【药物名称】
化学结构式(Chemical Structure):
参考文献No.49877
标题:Imidazopyrimidinyl and imidazopyridinyl derivs.
作者:Wilde, R.G.; Bakthavatchalam, R.; Beck, J.P.; Arvanitis, A. (Bristol-Myers Squibb Co.)
来源:EP 1244666; JP 2003516992; WO 0144248
合成路线图解说明:

Chlorination of 4-(trifluoromethoxy)aniline (V) employing N-chlorosuccinimide affords the 2-chloro aniline (VI). Diazotization of aniline (VI) and subsequent quenching with potassium iodide gives rise to the aryl iodide (VII). This is converted into the arylboronic acid (VIII) by lithiation with butyllithium, followed by reaction with triisopropyl borate. Suzuki coupling between chloropyridine (IV) and boronic acid (VIII) leads to the phenylpyridine (IX). Reduction of the nitro group of (IX) employing sodium dithionite provides the diaminopyridine (X). This is finally condensed with triethyl orthopropionate to produce the target imidazopyridine compound.

参考文献No.713309
标题:Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands
作者:Arvanitis, A.G.; Rescinito, J.T.; Arnold, C.R.; Wilde, R.G.; Fitzgerald, L.W.; Zaczek, R.; Hartig, P.R.; Grossman, S.; Arneric, S.P.; Gilligan, P.J.; Olson, R.E.; Robertson, D.W.
来源:Bioorg Med Chem Lett 2003,13(1),129
合成路线图解说明:

4-Chloro-2-hydroxy-3-nitropyridine (I) is condensed with (S)-2-pentylamine (II) to produce the aminopyridine adduct (III). Subsequent chlorination of (III) by means of POCl3 furnishes the chloropyridine derivative (IV).

合成路线图解说明:

Chlorination of 4-(trifluoromethoxy)aniline (V) employing N-chlorosuccinimide affords the 2-chloro aniline (VI). Diazotization of aniline (VI) and subsequent quenching with potassium iodide gives rise to the aryl iodide (VII). This is converted into the arylboronic acid (VIII) by lithiation with butyllithium, followed by reaction with triisopropyl borate. Suzuki coupling between chloropyridine (IV) and boronic acid (VIII) leads to the phenylpyridine (IX). Reduction of the nitro group of (IX) employing sodium dithionite provides the diaminopyridine (X). This is finally condensed with triethyl orthopropionate to produce the target imidazopyridine compound.

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