摘要 |
本发明提供制备((1R,3S)–3–异丙基–3–{〔3–(三氟甲基)–7,8–二氢–1,6–二氮杂–6(5H)–基〕羰基}环戊基)〔(3S,4S)–3–甲氧基四氢–2H–喃–4–基〕胺及其丁二酸盐之有效率的合成方法。此外,本发明还提供制备中间体(3R)–3–甲氧基四氢–4H–喃–4–酮;(1S,4S)–4–(2,5–二甲基–1H–咯–1–基)–异丙基环戊–2–烯–1–羧酸;及3–(三氟甲基)–5,6,7,8–四氢–1,6–二氮杂之有效率的合成方法;及前体(3S,4S)–N–((1S,4S)–4–异丙基–4–{〔3–(三氟甲基)–7,8–二氢–1,6–二氮杂–6(5H)–基〕羰基}环戊–2–烯–1–基)–3–甲氧基四氢–2H–喃–4–胺之制备方法。此外,本发明系在于((1R,3S)–3–异丙基–3–{〔3–(三氟甲基)–7,8–二氢–1,6–二氮杂–6(5H)–基〕羰基}环戊基)〔(3S,4S)–3–甲氧基四氢–2H–喃–4–基〕胺之丁二酸盐之超级性质。093132410-p01.bmp |