相似化合物
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B°C-glycine Isopropenyl Succinimido Carbonate 1,2,2,2-tetrachloroethyl-(N-succinimidyl)carbonate bis(N-hydroxysuccinimide) sulfite3)CH2COOHB°C-Gly-SCH(CH3)CH2COOH N-t-butoxycarbonyl-glycyl-L-methionine N-tert-butoxycarbonylglycyl-L-α-aminoadipic acid α-benzhydryl ester -L-tyrosine ethyl esterN-(benzyloxycarbonyl)-O-(tert-butoxycarbonyl)glycyl-L-tyrosine ethyl ester 2-(叔丁氧羰基氧亚氨基)-2-苯乙腈置于n,N'-二环己基碳二亚胺体系中,用 四氢呋喃,1,4-二氧六环,水 作为反应溶剂,化学反应 4.0H,反应生成 Boc-甘氨酸-N-羟基琥柏酰亚胺酯
参考文献:Dtdtpa配合物的新苄基取代衍生物的弛豫性和金属转移稳定性
标题:Dtdtpa配合物的新苄基取代衍生物的弛豫性和金属转移稳定性
摘要:在寻找具有更高弛豫度和选择性的新型特殊造影剂的过程中,我们准备了两种新型的苄基官能化的dtpa("二亚乙基三胺五乙酸盐")g配合物(S)-3和(r,S)-4,并对其进行了比较.具有与已知的区域异构体(S)-2和(S)-1相同的性质.所述的降低的横向弛豫率的理论拟合17 H的o形核2 ø得到的水的滞留时间值(τ中号)在310 K时为86-143 Ns,该值并不限制质子在体温下的弛豫性.1个h-NMRd(核磁松弛分散体)概况表明的弛豫1-4(-[r 1 = 4.3-5.1小号-1 毫-1在20兆赫和310 K)比用于gddtpa母体化合物更高5.过渡金属化评估表明,除(S)-2外,所有取代的化合物都比5更稳定.配合物3,1和4对zn 2+诱导的金属转移具有最高的稳定性(以降序排列).显然,分别在位置5,4和2的苄基取代基的空间位阻有利地降低了zn离子的可及性.从合成的观点来看,类型1的4
DOI:10.1002/hlca.200490098
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专利信息
专利号:US-7781488-B2
优先权日:2002-06-10
标 题:Post-cleavage sulfur deprotection for convergent protein synthesis by chemical ligation
发明人:BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT
权利人:AMYLIN PHARMACEUTICALS INC
摘要:The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
专利号:US-2025091989-A1
优先权日:2023-09-19
标 题 :Small molecule protein synthesis modulators
发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-4105652-A
优先权日:1977-08-05
标 题 :Synthesis of human β-endorphin
发明人:MEIENHOFER JOHANNES ARNOLD; WANG SU-SUN
权利人:HOFFMANN LA ROCHE
摘要:Human β-endorphin (β h -endorphin) is prepared by solution phase peptide synthesis. Synthesis proceeded via the protected β-endorphin fragments 1-9, 10-18, 19-21 and 22-31.
专利号:US-4891430-A
优先权日:1984-12-04
标 题:Process for synthesizing active esters of carboxylic acids, new alpha-halogenated carbonates which are useful for this synthesis and the method of producing them
发明人:BARCELO GERARD; CASTRO BERTRAND; JAOUADI MAHMOUD; MARTINEZ JEAN; SENET JEAN-PIERRE; SENNYEY GERARD
权利人:INT DES POUDRES ET EXPLOSIFS S
摘要:The invention relates to a new process for preparing active esters or carboyxlic acids, which consists in reacting a carboxylic acid, in the presence of an agent for binding hydrohalic acid, with a carbonate of formula: ##STR1## in which R 1 denotes either a radical of formula ##STR2## in which R 3 and R 4 , which may be identical or different, are not hydrogen atoms and denote organic radicals which may be substituted or unsubstituted and saturated or unsaturated, and may or may not be bound to a polymer, and which can be joined together to form a hetero-cyclic system with the nitrogen, atom, n or a substituted or unsubstituted aryl radical which may or may not be bound to a polymer, n R 2 denotes a hydrogen atom, an aliphatic or cycloaliphatic radical which may be substituted or unsubstituted and saturated or unsaturated, or a substituted or unsubstituted aromatic radical, n and X denotes a halogen atom. n This process is especially useful for the synthesis of active esters of N-protected amino acids. The invention also relates to the new carbonates described above and the method of producing them, which consists in reacting an alpha-halogenated chloroformate of formula: n n R.sup.2 --CHX--O--COCl n n with an alcohol of formula R 1 OH in an inert solvent medium in the presence of an organic or inorganic base.
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-2023064991-A1
优先权日:2021-10-22
标题 :Process for preparing bicyclic glycine-proline compounds and monocyclic glycine-proline intermediates thereof
发明人:SCOTT JEREMY PETER; KEEN STEPHEN PHILIP; ESPENSEN GEORGE MAX; PARRY-JONES DAVID; LAWRENCE RONNIE MAXWELL; BLOWER CLIVE JOHN
权利人:NEUREN PHARMACEUTICALS LTD
摘要:The present disclosure generally relates to a process for the synthesis of bicyclic glycine-proline compounds, and monocyclic glycine-proline intermediates thereof. In particular, the present disclosure also relates to a process for the synthesis of cyclic G-2-AllylP and its analogues. The present disclosure also relates to a process for the synthesis of optionally protected monocyclic glycine-proline intermediates. The present disclosure also relates to a process for the synthesis of esterified glycine-proline intermediates. The present disclosure also relates to compounds prepared by the processes and the use of such compounds to prepare compositions and to treat disorders.