cas 2183-56-4, hydromorphinol | Articles data

Articles about 2183-56-4Total 6 be found

PROCESS FOR MAKING MORPHINAN-6alpha-OLS
The present invention provides a process whereby morphinan-6-ones can be converted stereospecifically to the corresponding morphinan-6α-ols by catalytic hydrogenation under basic conditions.
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(2010/03/02)

IMPROVED PROCESS FOR THE PREPARATION OF 6-ALPHA-HYDROXY-N-ALKYLATED OPIATES
The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.
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(2009/01/20)

Probes for narcotic receptor mediated phenomena. 24. synthesis, single crystal X-ray analyses, in vitro and in vivo properties of 6α-and 6β-IODO-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinans
The 6α- and 6β-iodo-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinans, potential SPECT ligands, were synthesized and found to be μ-selective opioids, more potent in vitro and in vivo than their 6-hydroxy relatives. Single-crystal analysis showed that the 6α- and 6β-iodine atoms are spatially closely located although the C-ring conformations of these compounds are quite different (twist-boat form vs. chair). These epimeric conformational differences were not reflected in their binding affinities.
Kayakiri, Hiroshi,Jacobson, Arthur E.,Rice, Kenner C.,Rothman, Richard B.,Xu, Heng,Flippen-Anderson, Judith L.,George, Clifford,Aceto, Mario D.,Bowman, Edward R.,Harris, Louis S.,May, Everette L.,Partilla, John S.,Becketts, Karen
p. 427 - 438
(2007/10/03)

Morphine Alkaloids, Part 114 A. Stereohomogeneous Synthesis of N-Demethyl-N-Substituted-14-Hydroxydihydromorphines
A new route for the stereohomogeneous synthesis of N-demethyl-N-substituted-14-hydroxydihydromorphines 2a-f has been elaborated, involving O-demethylation of the novel dihydrocodeine derivatives 6a-f, obtained upon alkylation of the hitherto unknown N-demethyl-14-hydroxydihydrocodeine (5). Keywords. 6α,14β-Diacetoxy-4,5α-epoxy-3-methoxy-17-methyl-morphinan, N-demethylation of; 3,6α,14β-Triacetoxy-17-alkyl-4,5α-epoxymorphinan, N-demethylation of; 17-Alkyl-4,5α-epoxy-6α,14β-dihydroxy-3-methoxymorphinan, O-demethylation of; 4,5α-Epoxy-6α,14β-dihydroxy-3-methoxymorphinan, N-alkylation of.
Hosztafi, Sandor,Berenyi, Sandor,Toth, Geza,Makleit, Sandor
p. 435 - 442
(2007/10/02)

Synthesis and utilization of 17-methyl and 17-cyclopropylmethyl-3,14-dihydroxy-4,5α-epoxy 6β-fluoromorphinans (foxy and cyclofoxy) as (18F)-labeled opioid ligands for position emission transaxial tomography (PETT)
Fluorinated derivatives 3,14-dihydroxy-4,5α-epoxy-6β-fluoro-17-methylmorphinan (""fluorooxymorphone""; FOXY, compound 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5α-epoxy-6β-fluoromorphinan (CYCLOFOXY, compound 18) are prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11, respectively. Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6α-triflate functions in 8 and 16. The synthetic procedures were suitable for the production of the corresponding positron emitting 18 F-labeled analogs 18 F-FOXY and 18 F-CYCLOFOXY, which are useful for in vivo studies of the opioid receptor system using positron emission transaxial tomography. In addition, the tritiation of FOXY (10) to high specific activity is noted.
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(2008/06/13)

Probes for narcotic receptor mediated phenomena. 11. Synthesis of 17-methyl and 17-cyclopropylmethyl-3,14-dihydroxy-4,5α-epoxy-6β-fluoromorphinans (foxy and cyclofoxy) as model of opioid ligands suitable for positron emission transaxial tomography
Fluorinated derivatives 3,14-dihydroxy-4,5α-epoxy-6β-fluoro-17-methylmorphinan ("fluorooxymorphone": FOXY, 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5α-epoxy-6β-fluoromorphnian (CYCLOFOXY, 18) were prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11 respectively.Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6α-triflate functions in 8 and 16.The synthetic procedures are suitable for the production of the corresponding positron emitting 18F-labeled analogs 18F-FOXY and 18F-CYCLOFOXY, which may be usefuf for in vivo studies of the opioid receptor system using positron emission transaxial tomography.In addition, the tritiation of FOXY (10) to high specific activity is described
Burke, Terrence R.,Rice, Kenner C.,Pert, Candace B.
p. 99 - 106
(2007/10/02)