CAS: 77611-37-1; (S)-2-((Tert-Butoxycarbonyl)Amino)-6-Hydroxyhexanoic Acid

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81505-64-8 1359971-57-5 81505-49-9

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CAS号77302-72-8 B°C-L-2-氨基己二酸 | CAS号6033-32-5 L-6-羟基正亮氨酸 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号13734-28-6 B°C-L-赖氨酸

📜N-Alpha-叔丁氧羰基-L-赖氨酸置于sodium Nitroprusside,Sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应 6.0H,以38%的收率获得产物boc-L-6-羟基正亮氨酸
参考文献:含有deks基序作为构象受限的胶原蛋白端肽类似物的环肽:合成和构象分析†
标题:含有deks基序作为构象受限的胶原蛋白端肽类似物的环肽:合成和构象分析†
摘要:胶原蛋白端肽在赖氨酰氧化酶介导的交联中起重要作用,该过程在肿瘤进展过程中被解除调节.有人建议,位于i型胶原α1链n端肽的n端肽中的deks基序在对接至其三螺旋受体结构域时采用βi转构象,这似乎对赖氨酰氧化酶催化是至关重要的.脱氨和随后通过席夫碱的形成进行交联.在此,将描述以dek构象约束deks序列的环肽的设计和合成.赖氨酸侧链连接到2-氯三苯甲基氯改性的聚苯乙烯树脂上,然后进行微波辅助的固相肽合成和树脂上的环化反应,可以有效地从头到尾环化deks衍生的环状五肽和六肽.一个ñ ε-(4-氟苯甲酰基)赖氨酸残基被包括在环肽,以允许它们的潜在的放射性标记用氟-18为赖氨酰氧化的pet成像.通过1 H NMR和手性(电子和振动cd)光谱以及md模拟进行的构象分析表明,D-脯氨酸和另外的赖氨酸的同时掺入可用于潜在的放射性标记附着,从而可靠地诱导了所需的βi-Turn结构. Dmso和水中的de
DOI:10.1039/c4Ob02348J

专利信息

专利号:US-6063919-A
优先权日:1998-08-14
标题:Process for the synthesis of exochelins
发明人：GAUDIOSO LARRY A; WEGLARZ MICHAEL A
权利人:KEYSTONE BIOMEDICAL INC
摘要:A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc- epsilon -hydroxynorleucine and reacting same to produce L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester to give an L-N2-Boc-N6-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N2-Boc-N6-methyl, N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.

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-6335443-B1
优先权日:1998-08-14
标 题 :Chemical synthesis of exochelins
发明人：GERACI LEO S; LEVY STUART G; HUDSPETH JAMES P; BUSWELL RICHARD L; STEARNS JAY F
权利人:KEYSTONE BIOMEDICAL INC
摘要:A process for the synthetic generation of high affinity, iron binding compounds known as Exochelins, and more particularly, to a synthetic process for making Exochelins and to modifications to these newly synthesized compounds to vary their physiological properties, including applications of these newly synthesized and utile compounds for diagnosing and treating disease in mammals.

专利号:WO-0009547-A1
优先权日:1998-08-14
标题:Novel process for the synthesis of exochelins

专利号:US-9187524-B2
优先权日:2010-09-15
标题 :Broad spectrum antibiotic arylomycin analogs
发明人：ROMESBERG FLOYD E; SMITH PETER A; ROBERTS TUCKER C
权利人:ROMESBERG FLOYD E; SMITH PETER A; ROBERTS TUCKER C; SCRIPPS RESEARCH INST
摘要:Arylomycin analogs are provided, wherein the analogs can have broad spectrum bioactivity. Resistance to the antibiotic bioactivity of natural product arylomycin in a range of pathogenic bacterial species has been found to depend upon single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases), wherein the presence of a proline residue confers arylomycin resistance. Arylomycin analogs are provided herein that can overcome that resistance and provide for a broader spectrum of antibiotic bioactivity than can natural product arylomycins such as arylomycin A2. Methods for determining if a bacterial strain is susceptible to narrow spectrum arylomycin antibiotics, or if a broad spectrum analog is required for treatment, is provided. Pharmaceutical compositions and methods of treatment of bacterial infections, and methods of synthesis of arylomycin analogs, are provided.

专利号:CZ-2001530-A3
优先权日:1999-08-11
标 题:Process for the synthesis of exochelins