H-1152, H-1152P, HMN-1152

Chemical Name: 2-Methyl-1-(4-methylisoquinolin-5-ylsulfonyl)perhydro-1,4-diazepine hydrochloride; (4-Methylisoquinolin-5-yl)(2-methylperhydro-1,4-diazepin-1-yl)sulfone hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Nippon Shinyaku (Originator)
合成路线:Nitration of 4-methylisoquinoline (I) with KNO3 in H2SO4 provided the 5-nitro derivative (II).Subsequent catalytic hydrogenation of the nitro group of (II) gave amine (III).Diazotization of (III),followed by treatment with SO2 and CuCl2,generated the sulfonyl chloride (IV).This was condensed with 4-Boc-2-methyl-perhydro-1,4-diazepine (V) to furnish the sulfonamide (VI).The Boc protecting group of (VI) was finally cleaved using HCl in aqueous EtOH.