CAS: 32133-37-2; 3,5-Difluoro-Dl-Phenylalanine

该化合物是苯丙胺的氟化衍生物,其特点是在芳香环上的3和5个位置用氟代替氢原子,这种改变增强了其在药用化学和生化研究中的效用,特别是在开发酶抑制剂和氟化类似物用于结构活动关系研究方面;氟原子的存在提高了代谢稳定性,并改变了电子特性,使其对研究生物相互作用很有价值;其种族学(DL)形式允许广泛应用于合成应用;该化合物通常用于浸泡合成和作为药物的建筑块,为研究人员提供了一种药物发现和机械学研究的多种工具.

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CAS号266360-46-7 diethyl 2-aceta... | CAS号141776-91-2 3,5-二氟苄溴

合成工艺路线路线简述

  • 合成目标产物 Dl-3,5-Difluorophenylalanine 主要起始原料 3,5-Difluorobenzyl Bromide
  • (文献来源)合成步骤主要原料 3,5-Difluorobenzyl Bromide
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

海关参考信息

专利信息


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
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合成参考文献


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.
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