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【结 构 式】

【药物名称】VUF-K-8788

【化学名称】7-[3-[4-(2-Quinolinylmethyl)-1-piperazinyl]propoxy]-3,4-dihydro-2H-1,4-benzothiazin-3-one

【CA登记号】219741-10-3

【 分 子 式 】C25H28N4O2S

【 分 子 量 】448.59151

【开发单位】Kowa (Originator)

【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, RESPIRATORY DRUGS, Histamine H1 Antagonists

合成路线1

The alkylation of N-formylpiperazine (II) with 2-(chloromethyl)quinoline (I) produced the disubstituted piperazine (III). The formyl group of (III) was then cleaved by means of H2SO4 in boiling EtOH, yielding quinolylmethylpiperazine (IV). Subsequent alkylation of (IV) with 1-bromo-3-chloropropane (V) afforded the chloropropyl derivative (VI). This was finally condensed with 7-hydroxybenzothiazinone (VII) in the presence of K2CO3 and a phase-transfer catalyst to furnish the title compound.

1 Tohma, T.; Onogi, K.; Zang, M.; Timmerman, H.; Wada, Y.; Tamura, M. (Kowa Co., Ltd.); Diamine derivs. and pharmaceutical containing the same. EP 0957100; WO 9902520 .
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) 13162 2-(Chloromethyl)quinoline; alpha-Chloroquinaldine 4377-41-7 C10H8ClN 详情 详情
(II) 23801 1-piperazinecarbaldehyde; N-Formylpiperazine 7755-92-2 C5H10N2O 详情 详情
(III) 41113 4-(2-quinolinylmethyl)-1-piperazinecarbaldehyde C15H17N3O 详情 详情
(IV) 41114 2-(1-piperazinylmethyl)quinoline C14H17N3 详情 详情
(V) 10358 1-Bromo-3-chloropropane 109-70-6 C3H6BrCl 详情 详情
(VI) 41115 2-[[4-(3-chloropropyl)-1-piperazinyl]methyl]quinoline C17H22ClN3 详情 详情
(VII) 28290 7-hydroxy-2H-1,4-benzothiazin-3(4H)-one C8H7NO2S 详情 详情
Extended Information