合成路线:Ursodeoxycholic acid (I) was activated as the mixed anhydride (II) with ethyl chloroformate and triethylamine,and subsequently coupled with the triethylamine salt of taurine (III) to produce the title conjugated bile acid.Optionally,the mixed anhydride (II) was previously converted to the active phenol ester (V) by treatment with p-hydroxypropiophenone (IV),and subsequently condensed with taurine (III).Alternatively,ursodeoxycholic acid (I) was directly coupled to taurine (III) employing as the coupling reagents 2-isobutyl-N-isobutyloxycarbonyl-1,2-dihydroquinoline (IIDQ),diethylphosphorocyanidate (DEPC),or 2-ethoxy-N-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ) under microwave irradiation.
参考文献标题:Process for the preparation of taurine-conjugated bile acids
文献作者:Bonadi,A.; Molinari,E.
参考来源:EP 0582891
合成路线:A further method was based on the microbial hydroxylation of taurolithocholic acid (VIII) by the action of a microorganism belonging to the Mortierella genus.
参考文献标题:Procuding conjugated ursodeoxycholic acids
文献作者:Sawada,H.; Watanuki,M.(Yakult Honsha Co.,Ltd.)
参考来源:EP 0119040
合成路线:In a related method,ursodeoxycholic acid (I) was activated as either the mixed anhydrides (VI) or (VII) with pivaloyl chloride or benzoyl chloride,respectively.Subsequent coupling with taurine (III) produced the title conjugated bile acid.
参考文献标题:Process for the preparation of taurocholic acids
文献作者:Rossetti,V.; Arosio,R.(Sanofi-Synthabo)
参考来源:EP 0629634
合成路线:Ursodeoxycholic acid (I) was activated as the mixed anhydride (II) with ethyl chloroformate and triethylamine,and subsequently coupled with the triethylamine salt of taurine (III) to produce the title conjugated bile acid.Optionally,the mixed anhydride (II) was previously converted to the active phenol ester (V) by treatment with p-hydroxypropiophenone (IV),and subsequently condensed with taurine (III).Alternatively,ursodeoxycholic acid (I) was directly coupled to taurine (III) employing as the coupling reagents 2-isobutyl-N-isobutyloxycarbonyl-1,2-dihydroquinoline (IIDQ),diethylphosphorocyanidate (DEPC),or 2-ethoxy-N-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ) under microwave irradiation.
参考文献标题:An improved synthesis of taurine- and glycine-conjugated bile acids
文献作者:Momose,T.; Tsubaki,T.; Iida,T.; Nambara,T.
参考来源:Lipids 1997,32(7),775
合成路线:Ursodeoxycholic acid (I) was activated as the mixed anhydride (II) with ethyl chloroformate and triethylamine,and subsequently coupled with the triethylamine salt of taurine (III) to produce the title conjugated bile acid.Optionally,the mixed anhydride (II) was previously converted to the active phenol ester (V) by treatment with p-hydroxypropiophenone (IV),and subsequently condensed with taurine (III).Alternatively,ursodeoxycholic acid (I) was directly coupled to taurine (III) employing as the coupling reagents 2-isobutyl-N-isobutyloxycarbonyl-1,2-dihydroquinoline (IIDQ),diethylphosphorocyanidate (DEPC),or 2-ethoxy-N-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ) under microwave irradiation.
参考文献标题:Microwave-induced rapid synthesis of bile acid conjugates
文献作者:Dayal,B.; et al.
参考来源:Synlett 1997,(8),861
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