Synthesis of methylamino-2-phenyl-2-butyl-3,4,5-trimethoxybenzoate, the main bioactive metabolite of trimebutine maleate.
The first synthesis of the methylamino-2-phenyl-2-butyl-3,4,5-trimethoxybenzoate (desmethyltrimebutine) I is described. This compound is the main bioactive metabolite of trimebutine II (Debridat, CAS 39133-31-8), an antispasmodic widely used for intestinal diseases since 1969. It was used for pharmacokinetic and bioequivalence studies.
Unité de recherche CNRS-UCP-ESCOM, Ecole Supérieure de Chimie Organique et Minérale (ESCOM), Cergy-Pontoise, France.
A
A
Martin
B
B
Figadère
S
S
Saivin
G
G
Houin
J M
JM
Chomard
G
G
Cahiez
D001565:Benzoates / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D001711:Biotransformation; D002855:Chromatography, Thin Layer; D005765:Gastrointestinal Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D009682:Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared; D014287:Trimebutine / Q000493:pharmacokinetics*
D001565:Benzoates; D005765:Gastrointestinal Agents; C412875:methylamino-2-phenyl-2-butyl-3,4,5-trimethoxybenzoate; D014287:Trimebutine