【药物名称】FE-999011
化学结构式(Chemical Structure):
参考文献No.55378
标题:Compsns. for improving fertility
作者:Broqua, P. (Ferring BV Group Holding)
来源:WO 0056296
合成路线图解说明:

The condensation of N-(tert-butoxycarbonyl)-L-tert-butyl-glycine N-succinimidyl ester (I) with L-prolinamide (II) by means of DIEA in dichloromethane gives the dipeptide amide (III), which is dehydrated by means of POCl3 and imidazole in pyridine to yield N-(tert-butoxycarbonyl)-L-tert-butylglycyl-L-prolinenitrile (IV). Finally, this compound is deprotected by means of trifluoroacetic acid to provide the target dipeptide nitrile.

参考文献No.55379
标题:Compsns. for promoting growth
作者:Broqua, P. (Ferring BV Group Holding)
来源:WO 0056297
合成路线图解说明:

The condensation of N-(tert-butoxycarbonyl)-L-tert-butyl-glycine N-succinimidyl ester (I) with L-prolinamide (II) by means of DIEA in dichloromethane gives the dipeptide amide (III), which is dehydrated by means of POCl3 and imidazole in pyridine to yield N-(tert-butoxycarbonyl)-L-tert-butylglycyl-L-prolinenitrile (IV). Finally, this compound is deprotected by means of trifluoroacetic acid to provide the target dipeptide nitrile.

参考文献No.672609
标题:2-Cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV
作者:Ashworth, D.M.; et al.
来源:Bioorg Med Chem Lett 1996,6(10),1163
合成路线图解说明:

The condensation of N-(tert-butoxycarbonyl)-L-tert-butyl-glycine N-succinimidyl ester (I) with L-prolinamide (II) by means of DIEA in dichloromethane gives the dipeptide amide (III), which is dehydrated by means of POCl3 and imidazole in pyridine to yield N-(tert-butoxycarbonyl)-L-tert-butylglycyl-L-prolinenitrile (IV). Finally, this compound is deprotected by means of trifluoroacetic acid to provide the target dipeptide nitrile.

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