【药物名称】RTI-4229-336, RTI-336
化学结构式(Chemical Structure):
参考文献No.35946
标题:Cocaine receptor binding ligands
作者:Kuhar, M.J.; Carroll, F.I.; Boja, J.W.; Lewin, A.H.; Abraham, P. (Research Triangle Institute)
来源:EP 0993301; JP 2001525795; US 6531483; WO 9807427
合成路线图解说明:

Condensation of 3-beta-(4-chlorophenyl)-2-beta-(carbomethoxy)tropane (I) with the lithiated derivative of 4-methylacetophenone oxime (II) leads to the beta-keto oxime (III). Cyclizative dehydration of (III) upon heating in the presence of sulfuric acid provides the target isoxazole compound.

参考文献No.41316
标题:Cocaine receptor binding ligands
作者:Abraham, P.; Kuhar, M.J.; Boja, J.W.; Lewin, A.H.; Carroll, F.I. (Research Triangle Institute)
来源:EP 1079833; JP 2002516278; US 6482837; WO 9961023
合成路线图解说明:

Condensation of 3-beta-(4-chlorophenyl)-2-beta-(carbomethoxy)tropane (I) with the lithiated derivative of 4-methylacetophenone oxime (II) leads to the beta-keto oxime (III). Cyclizative dehydration of (III) upon heating in the presence of sulfuric acid provides the target isoxazole compound.

参考文献No.777481
标题:Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes
作者:Carroll, F.Y.; Pawlush, N.; Kuhar, M.J.; Pollard, G.T.; Howard, J.L.
来源:J Med Chem 2004,47(2),296
合成路线图解说明:

Condensation of 3-beta-(4-chlorophenyl)-2-beta-(carbomethoxy)tropane (I) with the lithiated derivative of 4-methylacetophenone oxime (II) leads to the beta-keto oxime (III). Cyclizative dehydration of (III) upon heating in the presence of sulfuric acid provides the target isoxazole compound.

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