- Method for preparing levallorphan tartrate
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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.
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- Anticonvulsant effects of new morphinan derivatives
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We synthesized a series of compounds that are modified in positions 3 and 17 of the morphinan ring system, with the intention of developing ideal anticonvulsant agents. We examined the effects of these compounds on kainic acid (KA)-induced seizures, and on locomotor patterns in rats. We found that compounds 5, 6, and 8 exhibit novel anticonvulsant effects, with negligible psychotropic effects.
- Kim, Hyoung-Chun,Nabeshima, Toshitaka,Jhoo, Wang-Kee,Ko, Kwang Ho,Kim, Won-Ki,Shin, Eun-Joo,Cho, Minkyoung,Lee, Phil Ho
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p. 1651 - 1654
(2007/10/03)
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- 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
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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.
- Neumeyer, John L,Gu, Xiao-Hui,Van Vliet,DeNunzio, Nicholas J,Rusovici, Daniela E,Cohen, Dana J,Negus,Mello, Nancy K,Bidlack, Jean M
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p. 2735 - 2740
(2007/10/03)
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