【药物名称】MR-20492
化学结构式(Chemical Structure):
参考文献No.465343
标题:Design and synthesis of a new type of non steroidal human aromatase inhibitors
作者:Sonnet, P.; Guillon, J.; Enguehard, C.; Dallemagne, P.; Bureau, R.; Rault, S.; Auvray, P.; Moslemi, S.; Sourdiane, P.; Galopin, S.; Seralini, G.E.
来源:Bioorg Med Chem Lett 1998,8(9),1041
合成路线图解说明:

Title compound was prepared by condensation of tetrahydroindolizinone (I) with pyridine-4-carboxyaldehyde (II) under phase transfer conditions using NaOH and tetrabutyl hydrogensulfate in a mixture of H2O and CH2Cl2.

参考文献No.554764
标题:MR 20492 and MR 20494: Two indolizinone derivatives that strongly inhibit human aromatase
作者:Auvray, P.; Sourdaine, P.; Moslemi, S.; S閞alini, G.-E.; Sonnet, P.; Enguehard, C.; Guillon, J.; Dallemagne, P.; Bureau, R.; Rault, S.
来源:J Steroid Biochem Mol Biol 1999,70(1-3),59
合成路线图解说明:

The cyclization of the amino group of 4-amino-3-(4-chlorophenyl)butyric acid (I) with 2,5-dimethoxytetrahydrofuran (II) by means of AcOH in THF gives the corresponding pyrrole (III), which is cyclized by means of TEA, ClCOOEt, pyrrolidine and POCl3 in toluene yielding the pyrrolopyridone (IV). Finally, this compound is condensed with pyridine-4-carbaldehyde (V) by means of tetrabutylammonium bisulfate and NaOH in water.

合成路线图解说明:

The cyclization of the amino group of 4-amino-3-(4-chlorophenyl)butyric acid (I) with 2,5-dimethoxytetrahydrofuran (II) by means of AcOH in THF gives the corresponding pyrrole (III), which is cyclized by means of TEA, ClCOOEt, pyrrolidine and POCl3 in toluene yielding the pyrrolopyridone (IV). Finally, this compound is condensed with pyridine-3-carbaldehyde (V) by means of tetrabutylammonium bisulfate and NaOH in water.

参考文献No.583429
标题:New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives
作者:Sonnet, P.; Dallemagne, P.; Guillon, J.; Enguehard, C.; Stiebing, S.; Tanguy, J.; Bureau, R.; Rault, S.; Auvray, P.; Moslemi, S.; Sourdaine,P.; Seralini, G.E.
来源:Bioorg Med Chem 2000,8(5),945
合成路线图解说明:

Title compound was prepared by condensation of tetrahydroindolizinone (I) with pyridine-4-carboxyaldehyde (II) under phase transfer conditions using NaOH and tetrabutyl hydrogensulfate in a mixture of H2O and CH2Cl2.

合成路线图解说明:

The cyclization of the amino group of 4-amino-3-(4-chlorophenyl)butyric acid (I) with 2,5-dimethoxytetrahydrofuran (II) by means of AcOH in THF gives the corresponding pyrrole (III), which is cyclized by means of TEA, ClCOOEt, pyrrolidine and POCl3 in toluene yielding the pyrrolopyridone (IV). Finally, this compound is condensed with pyridine-4-carbaldehyde (V) by means of tetrabutylammonium bisulfate and NaOH in water.

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