새로운 6-Substituted Pyridazin-3(2H)-one 유도체 및 토토머형의 합성

• 영문명: Synthesis of its Tautomeric Forms and New 6-Substituted Pyridazin-3(2H)-one Analogs
• 발행기관: 대한약학회
• 저자명: 김채원 박명숙
• 간행물 정보: 『약학회지』제57권 제5호 (2013년), 316~322쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2013.10.31

영문 초록

The new pyridazinone analogs were synthesized for development of candidates to retain anticancer activity. Various 6-substituted pyridazin-3(2H)-ones were prepared from the pyridazinyl chloride 3a~d via endothermic nucleophilic substitution with hydroxide ion as nucleophile for 2~48 h. Pyridazinyl chloride 3a~d could be converted to hydrox- ypyridazines (or pyridazin-3(2H)ones) using 1~5 equivalents of water (or 1 equivalent of sodium hydroxide) at reflux in DMF. The tautomerism of lactim form to lactam form was also accomplished in pyridazine derivatives. Formation of pyridazinones 10 was undertaken with stirring using sodium hydroxide at reflux in DMF for 2 h. Synthetic compounds were identified using NMR spectrum.

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키워드

pyridazinones hydroxypyridazines endothermic nucleophilic substitution tautomeric forms