indian Journal Of Chemistry-Section B Organic And Medicinal Chemistry,1980,Vol. 19,# 1,P. 62-64
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:US-10112976-B2 优先权日:2014-06-30 标 题:Process for the production of D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide 发明人:ZHAO XINJUN; ZHENG MINYU; YU XIAOZHONG; GAO HANRONG; CORNILLE FABRICE 权利人:FLAMMA SPA 摘要:The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.
专利号:US-4011182-A 优先权日:1975-03-21 标 题:Cyclic undecapeptide analogs of somatostatin and intermediates 发明人:SARANTAKIS DIMITRIOS 权利人:AMERICAN HOME PROD 摘要:Cyclic undecapeptide analogs of somatostatin without cysteine amino acid residues and intermediates obtained in the synthesis of such compounds are described. These cyclic undecapeptides inhibit the secretion of the hormone somatotropin (growth hormone) without materially affecting glucagon levels.
专利号:US-5175146-A 优先权日:1989-12-05 标题 :Synthetic calcitonin peptides 发明人:BASAVA CHANNA; HOSTETLER KARL Y 权利人:VICAL INC 摘要:Synthetic hypocalcemic peptides which are similar in biological properties to native calcitonins as clinically useful agents. The peptides comprise analogues of native calcitonins having amino acid substitutions and deletions which act to improve potency, prolong duration of the hormonal effect, enhance receptor binding, and increase oral or nasal bioavailability. The calcitonin peptide analogues are less expensive and more easily synthesized than native calcitonins, and have improved resistance to inactivation or degradation. Methods are provided for the synthesis of these peptides. Also, disclosed are novel cyclic peptides, including calcitonin, having increased stability with respect to proteolysis. Methods for the synthesis of these peptides are provided, comprising converting disulfide cyclic peptides and proteins to enzymatically and chemically stable cyclic peptide structures by the replacement of cysteine residues with dicarboxylic acids and diamino acids. The method is applicable to various naturally occurring peptides, their synthetic analogues or derivatives, and proteins.
专利号:US-7662914-B2 优先权日:2001-06-05 标 题 :Native chemical ligation with three or more components 发明人:VILLAIN MATTEO; GAERTNER HUBERT 权利人:AMYLIN PHARMACEUTICALS INC 摘要:The invention provides a method of assembling oligopeptide intermediates in a native chemical ligation reaction that eliminates self-ligation of bi-functional intermediates. An important aspect of the invention is a bi-functional intermediate with an N-terminal cyclic thiazolidine protecting group which effectively prevents self-ligation in the chemical assembly process. The present invention is useful in methods for convergent synthesis of polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where three or more peptide fragments are used to assemble a polypeptide or protein product.