3,5-二氟丁二酸置于petroselinum Crispum Phenylalanine Ammonialyase (1U) Ammonium Hydroxide体系中,化学反应 24.0H,以69%的收率获得产物l-3,5-二氟苯丙氨酸 参考文献:Phenylalanine Ammonia-Lyase: The Use Of Its Broad Substrate Specificity For Mechanistic Investigations And Biocatalysis-synthesis Ofl-Arylalanines 标题:Phenylalanine Ammonia-Lyase: The Use Of Its Broad Substrate Specificity For Mechanistic Investigations And Biocatalysis-synthesis Ofl-Arylalanines 摘要:Several Fluoro-And Chlorophenylalanines Were Found To Be Good Substrates Of Phenylalanine Ammonialyase (Pal/ec 4.3.1.5) From Parsley. The Enantiomerically Pure L-Amino Acids Were Obtained In Goad Yields By Reaction Of The Corresponding Cinnamic Acids With 5M Ammonia Solution (Buffered To Ph 10) In The Presence Of Pal. The Kinetic Constants For Nine Different Fluoro-And Chlorophenylalanines Do Not Provide A Rigorous Proof For But Are Consistent With The Previously Proposed Mechanism Comprising An Electrophilic Attack Of The Methylidene-Imidazolone Cofactor Of Pal At The Aromatic Nucleus As A First Chemical Step. In The Resulting Friedel-Crafts-Type Sigma Complex The Beta-Protons Are Activated For Abstraction And Consequently The Pro-S Is Abstracted By An Enzymic Base. Results From Semiempirical Calculations Combined With A Proposed Partial Active Site Model Showed A Correlation Between The Experimental Kinetic Constants And The Change In Polarization Of The Pro-S Cd-H Bond And Heat Of Formation Of The Ir Complexes,Thus Making The Electrophilic Attack At The Neutral Aromatic Ring Plausible. Furthermore,While 5-Pyrimidinylalanine Was Found To Be A Moderately Good Substrate Of Pal,2-Pyrimidinylalanine Was An Inhibitor. DOI:10.1002/1521-3765(20000915)6:18<3386::Aid-Chem3386>3.0.Co;2-5
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]: Fujita T, Et Al. Synthesis Of A Complete Set Of L-Difluorophenylalanines, L-(F2)Phe, As Molecular Explorers For The Ch/π Interaction Between Peptide Ligand And Receptor. Tetrahedron Letters. 2000, 41(6):923-927.
合成参考文献
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