专利号:US-11673912-B2 优先权日:2018-02-16 标 题 :Continuous, solvent-free and non-enzymatic peptide synthesis by reactive extrusion 发明人:YEBOUE YVES; GALLARD BENJAMIN; LE MOIGNE NICOLAS; LAMATY FRÉDÉRIC; MARTINEZ JEAN; METRO THOMAS-XAVIER 权利人:CENTRE NAT RECH SCIENT; UNIV MONTPELLIER; ENSCM; ECOLE DES MINES DALES; ASSOCIATION POUR LA RECH ET LE DEVELOPPEMENT DES METHODES ET PROCESSUS INDUSTRIELS 摘要:A continuous, solvent-free and non-enzymatic method for synthesizing a compound of formula (I): Ra-POLYPEP-Rc (I) wherein: POLYPEP is a poly-amino acid compound, Ra and Rc are as specified, the method including the steps of: a) feeding an extrusion reactor with (1) a compound of formula (II) Ra-PEPNt-Rg (II) wherein; PEPNt is a mono- or a poly-amino acid compound, Ra and Rg are as specified, and (2) a compound of formula (III) H-PEPCt-Rc (III) wherein: PEPCt is a mono- or a poly-amino acid compound, and Rc is as defined in the absence of any solvent, so that the compound of formula (II) and the compound of formula (III) react together for generating a compound of formula (I), and b) collecting the compound of formula (I) from the extrusion reactor.
参考标题:A Facile Synthesis And Crystallographic Analysis Of N-Protected β-Amino Alcohols And Short Peptaibols 作者:Sandip V. Jadhav,Anupam Bandyopadhyay,Sushil N. Benke,Sachitanand M. Mali,Hosahudya N. Gopi 摘要:For The Synthesis Of N-Protected β-Amino Alcohols And Peptaibols Using N-Hydroxysuccinimide Active Esters Is Described. Using This Method, Dipeptide, Tripeptide And Pentapeptide Alcohols Were Isolated In High Yields. The Conformations In Crystals Of β-Amino Alcohol, Dipeptide And Tripeptide Alcohols Were Analysed, With A Well-Defined Type Iii β-Turn Being Observed In The Tripeptide Alcohol Crystals
合成参考文献
参考文献:10.1021/jm00027a027 摘要:Ye QZ, Johnson LL, Nordan I, Hupe D, Hupe L. A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors. J Med Chem. 1994 Jan 07;37(1):206–9. doi: 10.1021/jm00027a027.