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Volumn 13, Issue 20, 2005, Pages 5717-5732

Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9- tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists

Author keywords

Effective bladder capacity; KRP 103; NK1 antagonist; Pyrimido 4,5 b 1,5 oxazocine

Indexed keywords

4,6 DICHLORO 2 (METHYLTHIO)PYRIMIDINE 5 CARBOXYLIC ACID; 6 [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 2 METHYLTHIO 4 PHENYL 6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 B][1,5]OXAZOCIN 5 ONE; 6 [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 4 (2 METHYLPHENYL) 2 METHYLTHIO 6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 B][1,5]OXAZOCIN 5 ONE; 6 [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 4 CHLORO 2 METHYLTHIO 5,6,7,8 TETRAHYDROPYRIMIDO[5,4 F][1,4]OXAZEPIN 5 ONE; 6 [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 4 CHLORO 2 METHYLTHIO 5,6,7,8,9,10 HEXAHYDROPYRIMIDO[4,5 B][1,5]OXAZOCIN 5 ONE; 6 [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 4 CHLORO 2 METHYLTHIO 6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 B][1,5]OXAZOCIN 5 ONE; 6 [3,5 BIS(TRIFLUOROMETHYL)BENZYL] 4 CHLORO 2 METHYLTHIO 6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 E][1,4]DIAZEPIN 5 ONE; NEUROKININ 1 RECEPTOR ANTAGONIST; OXAZOCINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 24344474075     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2005.06.015     Document Type: Article
Times cited : (36)

References (36)
  • 35
    • 33645610033 scopus 로고    scopus 로고
    • note
    • The study was carried out by Daiichi Pure Chemicals Co., Ltd.
  • 36
    • 33645611722 scopus 로고    scopus 로고
    • note
    • 1H NMR spectrum of 3g showed an AB pattern for the benzylic and oxazocine ring methylene protons at room temperature. Each pair of methylene protons deteriorated to a very broad peak at 100°C and collapsed to one peak but with distinct fission patterns at 150°C. These results indicate that attempts to isolate the atropisomers about the oxazocine ring would give only racemic products due to rapid interconversion.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.