1-[Nα-[[(S)-4-オキソ-2-アゼチジニル]カルボニル]-L-ヒスチジル]-L-プロリンアミド

1-[Nα-[[(S)-4-オキソ-2-アゼチジニル]カルボニル]-L-ヒスチジル]-L-プロリンアミド 化学特性,用途語,生産方法

• Originator

  Azetirelin,ZYF Pharm Chemical

• Manufacturing Process

  In 13 ml of DMF was dissolved 826.0 mg of L-histidyl-L-prolinamide 2- hydrobromide and then 2 ml of a DMF solution of 405.0 mg of triethylamine was added to the solution under ice-cooling. After maintaining 30 min under ice-cooling, the precipitates thus formed were filtered off to provide L-histidyl- L-prolinamide.
  In 10 ml of DMF was dissolved 230.0 mg of (S)-2-azetidinone-4-carboxylic acid and then 351.0 mg of N-hydroxy-1,2,3-benzotriazole and 453.0 mg of dicyclohexylcarbodiimide were added to the solution under ice-cooling. Then, after stirring the mixture for 15 min, the reaction was maintained for 15 min at room temperature. The reaction mixture was ice-cooled again and 15 ml of a DMF solution of foregoing L-histidyl-L-prolinamide was added to the reaction mixture followed by reaction overnight at 0°C. The precipitates thus formed were filtered off, the filtrate was concentrated to dryness, the residue was dissolved in 10 ml of chloroform-methanol (4:1) and subjected to silica gel column chromatography. The eluates by chloroform-methanol (7:3) were collected and concentrated to dryness to provide 509.0 mg of crude product. When the product was subjected to silica gel column chromatography again and eluted by a mixture of chloroform, methanol, and aqueous ammonia (40:10:1) to provide 394.0 mg of pure Nepsilon-[(S)-2-azetidinone-4-carbonyl]- L-histidyl-L-prolinamide, melting point 183°-185°C (crystallization from a small amount of methanol).

• Therapeutic Function

  TRH analogue

1-[Nα-[[(S)-4-オキソ-2-アゼチジニル]カルボニル]-L-ヒスチジル]-L-プロリンアミド 上流と下流の製品情報

1-[Nα-[[(S)-4-オキソ-2-アゼチジニル]カルボニル]-L-ヒスチジル]-L-プロリンアミド 生産企業

Global(7)Suppliers

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