Lifibrol, U-83860, K-12.148
利非贝罗Chemical Name: (?-4-(4'-tert-Butylphenyl)-1-(4'-carboxyphenoxy)-2-butanol; (?-4-[4-(4-tert-Butylphenyl)-2-hydroxybutoxy]benzoic acid
CAS No. 96609-16-4
项目整合开发状态: Phase II
项目研究机构: Fujisawa Deutschland (Originator), Merckle (Licensee)
合成路线:The reaction of 4-tert-butylbenzyl chloride (I) with Mg in ether gives the corresponding Grignard reagent (II),which is condensed with epichlorohydrin (III) yielding 4-(4-tert-butylphenyl)-1,2-epoxybutane (IV).The condensation of (IV) with methyl 4-hydroxybenzoate (V) by means of KOH in refluxing methanol affords 4-[4-(4-tert-butylphenyl)-2-hydroxybutoxy]benzoic acid methyl ester (VI),which is finally saponified with KOH in refluxing ethanol/water.
📌 参考资料/链接：
参考文献标题:p-Oxybenzoic acid derivs.,as well as process for their preparation and their use as medicines
文献作者:Grill,H.; Reiter,F.; Ler,R.; Schliack,M.; Seibel,K.(Klinge Pharma GmbH)
参考来源:DE 3326164; EP 0133935; US 4582857
📄 详细内容
合成路线:The reaction of 4-tert-butylbenzyl chloride (I) with Mg in ether gives the corresponding Grignard reagent (II),which is condensed with epichlorohydrin (III) yielding 4-(4-tert-butylphenyl)-1,2-epoxybutane (IV).The condensation of (IV) with methyl 4-hydroxybenzoate (V) by means of KOH in refluxing methanol affords 4-[4-(4-tert-butylphenyl)-2-hydroxybutoxy]benzoic acid methyl ester (VI),which is finally saponified with KOH in refluxing ethanol/water.
参考文献标题:Lifibrol
文献作者:Rabasseda,X.; Castar,J.; Mealy,N.
参考来源:Drugs Fut 1995,20(4),325
产品链接: CAS No. 96609-16-4››