【药物名称】PD-117302
化学结构式(Chemical Structure):
参考文献No.108370
标题:Synthesis of carbon-14 labeled PD 117,302 and PD 126,212, potential new analgesic agents
作者:Huang, C.C.; Hicks, J.L.; Butler, D.E.; Hays, S.J.
来源:J Label Compd Radiopharm 1990,28(1),15
合成路线图解说明:

A new synthesis of [14C]-PD-117302 has been described: The Reformatsky condensation of 4,5,6,7-tetrahydrobenzo[b]thiophen-4-one (II) with methyl [1-14C]-bromoacetate (I) by means of Zn in reflux toluene gives a mixture of methyl [1-14C]-2-(4,5,6,7-tetrahydrobenzothiophen-4-ylidene)acete (III) and methyl [1-14C]-2-(6,7-dihdyrobenzothiophen-4-yl)acetate (IV) which, without separation, are treated with Pd/C and S in refluxing N-methylpyrrolidone to afford methyl [1-14C]-2-(benzothiophen-4-yl)acetate (V). The hydrolysis of (V) with methanolic KOH yields the corresponding acid (VI), which is treated with refluxing SOCl2 to give the acyl chloride (VII). Finally, this compound is condensed with trans-1-[2-(methylamino)cyclohexyl]pyrrolidine (VIII) in dichloromethane ethyl ether.

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