Quinupristin mesilate, RP-57669

奎奴普丁Chemical Name: N-(3-Hydroxy-2-pyridylcarbonyl)-(S)-threonyl-(R)-(alpha-aminobutyryl)-(S)-prolyl-[N-methyl-4-(dimethylamino)-(S)-phenylalanyl]-[4-oxo-5(R)-[quinuclidin-3(S)-ylthiomethyl]-(S)-homoprolyl]-(S)-phenylglycine C-1.6-O-3.1-lactone methanesulfonate; 5(R)delta-[3(S)-Quinuclidinylthiomethyl]pristinamycin IA methanesulfonate; (15aS,24aS)-18(R)-[1-Azabicyclo[2.2.2]oct-3(S)-ylthiomethyl]-22(S)-[4-(dimethylamino)benzyl]-6(R)-ethyl-9(S)-(3-hydroxypyridin-2-ylcarboxamido)-10(R),23-dimethyl-13(S)-phenyldocosahydro-12H-pyrido[2,1-f]pyrrolo[2,1-b][1,4,7,10,13,16]oxapentaazacyclononadecine-5,8,12,15,17,21,24-heptaone methanesulfonate; N-[(6R,9S,10R,13S,15aS,18R,22S,24aS)-22-[p-(dimethylamino)benzyl]-6-ethyldocosahydro-10,23-dimethyl-5,8,12,15,17,21,24-heptaoxo-13-phenyl-18-[[(3S)-3-quinuclidinylthio]methyl]-12H-pyrido[2,1-f]pyrrolo[2,1-l][1,4,7,10,13,16]oxapentaazacyclononadecin-9-yl]-3-hydroxypicolinamide
CAS No. 120138-50-3 (free base)
项目整合开发状态: Launched-1999
项目研究机构: Aventis Pharma (Originator)
合成路线:The condensation of the cyclopeptide analogue (I) with morpholine (II) and formaldehyde by means of MsOH in hot methanol gives the 4-morpholinylmethyl derivative (III),which by a treatment with NaOAc in hot acetic acid yields the methylene derivative (IV).Finally this compound is condensed with quinuclidine-3(S)-thiol in hot acetone.