インジセトロン塩酸塩

インジセトロン塩酸塩 化学特性,用途語,生産方法

• 効能

  制吐薬, セロトニン5-HT3受容体拮抗薬

• 商品名

  シンセロン (杏林製薬)

• Originator

  Nisshin (Japan)

• brand name

  Sinseron

• 合成

  The synthesis is highlighted in the Scheme. Bromoacetaldehyde dimethyl acetal (44) was condensed with methylamine with KOH in refluxing ethyleneglycol for 3 hr to give 33% yield of bis(2,2-dimethoxyethyl)amine (45), which was cyclized with acetonedicarboxylic acid (46) and methylamine to generate 3,9-dimethyl-3,9-diazabicyclo- [3.3.1]nonan-7-one (47) in 12% yield. Compound 47 was reacted with hydroxylamine in refluxing pyridine and ethanol mixture to give corresponding oxime 48 in 88% yield, which was subsequently reduced with hydrogen over Raney Ni in hot ethanol in the presence of ammonium acetate at 50 kg/cm2 to give amine 49 in 89% yield. Compound 49 was condensed with 1H-indazole-3-carbonyl chloride (50) in pyridine with catalytic amount of DMAP to give crude indisteron free base, which was re-crystallized from chloroform/hexane to give indisteron free base as colorless crystals in 16% yield. Finally, the free base was treated with hydrogen chloride to give indisteron hydrochloride (VII).

  

インジセトロン塩酸塩 生産企業

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