Fasudil hydrochloride, AT-877, HA-1077, Fasdil, Eril, -Drug Synthesis Database

【结构式】

【药物名称】Fasudil hydrochloride, AT-877, HA-1077, Fasdil, Eril

【化学名称】1-(5-Isoquinolinesulfinyl)hexahydro-1H-1,4-diazepine hydrochloride
　　　　　　1-(5-Isoquinolinesulfinyl)homopiperazine hydrochloride

【CA登记号】105628-07-7, 103745-39-7 (free base)

【分子式】C₁₄H₁₈ClN₃O₂S

【分子量】327.83546

【开发单位】Asahi Kasei (Originator), Schering AG (Licensee)

【药理作用】Angina pectoris, Treatment of, CARDIOVASCULAR DRUGS, Cerebrovascular Diseases, Treatment of, Hypertension, Treatment of, NEUROLOGIC DRUGS, Stroke, Treatment of, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, Vasodilators, Calcium Channel Blockers, Rho Kinase Inhibitors

合成路线1

5-Isoquinolinesulfonic acid (I) is heated at 85 C with SOCl2 and DMF yielding 5-isoquinolinesulfonyl chloride hydrochloride (II). The reaction of (II) with hexahydro-1H-1,4-diazepine affords hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine (III) in CH2Cl2. Finally, the reaction of (III) with HCl gives hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine hydrochloride (IV). (scheme 10964901a)

参考文献中间体

【1】 Ishida, T.; Asano, T.; HA 1077. Drugs Fut 1989, 14, 12, 1159.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	21501	5-isoquinolinesulfonic acid	27655-40-9	C₉H₇NO₃S	详情	详情
(II)	21502	5-isoquinolinesulfonyl chloride hydrochloride		C₉H₇Cl₂NO₂S	详情	详情
(III)	21503	5-(1,4-diazepan-1-ylsulfonyl)isoquinoline		C₁₄H₁₇N₃O₂S	详情	详情
(IV)	25030	1,4-diazepane	505-66-8	C₅H₁₂N₂	详情	详情

Extended Information