【药物名称】Cipamfylline, HEP-688, BRL-61063
化学结构式(Chemical Structure):
参考文献No.13118
标题:Xanthine derivs., process for their preparation and their pharmaceutical use
作者:Maschler, H.; Spicer, B.A.; Smith, H. (GlaxoSmithKline plc)
来源:AU 9052083; EP 0389282; EP 1120417; JP 1990273676; US 5734051; US 5981535; US 6180791; US 6531600
合成路线图解说明:

N,N'-Bis(cyclopropylmethyl)urea (II) was prepared by the action of phosgene on cyclopropylmethylamine (I). Cyclization of urea (II) with cyanoacetic acid (III) in hot acetic anhydride produced the 6-aminouracil (IV). Subsequent nitrosation of (IV) by means of sodium nitrite and formic acid afforded the 5-nitroso derivative (V), which was further reduced to the 5,6-diaminouracil (VI) with sodium dithionite. Formylation of diamine (VI), followed by cyclization of the intermediate formamide (VII), gave rise to 1,3-bis(cyclopropylmethyl)xanthine (VIII). Nitration of xanthine (VIII) with HNO3 in acetic acid yielded the 8-nitro derivative (IX), which was finally reduced to the corresponding amine employing either tin and HCl or sodium dithionite.

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