3,5-二氟溴苄置于氢溴酸,Sodium Ethanolate体系中,用 乙醇 用作溶剂,化学反应 16.17H,反应生成3,5-二氟苯丙氨酸 参考文献:Optimization And Mechanistic Studies Of Psammaplin A Type Antibacterial Agents Active Against Methicillin-Resistantstaphylococcus Aureus (Mrsa) 标题:Optimization And Mechanistic Studies Of Psammaplin A Type Antibacterial Agents Active Against Methicillin-Resistantstaphylococcus Aureus (Mrsa) 摘要:As Described In The Preceding Article,Utilizing A Novel Combinatorial Disulfide Exchange Strategy,A Library Of Psammaplin A (1) Analogues Was Constructed And Screened For Antibacterial Activity Leading To The Identification Of A Collection Of Diverse Lead Compounds. These Combinatorial Leads Were Subsequently Refined,Through Parallel Synthesis,To Afford A Series Of Highly Potent Antibacterial Agents (E.G. 17. 57,58,69,And 70). Some Possessing Greater Than 50-Fold Higher Activities Than The Natural Product. Evaluation Of The Selectivity And Serum Binding Properties Of Some Of The Most Promising Compounds And Preliminary Studies Directed At Deciphering The Mechanism Of Action Of This Novel Class Of Antibacterial Agents Are Also Included. Doi:10.1002/1521-3765(20011001)7:19<4296::Aid-Chem4296>3.0.Co;2-2
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
专利号:US-8546533-B2 优先权日:2008-08-29 标 题:Pipecolic linker and its use for chemistry on solid support 发明人:MARTINEZ JEAN; ZAJDEL PAWEL; PAWLOWSKI MACIEJ; SUBRA GILLES 权利人:MARTINEZ JEAN; ZAJDEL PAWEL; PAWLOWSKI MACIEJ; SUBRA GILLES; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER 1; UNIV JAGELLONE; UNIV MONTPELLIER II 摘要:The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
专利号:US-7763734-B2 优先权日:2006-04-19 标题 :Synthesis, structure and use of bisoxazolidines for asymmetric catalysis and synthesis 发明人:WOLF CHRISTIAN; LIU SHUANGLONG 权利人:UNIV GEORGETOWN 摘要:One aspect of the invention relates to chiral bisoxazolidines and their use in asymmetric catalysis. The chiral bisoxazolidines are a novel class of compounds that is expected to find multiple applications, for example, in asymmetric synthesis. For example, a bisoxazolidine ligand enabled the catalytic enantioselective alkynylation and alkylation of a range of aromatic and aliphatic aldehydes, generating chiral propargylic alcohols and secondary alcohols in high yields and enantiomeric excess.
专利号:WO-2011000848-A1 优先权日:2009-06-29 标题 :Solid phase peptide synthesis of peptide alcohols
专利号:US-11759496-B2 优先权日:2016-05-10 标题:Compounds and pharmaceutical use thereof in the treatment of cancer 发明人:SUSIN SANTOS A; KAROYAN PHILIPPE; MERLE-BERAL HÉLÈNE 权利人:KAROYAN PHILIPPE 摘要:The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.
专利号:US-2012108748-A1 优先权日:2009-06-29 标 题:Solid phase peptide synthesis of peptide alcohols
参考文献:10.1038/nchembio.622 摘要:Pless SA, Galpin JD, Niciforovic AP, Ahern CA. Contributions of counter-charge in a potassium channel voltage-sensor domain. Nature Chemical Biology. 2011 Jul 24;7(9):617–23. doi: 10.1038/nchembio.622.