【药物名称】GPI-1234
化学结构式(Chemical Structure):
参考文献No.36258
标题:Heterocyclic thioesters and ketones
作者:Hamilton, G.S.; Li, J.-H. (Guilford Pharmaceuticals Inc.)
来源:EP 0934263; US 5786378; US 5990131; WO 9813343
合成路线图解说明:

Acylation of L-proline methyl ester (I) with methoxalyl chloride (II) afforded oxamate (III), which was condensed with 1,1-dimethylpropyl magnesium chloride to produce ketoamide (IV). Hydrolysis of the methyl ester of (IV) with LiOH gave carboxylic acid (V). This was finally coupled with 3,3-diphenylpropyl mercaptan (VI) using DCC and dimethylaminopyridine to give the title thioether.

参考文献No.38942
标题:Hair growth compsns. and uses
作者:Hamilton, G.S.; Steiner, J.P. (Guilford Pharmaceuticals Inc.)
来源:WO 9855090
合成路线图解说明:

Acylation of L-proline methyl ester (I) with methoxalyl chloride (II) afforded oxamate (III), which was condensed with 1,1-dimethylpropyl magnesium chloride to produce ketoamide (IV). Hydrolysis of the methyl ester of (IV) with LiOH gave carboxylic acid (V). This was finally coupled with 3,3-diphenylpropyl mercaptan (VI) using DCC and dimethylaminopyridine to give the title thioether.

参考文献No.536853
标题:Synthesis of thioester FKBP12 ligands and evaluation of their in vitro and in vivo nerve regenerative effects
作者:Limburg, D.C.; et al.
来源:217th ACS Natl Meet (March 21 1999, Anaheim) 1999,Abst MEDI 237
合成路线图解说明:

Acylation of L-proline methyl ester (I) with methoxalyl chloride (II) afforded oxamate (III), which was condensed with 1,1-dimethylpropyl magnesium chloride to produce ketoamide (IV). Hydrolysis of the methyl ester of (IV) with LiOH gave carboxylic acid (V). This was finally coupled with 3,3-diphenylpropyl mercaptan (VI) using DCC and dimethylaminopyridine to give the title thioether.

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