96568-07-9
100361-18-0
以7-氯-1-環(huán)丙基-6-氟-4-氧代-1,4-二氫-1,8-萘啶-3-羧酸乙酯(0.1g,0.32mmol)為原料,將其溶解于THF(5ml)中。向該溶液中加入濃HCl(45μL,0.7mmol)。將反應(yīng)混合物加熱至回流狀態(tài),持續(xù)反應(yīng)2小時(shí)。通過薄層色譜(TLC)監(jiān)測(cè)反應(yīng)進(jìn)度,確認(rèn)反應(yīng)完成后,將反應(yīng)混合物冷卻至室溫。過濾收集析出的固體,得到目標(biāo)產(chǎn)物7-氯-1-環(huán)丙基-6-氟-1,4-二氫-4-氧代-1,8-萘啶-3-羧酸,產(chǎn)量為70mg,收率為78%。
參考文獻(xiàn):
[1] Bioorganic and Medicinal Chemistry Letters, 2012, vol. 22, # 7, p. 2428 - 2433
[2] Journal of Medicinal Chemistry, 2002, vol. 45, # 25, p. 5564 - 5575
[3] Patent: WO2005/40164, 2005, A1. Location in patent: Page/Page column 10-12