(1S-cis)-밀나시프란염산염

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

  P321：(…) 처치를 하시오.

  P332+P313：피부 자극이 생기면 의학적인 조치· 조언을 구하시오.

  P362：오염된 의복을 벗고 세척 후에 재사용하기

(1S-cis)-밀나시프란염산염 화학적 특성, 용도, 생산

• 개요

  Levomilnacipran (Fetzima®) is a dual serotonin–norepinephrine reuptake inhibitor (SNRI) approved by the FDA in 2013 for the treatment of major depressive disorders (MDD). Levomilnacipran is the most active enantiomer of the racemate Milnacipran, which is currently used to treat pain associated with fibromyalgia. The drug was developed by Forest Laboratories and the Pierre Fabre group.

• 용도

  The S-enatiomer of Milnacipran (M344600).

• Synthesis

  Reaction of phenylacetonitrile (100) and commercially available (R)-epichlorohydrin (101) with NaNH2 led to chloride displacement and intramolecular cyclopropanation, yielding lactone 102 after a one-pot nitrile hydrolysis and acid-promoted lactonization (75% yield over 3 steps). Lactone ring-opening with Et2NH¨CAlCl3 complex provided amido-alcohol 103, which was converted to its phthalimido derivative 104 by sequential treatment with thionyl chloride and potassium phthalimide in 80% over three steps. Finally, levomilnacipran hydrochloride (XIII) was obtained in >95% optical purity after phthalimide cleavage, HCl salt formation, and crystallization from HCl/i-PrOH/i-PrAc. This sequence represents a highly efficient route to levomilnacipran, requiring no isolation of intermediates, resulting in >40% overall yield, and allowing use of the same solvent solution (toluene) for all steps.

  

(1S-cis)-밀나시프란염산염 공급 업체

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