(R)-5-氯-2-(5-甲基-[1,4]二氮杂环庚烷-1-基)-苯并噁唑盐酸盐合成路线 (共 2 条)
反应条件
1: 2-(2H-1,2,3-triazol-2-yl)-5-methylbenzoic acid With oxalyl dichloride; N,N-dimethyl-formamide in isopropanol acetate T=20 - 25°C; Inert atmosphere; 2: 5-chloro-2-((R)-5-methyl-[1,4]diazepan-1-yl)benzooxazole hydrochloride With triethylamine in isopropanol acetate; acetonitrile T=20 - 40°C; Product distribution / selectivity;
参考文献
MERCK SHARP and DOHME CORP.; MERCK SHARP and DOHME LIMITED; BAXTER, Carl, A.; CLEATOR, Edward; KRSKA, Shane, W.; SHEEN, Faye; STEWART, Gavin; STROTMAN, Neil; WALLACE, Debra, J.; WRIGHT, Timothy
Patent: WO2012/148553 A1, 2012 ;
Location in patent: Page/Page column 52-53 ;
WO 2012/148553 A1
反应条件
potassium carbonate in isopropanol acetate; water T=0°C; 1.25 h; Inert atmosphere;
参考文献
Mangion, Ian K.; Sherry, Benjamin D.; Yin, Jingjun; Fleitz, Fred J.
Organic Letters, 2012 , vol. 14, # 13 p. 3458 - 3461