【药物名称】S-16961-1, S-16961
化学结构式(Chemical Structure):
参考文献No.22394
标题:Diacylglycerol nicotinates
作者:Cordi, A.; Lacoste, J.-M.; Duhault, J.; Espinal, J.; Boulanger, M. (ADIR et Cie.)
来源:EP 0574312; JP 1994056786; US 5385920
合成路线图解说明:

The compound S 16961-1 was synthesized in three steps from solketal (I) by acylation with nicotinoyl chloride (II), deprotection of the isopropylidene ketal (III) by heating in dilute aqueous acetic acid and acylation of this key intermediate (IV) with a slight excess of palmitoyl chloride (V) in the presence of triethylamine and 4-dimethylaminopyridine (DMAP) as catalyst. The enantiomers of S 16961-1 were obtained independently in one step from the commercially available (d)- and (l)-1,2-dipalmitoyl glycerols by acylation with nicotinoyl chloride in the presence of triethylamine. The enantiomers were found equiactive and therefore were not pursued individually.

参考文献No.354019
标题:S 16961-1
作者:Cordi, A.A.; Duhault, J.; Laudignon, N.; Castagne, I.
来源:Drugs Fut 1996,21(5),490
合成路线图解说明:

The compound S 16961-1 was synthesized in three steps from solketal (I) by acylation with nicotinoyl chloride (II), deprotection of the isopropylidene ketal (III) by heating in dilute aqueous acetic acid and acylation of this key intermediate (IV) with a slight excess of palmitoyl chloride (V) in the presence of triethylamine and 4-dimethylaminopyridine (DMAP) as catalyst. The enantiomers of S 16961-1 were obtained independently in one step from the commercially available (d)- and (l)-1,2-dipalmitoyl glycerols by acylation with nicotinoyl chloride in the presence of triethylamine. The enantiomers were found equiactive and therefore were not pursued individually.

参考文献No.608353
标题:Regression of coronary artery disease as a result of intensive lipid lowering therapy in men with high level of apolipoprotein B
作者:Brown, G.; Albers, J.J.; Fisher, L.D.; Schaeffer, S.; Lin, J.; Kaplan, C.; Zhao, X.; Bisson, B.; Fitzpatrick, V.; Dodge, H.
来源:New Engl J Med 1990,323(19),1289-98
合成路线图解说明:

The compound S 16961-1 was synthesized in three steps from solketal (I) by acylation with nicotinoyl chloride (II), deprotection of the isopropylidene ketal (III) by heating in dilute aqueous acetic acid and acylation of this key intermediate (IV) with a slight excess of palmitoyl chloride (V) in the presence of triethylamine and 4-dimethylaminopyridine (DMAP) as catalyst. The enantiomers of S 16961-1 were obtained independently in one step from the commercially available (d)- and (l)-1,2-dipalmitoyl glycerols by acylation with nicotinoyl chloride in the presence of triethylamine. The enantiomers were found equiactive and therefore were not pursued individually.

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