【药物名称】Imatinib mesylate, GGP-57148B, STI-571, CGP-57148(free base), Gleevec, Glivec
化学结构式(Chemical Structure):
参考文献No.21932
标题:Pyrimidine derivs. and process for their preparation
作者:Zimmermann, J. (Novartis AG)
来源:EP 0564409; JP 1994087834; US 5521184
合成路线图解说明:

The condensation of 1-(3-pyridyl)ethanone (I) with dimethylformamide dimethylacetal (II) gives 3-(dimethylamino)-1-(3-pyridyl)-2-propen-1-one (III), which is cyclized with 1-(2-methyl-5-nitrophenyl)guanidine (IV) [obtained by reaction of 2-methyl-5-nitroaniline (V) with cyanamide (VI)] in refluxing isopropanol to yield the pyrimidine derivative (VII). Reduction of the nitro group of (VII) with H2 over Pd/C in THF affords the corresponding amino compound (VIII), which is finally condensed with 4-(4-methylpiperazin-1-ylmethyl)benzoyl chloride (IV) in pyridine.

参考文献No.72294
标题:A process of preparing imatinib and imatinib prepared thereby
作者:Kankan, R.N.; Rao, D.R.; Wain, C.P. (Cipla Ltd.)
来源:GB 2398565; WO 0474502
合成路线图解说明:

The condensation of 1-(3-pyridyl)ethanone (I) with dimethylformamide dimethylacetal (II) gives 3-(dimethylamino)-1-(3-pyridyl)-2-propen-1-one (III), which is cyclized with 1-(2-methyl-5-nitrophenyl)guanidine (IV) [obtained by reaction of 2-methyl-5-nitroaniline (V) with cyanamide (VI)] in refluxing isopropanol to yield the pyrimidine derivative (VII). Reduction of the nitro group of (VII) with H2 over Pd/C in THF affords the corresponding amino compound (VIII), which is finally condensed with 4-(4-methylpiperazin-1-ylmethyl)benzoyl chloride (IV) in pyridine.

参考文献No.422282
标题:Potent and selective inhibitors of the Abl-kinase: Phenylaminopyrimidine (PAP) derivatives
作者:Buchdunger, E.; Mett, H.; Meyer, T.; Lydon, N.B.; Zimmermann, J.
来源:Bioorg Med Chem Lett 1997,7(2),187
合成路线图解说明:

The condensation of 1-(3-pyridyl)ethanone (I) with dimethylformamide dimethylacetal (II) gives 3-(dimethylamino)-1-(3-pyridyl)-2-propen-1-one (III), which is cyclized with 1-(2-methyl-5-nitrophenyl)guanidine (IV) [obtained by reaction of 2-methyl-5-nitroaniline (V) with cyanamide (VI)] in refluxing isopropanol to yield the pyrimidine derivative (VII). Reduction of the nitro group of (VII) with H2 over Pd/C in THF affords the corresponding amino compound (VIII), which is finally condensed with 4-(4-methylpiperazin-1-ylmethyl)benzoyl chloride (IV) in pyridine.

参考文献No.627415
标题:Imatinib Mesilate
作者:Casta馿r, J.; Fern醤dez, R.; de Bree, F.; Sorbera, L.A.
来源:Drugs Fut 2001,26(6),545
合成路线图解说明:

The condensation of 1-(3-pyridyl)ethanone (I) with dimethylformamide dimethylacetal (II) gives 3-(dimethylamino)-1-(3-pyridyl)-2-propen-1-one (III), which is cyclized with 1-(2-methyl-5-nitrophenyl)guanidine (IV) [obtained by reaction of 2-methyl-5-nitroaniline (V) with cyanamide (VI)] in refluxing isopropanol to yield the pyrimidine derivative (VII). Reduction of the nitro group of (VII) with H2 over Pd/C in THF affords the corresponding amino compound (VIII), which is finally condensed with 4-(4-methylpiperazin-1-ylmethyl)benzoyl chloride (IV) in pyridine.

Drug Information Express,Drug R&D,Chemical Database,Patent Search.
Copyright © 2006-2024 Drug Future. All rights reserved.Contact Us