N-叔丁氧羰基-L-谷氨酸 5-甲酯置于ammonium Hydroxide体系中,用 水 用作溶剂,化学反应生成Boc-L-谷氨酰胺 参考文献: A Process For The Preparation Of L-Glutamine[fr] Procédé De Préparation De L-Glutamine 标题: A Process For The Preparation Of L-Glutamine[fr] Procédé De Préparation De L-Glutamine 摘要:本发明涉及一种制备化学式(i)的l-谷氨酰胺的方法.本发明还涉及一种改进的用于纯化具有特定堆积密度和豪斯纳比的化学式(i)的l-谷氨酰胺的方法.
专利号:US-4515920-A 优先权日:1984-04-30 标题 :Synthesis of peptides and proteins 发明人:ERICKSON BRUCE W 权利人:UNIV ROCKEFELLER 摘要:Solid phase synthesis of peptides and proteins have been improved by the use of a trifunctional segment, one functional group of which is bound to a solid support, the other two functional groups being available as substrates upon which identical proteins are synthesized.
专利号:US-4786684-A 优先权日:1986-08-21 标题 :Benzylthioether-linked solid support-bound thiol compounds and method for peptide synthesis 发明人:GLASS JOHN D 权利人:SINAI SCHOOL MEDICINE 摘要:A method for the synthesis of sulfydryl-containing peptides which comprises forming a benzylthioether-linked solid support-bound thiol compound having at least one functional group for generating at least one peptide bond, sequentially coupling at least one protected amino acid or peptide to the compound until a peptide having desired amino acid sequence is obtained, and cleaving the benzylthioether linkage to release the peptide from the support with concomitant regenertion of the sulfydryl group in the peptides. The invention also encompasses compounds having the general formula wherein X is H, NH2, or acyl-NHY, said acyl being an amino acid or a peptide; Y is H, COOH, CONHNH2, the ester COOR1 in which R1 is selected from the group consisting of methyl, ethyl, phenyl, ortho-nitrophenyl and para-nitrophenyl, the amide CONH2, or the amide CONHR2 in which R2 is an amino acid or peptide; and providing that X and Y cannot both be H.
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-9005738-A1 优先权日:1988-11-19 标 题:Trialkysilyl esters of amino acids and their use in the synthesis of peptides 发明人:ATKINSON ANTHONY; CALDER MICHAEL ROGER; SHARMA RAM PRAKASH 权利人:HEALTH LAB SERVICE BOARD; UNIV SOUTHAMPTON 摘要:A novel procedure is described for synthesising peptides in which successive amino acids are attached to an incipient polypetide chain by addition of a carboxy-protected amino acid to the carboxy end of said chain. The procedure involves the use of silyl esters of amino acids, many of which are novel and form a further aspect of the invention.
专利号:US-4212795-A 优先权日:1978-11-13 标题:Cyclization of peptides 发明人:HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K 权利人:ARMOUR PHARMA 摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing two cysteine moieties, each of which is protected by an n-alkylthio group, or when one of such moieties is in an amino terminal position, this one moiety may be protected by a cysteine group while the other is protected by an n-alkylthio group, and placing such intermediate peptide in a solution substantially free of oxygen and preferably at a pH of from 5 to 10 until rearrangement has taken place, to yield a cyclic disulfide peptide. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.
专利号:US-6552166-B1 优先权日:1999-10-19 标 题:Process for the preparation of conjugates useful in the treatment of prostate cancer 发明人:LYNCH JOSEPH E; ROBBINS MICHAEL A; SHI YAO-JUN; LIEBERMAN DAVID R 权利人:MERCK & CO INC 摘要:The present invention is directed to the improved synthesis of compounds of formula I:which may be useful in the treatment of prostate cancer. Such compounds are synthesized in the presence of a carboxyl activating agent, an additive and a base for the preparation of a PSA conjugate which comprises an anthracycline antibiotic and an oligopeptide.
参考文献:10.1055/s-0028-1083179 摘要:Greig N, Luo W, Yu Q, Tweedie D, Deschamps J, Parrish D, Holloway H, Li Y, Brossi A. Syntheses of Aromatic Substituted 6′-Thiothalidomides. Synthesis. 2008 Oct 16;2008(21):3415–22. doi: 10.1055/s-0028-1083179.