DC Field | Value | Language |
---|---|---|
dc.contributor.advisor | Lee, Hee-Yoon | - |
dc.contributor.advisor | Kim, Yong-Hae | - |
dc.contributor.advisor | 이희윤 | - |
dc.contributor.advisor | 김용해 | - |
dc.contributor.author | Park, Hee-Sock | - |
dc.contributor.author | 박희석 | - |
dc.date.accessioned | 2011-12-13T04:30:36Z | - |
dc.date.available | 2011-12-13T04:30:36Z | - |
dc.date.issued | 2006 | - |
dc.identifier.uri | http://library.kaist.ac.kr/search/detail/view.do?bibCtrlNo=254193&flag=dissertation | - |
dc.identifier.uri | http://hdl.handle.net/10203/31664 | - |
dc.description | 학위논문(박사) - 한국과학기술원 : 화학과, 2006.2, [ v, 131 p. ] | - |
dc.description.abstract | A variety of buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and $[^{35}S]GTP\gammaS$ binding assay in human brain tissue, the new compound 16 has been identified as a selective κ partial agonist which gives antinociceptive effects, but is not self-administered. It is reported that the activation of κ receptors leads to the suppression of unpleasant μ- and δ-mediated side effects such as the rewarding effect. The fact that this compound has a profile (κ partial agonist) may lead to lower degrees of dysphoria than full κ agonists. The compound may be valuable for the development of long-lasting analgesic, as a requirement for protracted use in neuropathic pain and drug abuse medication. In addition, a new method for the efficient radical deoxygenation of alcohols is described for preparing bulk chemicals avoiding scale-up problems. Treatment of various thiocarbonyl derivatives with $(Bu_4N)_2S_2O_8$ and $HCO_2Na$ in DMF afforded the corresponding deoxygenated products in excellent yields. The deoxygenation appears to be initiated by the transfer of a single electron to thiocarbonyl derivatives from $CO_2^{\bullet -}$ rather than from $SO_4^{\bullet -}$. This type of reduction is especially important in many areas of natural product chemistry such as sugars, glycosides, and nucleosides since a selective deoxygenation of the hindered hydroxy-groups is often required in order to enhance their biological activities. Of particular note, in the case of 27c (phenyl thionocarbonate) the $(Bu_4N)_2S_2O_8/DCO_2Na$ deoxygenation system in DMSO can provide the deuterated furanose derivatives at C3 position. | eng |
dc.language | eng | - |
dc.publisher | 한국과학기술원 | - |
dc.subject | tetrabutylammonium peroxydisulfate | - |
dc.subject | formate ion | - |
dc.subject | 오피오이드 | - |
dc.subject | 진통제 | - |
dc.subject | 탈산소화 | - |
dc.subject | 테트라부틸암모늄 퍼옥시다이설페이트 | - |
dc.subject | 포름산염 | - |
dc.subject | Opioid | - |
dc.subject | analgesic | - |
dc.subject | deoxygenation | - |
dc.subject | tetrabutylammonium peroxydisulfate | - |
dc.subject | formate ion | - |
dc.subject | 오피오이드 | - |
dc.subject | 진통제 | - |
dc.subject | 탈산소화 | - |
dc.subject | 테트라부틸암모늄 퍼옥시다이설페이트 | - |
dc.subject | 포름산염 | - |
dc.subject | Opioid | - |
dc.subject | analgesic | - |
dc.subject | deoxygenation | - |
dc.title | Synthesis and biological activity of opioid analgesics | - |
dc.title.alternative | 오피오이드 진통제의 합성 및 생체활성 ; | - |
dc.type | Thesis(Ph.D) | - |
dc.identifier.CNRN | 254193/325007 | - |
dc.description.department | 한국과학기술원 : 화학과, | - |
dc.identifier.uid | 020015129 | - |
dc.contributor.localauthor | Lee, Hee-Yoon | - |
dc.contributor.localauthor | Kim, Yong-Hae | - |
dc.contributor.localauthor | 이희윤 | - |
dc.contributor.localauthor | 김용해 | - |
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