149437-76-3

基本信息
對氟苯甲酰丁酸
對氟苯甲酰基丁酸
依替米貝中間體 2
4-(4-氟苯甲?;?丁酸,98%
4-(4-FLUOROBENZOYL)BUTYRIC ACID
4-(4-FLUOROPHENYL)BUTYRIC ACID
4-FLUORO BENZOYL BUTYRIC ACID
4-FLUORO-GAMMA-OXO-BENZENEPENTANOIC ACID
4-FLUOROPHENYL-5-OXOPENTANOIC ACID
5-(4'-FLUOROPHENYL)-5-OXOPENTANOIC ACID
5-(4-FLUOROPHENYL)-5-OXO-PENTANOIC ACID
5-(4-FLUOROPHENYL)-5-OXOVALERIC ACID
5-(P-FLUOROPHENYL)-5-OXO-PENTANOIC ACID
CHEMBRDG-BB 4002813
TIMTEC-BB SBB000492
TIMTEC-BB SBB010216
4-(4-Flurobenzoyl-)butyric Acid (FBBA)
4-(p-Fluorobenzoyl)-butyric acid
5-(4-FLUOROPHENYL)-5-OXOPENTANOIC ACID 4-(4-FLUOROPHENYL) BUTYRIC ACID
4-(Fluorobenzoyl)ButyricAcid,IntermediateOfEzetimibe
4-(Fluorobenzoyl) Butyric Acid Intermediate Of Ezetimibe (Apis)
4-Fluorophenyl-5oxobutyric Acid
4-(4-Fluorobenzoyl)butyric
物理化學性質(zhì)
安全數(shù)據(jù)
制備方法

108-55-4

462-06-6

149437-76-3
4-(4-氟苯甲酰基)丁酸的合成步驟如下:在2L三頸圓底燒瓶中加入250g無水AlCl3(1.87摩爾)和300mL氟苯(307.5g; 3.2摩爾),將混合物在冰浴中冷卻至5℃。通過加料漏斗在45分鐘內(nèi)緩慢加入100g戊二酸酐(0.86mol)溶于400mL氟苯(4.3摩爾)的渾濁懸浮液,保持反應(yīng)溫度低于12℃。反應(yīng)混合物逐漸升溫至室溫并攪拌90分鐘,通過NMR監(jiān)測反應(yīng)完成。將反應(yīng)混合物冷卻至0至5℃,小心加入700mL 1N HCl的冷水溶液以淬滅未反應(yīng)的AlCl3,初期保持溫度低于20℃,后期不超過40℃。將混合物倒入2L 1:1的水和冰混合物(v/w)中沉淀粗產(chǎn)物,過濾白色懸浮液并用水充分洗滌。將白色固體溶于3L 5% NaHCO3飽和水溶液中,蒸汽浴加熱1小時后趁熱通過硅藻土墊過濾。濾液冷卻至室溫,逐滴加入約320mL濃HCl調(diào)節(jié)至pH 1,產(chǎn)物結(jié)晶析出,冰浴中攪拌30分鐘。過濾,冰冷水洗滌濕濾餅,50℃真空干燥16小時,得到143.2g 4-(4-氟苯甲?;?丁酸,熔點141至142℃,產(chǎn)率79.3%。
參考文獻:
[1] Patent: WO2004/99132, 2004, A2. Location in patent: Page 7-8
[2] Bioorganic and Medicinal Chemistry Letters, 2010, vol. 20, # 15, p. 4424 - 4426
[3] Patent: CN106397292, 2017, A. Location in patent: Paragraph 0053; 0083; 0084
[4] Patent: US2006/135755, 2006, A1. Location in patent: Page/Page column 15
[5] Patent: EP1137634, 2005, B1. Location in patent: Page/Page column 9
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2025/05/22 | F0476 | 4-(4-氟苯甲酰基)丁酸 4-(4-Fluorobenzoyl)butyric Acid | 149437-76-3 | 1G | 40元 |
2025/05/22 | F0476 | 4-(4-氟苯甲?;?丁酸 4-(4-Fluorobenzoyl)butyric Acid | 149437-76-3 | 5g | 45元 |
2025/05/22 | XW1494377631 | 4-(4-氟苯甲酰基)丁酸 4-(4-fluorobenzoyl)butyric acid;p-fluorobenzoylbutanoic acid;5-(4-fluorophenyl)-5-oxopentanoic acid | 149437-76-3 | 5G | 13元 |