【药物名称】
化学结构式(Chemical Structure):
参考文献No.616090
标题:2,4-Thiazolidinediones as potent and selective human beta3 agonists
作者:Hu, B.; Ellingboe, J.; Gunawan, I.; Han, S.; Largis, E.; Li, Z.; Malamas, M.S.; Mulvey, R.; Oliphant, A.; Sum, F.W.; Tillett, J.; Wong, V.
来源:Bioorg Med Chem Lett 2001,11(6),757
合成路线图解说明:

The condensation of benzaldehyde (I) with thiazolidine-2,4-dione (II) by means of piperidine in ethanol gives the benzylidene-thiazolidinedione (III), which is reduced with H2 over Pd/C in methanol to yield the benzyl derivative (IV). The cleavage of the cyclic ketal group of (IV) with HCl affords the piperidone (V), which is finally reductocondensed with the chiral ethanolamine (VI) by means of sodium triacetoxyborohydride in DMF to provide the target compound. The intermediate ethanolamine (VI) has been obtained as follows: The reaction of 3-amino-4-(benzyloxy)acetophenone (VII) with Ms-Cl and pyridine in dichloromethane gives the expected sulfonamide (VIII), which is brominated with CuBr2 in chloroform to yield the phenacyl bromide (IX). Enantioselective reduction with the Corey's chiral oxazaborolidine catalyst affords the (R)-bromoethanol derivative (X), which is treated with NaN3 in DMSO to provide the azido compound (XI). Finally, this compound is reduced and debenzylated by hydrogenation with H2 over Pd/C in methanol to furnish the desired ethanolamine intermediate (VI).

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