XR-835

Chemical Name: (4R,5S,6S,7R)-4,7-Dibenzyl-5,6-dihydroxy-1,3-bis(1H-indazol-5-ylmethyl)perhydro-1,3-diazepin-2-one
CAS No. 167825-84-5
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线: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: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.