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• 영문명: Synthesis of Fluorinated New Thebaine Derivatives
• 발행기관: 대한약학회
• 저자명: 김근재(Keun Jae Kim) 김수만(Su Man Kim)
• 간행물 정보: 『약학회지』제42권 제3호 (1998년), 257~264쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.06.30

영문 초록

5-Methylthebaine was obtained by treating thebaine with n-butyllithium and methylfluorosulfonate. Hetero Diels-Alder reaction of thebaine and 5-methylthebaine with trifluoroacetaldehyde afforded 14-beta-(triflu-oro-2-hydroxyethyl)codeine (2) and 14-beta-(trifluoro-2-hydroxyethyl)-5-methylcodeinone (9). 6-alpha-OH compound (4) was obtained by employing CeCl2 and NaBH4. After synthesized a derivative substituted for 3-OH (5), using boron tribromied, We synthesized a new derivative that make double bond in C-7, C-8 into epoxode (6), (10). Through inspecting an influence on structure-activity and analgetic action, we are going to examine which opiold acceptor has a selectivity.

키워드

14-β-(trifluoro-2-hydroxyethyl)-codeinone 14-β-(trifluoro-2-hydroxyethyl)-5-methylcodeinone structure-activity analgetic action.