Bromerguride, 2-Br-LIS, ZK-95451

溴麦角脲Chemical Name: 3-(2-Bromo-9,10-didehydro-6-methylergolin-8alpha-yl)-1,1-diethylurea; 2-Bromolisuride; (6aR,9S)-N'-[5-Bromo-7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinolin-9-yl]-N,N-diethylurea
CAS No. 83455-48-5, 83455-49-6 (monoBr salt)
项目整合开发状态: Phase II
项目研究机构: Schering AG (Originator)
合成路线:The condensation of 1 2-benzenediamine (I) with methyltetrahydro-5-methyl 4-oxo-3-thiophenecarboxylate (II) in toluene using a Dean-Stark trap gives the triyclic system (III),which is dehydrogenated to 4,9-dihydro-3-methyl-10H-thienol[3,4-b][1,5]benzodiazepin-10-one (IV).Treatment of (IV) with chloroacetyl chloride in dioxane in the presence of K2CO3 yields 4-chloroacetyl-4,9-dihydro-3-methyl-10H-thieno[3,4-b][1,5]benzodiazepin-10-one (V),which is finally reacted with N-methylpiperazine to produce telenzepine,which is isolated as the hydrochloride.

合成路线:Bromerguride is prepared by bromination of lisuride (I).