【药物名称】
化学结构式(Chemical Structure):
参考文献No.485994
标题:Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors
作者:Hirokawa, Y.; Yoshida, N.; Kato, S.
来源:Bioorg Med Chem Lett 1998,8(12),1551
合成路线图解说明:

Esterification of 2,6-difluoronicotinic acid (I) with methanol and sulfuric acid afforded methyl ester (II). This was treated with methylamine in DMF at 5 C to give a 2:1 mixture of the desired 6-methylaminonicotinate (III) and its regioisomer (IV), which were separated by column chromatography. Reaction of (III) with potassium methoxide generated from methanol and potassium tert-butoxide yielded methyl ether (V). Then, bromination with N-bromosuccinimide in DMF gave bromoester (VI), which was subsequently hydrolyzed with aqueous NaOH to provide acid (VII). Finally, the target amide was prepared by condensation of acid (VII) with the chiral amine (VIII) in the presence of carbonyldiimidazole.

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