专利号:US-2010022767-A1 优先权日:2008-07-25 标题 :Development of a synthesis of syringolin a and b and derivatives thereof 发明人:KAISER MARKUS; CLERC JEROME 权利人:MAX PLANCK GESELLSCHAFT 摘要:The synthesis of syringolin A and B and derivatives thereof as well as to pharmaceutical compositions containing the syringolin A or B or derivatives thereof and the use of syringolin A and B and derivatives thereof for prophylaxis and treatment of cancer.
专利号:US-5280093-A 优先权日:1989-06-29 标题 :Chiral polymers for the synthesis of pure enantiomers of amino acids 发明人:JACQUIER ROBERT; CALMES MONIQUE; DAUNIS JACQUES 权利人:RHONE POULENC CHIMIE 摘要:The present invention relates to chiral polymers and to their uses for operations of asymmetric synthesis, deracemization and optical inversion. n These polymers are characterized in that they comprise: n a chiral unit n a functionalizing unit n an optional crosslinking unit n Application to chiral organic synthesis.
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
专利号:WO-2024075813-A1 优先权日:2022-10-07 标 题:Polypeptide synthesis using diketopiperazine compound 发明人:YAMAMOTO HISASHI; MITSUDA MASARU; HATTORI TOMOHIRO 权利人:CHUBU UNIV EDUCATIONAL FOUNDATION 摘要:Provided are: a novel diketopiperazine compound for rapid and easy synthesis of various polypeptides; and a method for manufacturing the same. The diketopiperazine compound is represented by general formula (1). (In the formula, R 1 , R 2 , R 3 , R 4 , and R 5 are each independently a hydrogen atom, a substituted or unsubstituted hydrocarbon group, or a substituted or unsubstituted heterocyclic group. R 1 and R 2 , R 1 and R 5 , R 2 and R 5 , and/or R 3 and R 4 are each optionally bonded to form a ring. PGE represents an electron-withdrawing protective group.)
专利号:US-4111933-A 优先权日:1976-04-30 标题:Protection of functional groups during reaction and their subsequent restoration 发明人:ECKERT HEINER; UGI IVAR; KABBE HANS-JOACHIM 权利人:BAYER AG 摘要:In the process for preparing an organic compound of the formula n n A' -- X n n in which n X is an amino group, a hydroxyl group or a carboxyl group, and n A' is the remainder of the molecule, from an organic compound of the formula n n A -- X n n in which n A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula n n A -- Z -- COOR n n in which n Z is --NH--, --O-- or a direct C--C bond, and n R is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CHâ•?CH-- group or an arylene group, n R 1 to R 4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or n R 1 + r 2 and R 3 + R 4 each independently completes a 5- or 6-membered carbocyclic ring, or n R 1 and R 3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, n Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula n n A' -- Z -- COOR n n and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporis.
专利号:US-8044173-B2 优先权日:2005-09-13 标 题 :Asymmetric synthesis of peptides 发明人:HARWOOD LAURENCE M; YAN RAN 权利人:UNIV READING 摘要:A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemisation, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.
参考标题:Allenone-Mediated Racemization/epimerization-Free Peptide Bond Formation And Its Application In Peptide Synthesis 作者:Zhengning Wang,Xuewei Wang,Penghui Wang,Junfeng Zhao |发布日期:2021.7.14 摘要:Peptide Synthesis (Spps). The Robustness Of The Allenone-Mediated Peptide Bond Formation Was Showcased Incisively By The Synthesis Of Carfilzomib, Which Involved A Rare Racemization-/epimerization-Free N To C Peptide Elongation Strategy. Furthermore, The Successful Synthesis Of The Model Difficult Peptide Acp (65-74) On A Solid Support Suggested That This Method Was Compatible With Spps. This Method Combines
合成参考文献
参考文献:10.1055/s-0029-1216931 摘要:Forsyth C, Wang B. Total Synthesis of Largazole - Devolution of a Novel Synthetic Strategy. Synthesis. 2009 Aug 14;2009(17):2873–80. doi: 10.1055/s-0029-1216931. 参考文献:10.1007/978-3-642-28118-1_2 摘要:Reisinger C. Background. 2012. In: Springer Theses. 参考文献:10.1007/978-3-642-28118-1_3 摘要:Reisinger C. Objectives of This Ph.D. Work. 2012. In: Springer Theses.