6230-11-1Relevant articles and documents
Schiller et al.
, p. 1831,1832 (1977)
C(sp3) -C(sp2) Method for constructing key and β - aryl amino acid preparation method
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Paragraph 0037; 0043-0044; 0046, (2021/10/27)
The invention provides C. (sp3) - C(sp2) A method for constructing a key and β -aryl amino acid relates to the technical field of chemical substance synthesis and transition metal application, which comprises β-C amino acid. (sp3) Ring carbon C in place of phenolic hydroxyl group(sp2) A method of constructing C-C keys by direct coupling. The process will contain inactive β-C. (sp3) Amino acids of - H and ligands L of specific structure1 The tetradentate chelate is generated by complexation with bivalent nickel, and the amino acid labile β-C is completed under the catalysis of palladium with phenolic ester under basic conditions. (sp3) - H Aryl, proton transfer and the like are reacted to achieve C. (sp3) - C(sp2) Construction of a bond, finally hydrolytically releasing β-C aryl amino acid and ligand L1 C. (sp3) - C(sp2) The key construction method is simple and convenient to operate. The method has the advantages of low cost, strong reaction universality, high yield and stereoselectivity. The synthetic method provides a novel method for preparing various non-natural β - aryl amino acids, and provides a novel method for amino acidification/peptide modification of phenolic compounds with biological activity, and provides a novel approach and selection for the design and synthesis of new drugs.
EPHA4 CYCLIC PEPTIDE ANTAGONISTS AND METHODS OF USE THEREOF
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, (2019/11/19)
Disclosed herein are compounds and methods of use thereof for the modulation of EphA4 receptor activity. In an aspect, is provided a method of treating or preventing a disease or disorder mediated by EphA4, comprising administering to a subject in need thereof a therapeutically effective amount of a compound as described herein, including certain embodiments, or the structural Formula (I), (l-A), (II), (III), (IV), (IV-1), (V), (Vl-A), (Vl-B), (VII-1), (VII-2), (VIII-1), or (VIII-2), or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or an isotopic variant thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof.
Tailored Mutants of Phenylalanine Ammonia-Lyase from Petroselinum crispum for the Synthesis of Bulky l- and d-Arylalanines
Filip, Alina,Nagy, Emma Z. A.,Tork, Souad D.,Bánóczi, Gergely,To?a, Monica I.,Irimie, Florin D.,Poppe, László,Paizs, Csaba,Bencze, László C.
, p. 2627 - 2633 (2018/05/03)
Tailored mutants of phenylalanine ammonia-lyase from Petroselinum crispum (PcPAL) were created and tested in ammonia elimination from various sterically demanding, non-natural analogues of phenylalanine and in ammonia addition reactions into the corresponding (E)-arylacrylates. The wild-type PcPAL was inert or exhibited quite poor conversions in both reactions with all members of the substrate panel. Appropriate single mutations of residue F137 and the highly conserved residue I460 resulted in PcPAL variants that were active in ammonia elimination but still had a poor activity in ammonia addition onto bulky substrates. However, combined mutations that involve I460 besides the well-studied F137 led to mutants that exhibited activity in ammonia addition as well. The synergistic multiple mutations resulted in substantial substrate scope extension of PcPAL and opened up new biocatalytic routes for the synthesis of both enantiomers of valuable phenylalanine analogues, such as (4-methoxyphenyl)-, (napthalen-2-yl)-, ([1,1′-biphenyl]-4-yl)-, (4′-fluoro-[1,1′-biphenyl]-4-yl)-, and (5-phenylthiophene-2-yl)alanines.
