【药物名称】PD-116948, DPCPX, CPX
化学结构式(Chemical Structure):
参考文献No.139958
标题:8-Aryl- and 8-cycloalkyl-1,3-dipropylxanthines: Further potent and selective antagonists for A1-adenosine receptors
作者:Shamim, M.T.; Ukena, D.; Padgett, W.L.; Hong, O.; Daly, J.W.
来源:J Med Chem 1988,31(3),613
合成路线图解说明:

CPX has been obtained by two related ways: 1) Nitrosation of 6-amino-1,3-dipropyluracil (I) with NaNO2 in acetic acid gives the 5-nitrosouracil derivative (II), which is reduced with H2 over Pd/C in ethanol to yield 5,6-diamino-1,3-dipropyluracil (III). Acylation of (III) with cyclopentanecarboxylic acid (IV) by heating up to the mixture's melting point or by treatment with diisopropylcarbodiimide (DIC) gives the amide (V), which is finally cyclized by means of NaOH in refluxing water or refluxing methanol/water. 2) Acylation of the 5-nitrosouracil (II) with cyclopentanecarbonyl chloride (VI) by means of lithium hexamethyldisilazane (LHMDS) in THF gives the amide (VII), which is submitted to a reductive cyclization with Sn(OAc)2 in the same solvent.

参考文献No.590895
标题:1,3,8-Trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity
作者:Erickson, R.H.; Hiner, R.N.; Feeney, S.W.; Blake, P.R.; Rzeszotarski, W.J.; Hicks, R.P.; Costello, D.G.; Abreu, M.E.
来源:J Med Chem 1991,34(4),1431
合成路线图解说明:

CPX has been obtained by two related ways: 1) Nitrosation of 6-amino-1,3-dipropyluracil (I) with NaNO2 in acetic acid gives the 5-nitrosouracil derivative (II), which is reduced with H2 over Pd/C in ethanol to yield 5,6-diamino-1,3-dipropyluracil (III). Acylation of (III) with cyclopentanecarboxylic acid (IV) by heating up to the mixture's melting point or by treatment with diisopropylcarbodiimide (DIC) gives the amide (V), which is finally cyclized by means of NaOH in refluxing water or refluxing methanol/water. 2) Acylation of the 5-nitrosouracil (II) with cyclopentanecarbonyl chloride (VI) by means of lithium hexamethyldisilazane (LHMDS) in THF gives the amide (VII), which is submitted to a reductive cyclization with Sn(OAc)2 in the same solvent.

参考文献No.590898
标题:Convenient one-pot synthesis of xanthines from 6-amino-5-nitrosouracils
作者:Schow, S.R.; Lum, R.T.; Melville, C.R.; Nelson, M.G.; Moore, A.G.
来源:Synthesis 1999,(7),1123
合成路线图解说明:

CPX has been obtained by two related ways: 1) Nitrosation of 6-amino-1,3-dipropyluracil (I) with NaNO2 in acetic acid gives the 5-nitrosouracil derivative (II), which is reduced with H2 over Pd/C in ethanol to yield 5,6-diamino-1,3-dipropyluracil (III). Acylation of (III) with cyclopentanecarboxylic acid (IV) by heating up to the mixture's melting point or by treatment with diisopropylcarbodiimide (DIC) gives the amide (V), which is finally cyclized by means of NaOH in refluxing water or refluxing methanol/water. 2) Acylation of the 5-nitrosouracil (II) with cyclopentanecarbonyl chloride (VI) by means of lithium hexamethyldisilazane (LHMDS) in THF gives the amide (VII), which is submitted to a reductive cyclization with Sn(OAc)2 in the same solvent.

参考文献No.597450
标题:CPX
作者:Casta馿r, J.; Mart韓, L.; Sorbera, L.A.
来源:Drugs Fut 2000,25(10),1011
合成路线图解说明:

CPX has been obtained by two related ways: 1) Nitrosation of 6-amino-1,3-dipropyluracil (I) with NaNO2 in acetic acid gives the 5-nitrosouracil derivative (II), which is reduced with H2 over Pd/C in ethanol to yield 5,6-diamino-1,3-dipropyluracil (III). Acylation of (III) with cyclopentanecarboxylic acid (IV) by heating up to the mixture's melting point or by treatment with diisopropylcarbodiimide (DIC) gives the amide (V), which is finally cyclized by means of NaOH in refluxing water or refluxing methanol/water. 2) Acylation of the 5-nitrosouracil (II) with cyclopentanecarbonyl chloride (VI) by means of lithium hexamethyldisilazane (LHMDS) in THF gives the amide (VII), which is submitted to a reductive cyclization with Sn(OAc)2 in the same solvent.

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