-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	32364
标题:	Heterocyclic cpds. as pharmaceutical
作者:	Haigh, D.; Sime, J. (SmithKline Beecham plc)
来源:	EP 1000938; US 5869495; US 6048883; WO 9401420

合成路线图解说明: Rhodium acetate-mediated insertion of methanol into diazotyrosine methyl ester (I) provided the alpha-methoxy ester (IIa-b). Subsequent alkylation of (IIa-b) with mesylate (III) using NaH in DMF gave the racemic adduct (IVa-b). Finally, kinetic resolution of (Va-b) employing the lipase from Rhizopus delemar at a pH of 7.0 produced the desired (S)-acid while leaving the unchanged (R)-ester (V).

参考文献No.	539886
标题:	Non-thiazolidinedione antihyperglycaemic agents. Part 3: The effects of stereochemistry on the potency of alpha-methoxy-beta-phenylpropanoic acids
作者:	Haigh, D.; Allen, G.; Birrell, H.C.; Buckle, D.R.; Cantello, B.C.; Eggleston, D.S.; Haltiwanger, R.C.; Holder, J.C.; Lister, C.A.; Pinto, I.L.; Rami, H.K.; Sime, J.T.; Smith, S.A.; Sweeney, J.D.
来源:	Bioorg Med Chem 1999,7(5),821

合成路线图解说明: Rhodium acetate-mediated insertion of methanol into diazotyrosine methyl ester (I) provided the alpha-methoxy ester (IIa-b). Subsequent alkylation of (IIa-b) with mesylate (III) using NaH in DMF gave the racemic adduct (IVa-b). Finally, kinetic resolution of (Va-b) employing the lipase from Rhizopus delemar at a pH of 7.0 produced the desired (S)-acid while leaving the unchanged (R)-ester (V).