Sufentanyl (N-4-methoxymethyl-1- 2- (thienyl) ethyl -4-piperidinyl-N-phenyl propanamide) having an anesthetic analgesic action and its N-arylalkyl-4- How to prepare piperidone intermediates

摘要

The present invention is prepared by reacting a primary amine salt of formula (III), an aldehyde of formula (IV) and allylsilane of formula (V) in water or in a mixed solvent of water and an organic solvent. To obtain the compound of (VI) and to prepare the 1-arylalkyl-4-piperidone of the general formula (II) which is useful as an intermediate for the production of 4-anilido piperidine-based anesthetic analgesics by oxidation reaction. It is about a method.;The present invention also relates to a novel process for preparing sufentanil using 1-arylalkyl-4-piperidone derivatives.