131180-40-0Relevant articles and documents
Friedel-Crafts α-aminoacylation of aromatic compounds with a chiral N- carboxy-α-amino acid anhydride (NCA); Part 2
Itoh, Osamu,Amano, Akira
, p. 423 - 428 (1999)
The N-carboxy-α-amino acid anhydrides (NCA) derived from L-Asp(OEt), L- Glu(OMe), L-Met, and L-Pro reacted with aromatic compounds (toluene or benzene) in the presence of AlCl3 to afford the corresponding α-aminoalkyl aryl ketones as hydrochloride salts in moderate yields. The β- and γ-amino acid esters, which were obtained from the reaction of the aromatic compounds with L-Asp(OEt)- and L-Glu(OMe)-NCA, were hydrolyzed by hydrochloric acid to the corresponding β- and γ-amino acids as hydrochloride salts. L-Phe-NCA did not react with benzene in the presence of AlCl3, instead an intramolecular acylation occurred to afford (S)-2-aminoin-danone hydrochloride. The chiralities of the original L-α-amino acids were most retained during these α-aminoacylation.
Oxazolidinone compound as well as preparation method, application and pharmaceutical composition thereof
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Paragraph 0093-0095, (2020/11/05)
The invention relates to an oxazolidinone compound used as an Lp-PLA2 covalent inhibitor and a pharmaceutical composition of the oxazolidinone compound, the structure of the oxazolidinone compound isshown as a general formula I, and R1, R2 and R3 are defined as the specification and claims. The compound shown in the general formula I or the stereoisomer or the pharmaceutically acceptable salt thereof can be used as the Lp-PLA2 covalent inhibitor to prevent and/or treat and/or improve diseases related to Lp-PLA2 enzyme activity. Meanwhile, the stereoisomer or the pharmaceutically acceptable salt of the compound shown in the general formula I can be used as an Lp-PLA2 specific molecular probe.
Synthesis of homopolypeptides with PPII structure
Martin, Charlotte,Lebrun, Aurelien,Martinez, Jean,Cavelier, Florine
, p. 3103 - 3109 (2013/07/26)
Polyprolines are attractive polymers because of their folding property into polyproline II (PPII) structure, their significance in protein/protein interactions, and their potential as new therapeutic targets. Silaproline (Sip) is an analogue of proline, which exhibits similar conformational properties. The presence of dimethylsilyl group confers to Sip a higher lipophilicity as well as an improved resistance to biodegradation. Enantiomerically pure Sip was available in gram quantities from resolution of the enantiomers by chiral high performance liquid chromatography. This study describes the first synthesis of Sip N-carboxyanhydride (NCA) and shows preliminary results on comparison of polymerization of (l)Pro-NCA and (d)Sip-NCA to obtain homopolypeptides with PPII structure, polyproline, and polysilaproline polymers.