Convenient routes to 2-aryl-2-fluoropropionic acids: Synthesis of monofluorinated analogues of (+/-)-ibuprofen, (+/-)-naproxen and related compounds
Convenient routes to 2-aryl-2-fluoropropionic acids: Synthesis of monofluorinated analogues of (+/-)-ibuprofen, (+/-)-naproxen and related compounds
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DOI：
10.1016/0040-4020(96)00758-2
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发表时间：
1996-09-23
期刊：
影响因子：
2.1
通讯作者：
Haufe, G
中科院分区：
文献类型：
--
作者：
Goj, O;Kotila, S;Haufe, G
作为非甾体抗炎药（NSAID）氟比洛芬1、布洛芬3和萘普生4的类似物的α-氟化芳基丙酸5的合成是通过相应的伯醇9的氧化来完成的。后者可以通过两种不同的途径获得，通过改变芳族部分显示其普遍适用性。此外，氟取代基对晶格中酸部分的构象的影响通过化合物5c的比较X射线研究示出。版权所有（C）1996 Elsevier Science Ltd
The synthesis of alpha-fluorinated arylpropionic acids 5 as analogues of the nonsteroidal anti-inflammatory agents (NSAIDs) flurbiprofen 1, ibuprofen 3 and naproxen 4 is accomplished by the oxidation of the corresponding primary alcohols 9 The latter are accessible on two different pathways showing their general applicability by variation of the aromatic moiety. Furthermore the influence of the fluorine substituent towards the conformation of the acid moiety in the crystal lattice is shown by comparative X-ray studies of compound 5c. Copyright (C) 1996 Elsevier Science Ltd