Synthesis and process optimization of key intermediate of suvorexant-chiral homopiperazine
Suvorexant is a dual orexin receptor antagonist for treating insomnia.The synthetic process of the key intermediate of suvorexant,chiral homopiperazine,was improved in this work.Using methyl(S)-3-hydroxybutyrate(1)as the starting material,the key intermediate(R)-7-methyl-l-[(4-nitrophenyl)sulfonyl]-1,4-diazepane hydrochloride(6)was obtained through substitution,reduction,ring cleavage,Mitsunobu cyclization and deprotection.The structure of target compound was confirmed by ESI-MS and 1H-NMR.This improved process has advantages of inexpensive raw materials,simple purifying operation and stable and controllable product quality.
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