Prazosin hydrochloride, CP-12299-1, Eurex, Hypovase, Minipress

盐酸哌唑嗪 哌唑嗪 Chemical Name: 1-(4-Amino-6,7-dimethoxyquinazolin-2-yl)-4-(2-furanylcarbonyl)piperazine hydrochloride
CAS No. 19237-84-4, 19216-56-9 (free base)
项目整合开发状态: Launched-1974
项目研究机构: Pfizer (Originator), Sanofi-Aventis (Not Determined)
合成路线:Treatment of carboxy polystyrene resin (I) with oxalyl chloride in dichloromethane,followed by reaction with Bu4NNCS in THF/DCM,affords isothiocyanate resin (II),to which 2-amino-4,5-dimethoxybenzonitrile (III) is attached by means of NMP to provide derivative (IV).Treatment of resin (IV) with 1-(2-furoyl)-piperazine (V) and EDC in chloroform in the presence of DIEA furnishes resin-bound guanidine (VI),from which prazosin is obtained as its trifluoroacetic acid salt (VII) by acidolysis with TFA/H2O at 80 C.Finally,the hydrochloride salt of prazosin can be obtained by treatment with HCl.