152-02-3Relevant articles and documents
Method for preparing levallorphan tartrate
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, (2017/08/29)
The invention provides a method for preparing levallorphan tartrate and belongs to the technical field of drug and chemical synthesis. The method takes methoxyphenylacetic acid and 2-(cyclohexenyl)ethylamine as initial raw materials, and comprises nine reaction steps such as acylation condensation, Bischler-Napieralski ring formation reaction, imine reduction, ether bond hydrolysis, resolution, N-alkylation, Grewe cyclization reaction, and salifying. According to the method, the levallorphan tartrate and each intermediate can be obtained at high yield and high purity, and the method can serve as an industrial method for performing large-scale production.
Mixed κ agonists and μ agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: Synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan
Neumeyer, John L,Gu, Xiao-Hui,Van Vliet,DeNunzio, Nicholas J,Rusovici, Daniela E,Cohen, Dana J,Negus,Mello, Nancy K,Bidlack, Jean M
, p. 2735 - 2740 (2007/10/03)
A series of new N-substituted derivatives of morphinan was synthesized and their binding affinity for the three opioid receptors (μ, δ, and κ) was determined. A paradoxical effect of N-propargyl (MCL-117) and N-(3-iodoprop-(2E)-enyl) (MCL-118) substituents on the binding affinities for the μ and κ opioid receptors was observed. All of these novel derivatives showed a preference for the μ and κ versus δ binding.
