Telenzepine hydrochloride, SK-871, B-818-04(hemifumarate), B-803-32(free base), B-818-03

替仑西平Chemical Name: 3-Methyl-4-[2-(4-methylpiperazin-1-yl)acetyl]-9,10-dihydro-4H-thieno[3,4-b][1,5]benzodiazepin-10-one dihydrochloride
CAS No. 80880-90-6 (free base)
项目整合开发状态: Phase III
项目研究机构: Altana Pharma (Originator), Sanwa (Licensee)
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).