【药物名称】XR-835
化学结构式(Chemical Structure):
参考文献No.409789
标题:Potent cyclic urea HIV protease inhibitors with benzofused heterocycles as P2/P2' groups
作者:Wang, H.; Johnson, B.L.; Rodgers, J.D.; et al.
来源:Bioorg Med Chem Lett 1996,6(24),2919
合成路线图解说明:

The reduction of indazole-5-carboxylic acid (I) with diisobutylaluminum hydride (DIBAL) in dichloromethane gives the expected methanol (II), which by reaction with mesyl chloride and ethyldiisopropylamine in DMF is converted into 5-(chloromethyl)indazole (III). Finally, this compound is condensed with (4R,5S,6S,7R)-4,7-dibenzyl-5,6-dihydroxyperhydro-1,3-diazepin-2-one (IV) by means of NaH in DMF.

合成路线图解说明:

The radical bromination of 5-methylidazole (V) by means of N-bromosuccinimide (NBS) and benzoyl peroxide in refluxing CCl4 gives the corresponding bromomethyl derivative (VI), which is then condensed with the diazepine (IV) as before.

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