An Improved Scalable Process for the Synthesis of (S,S)-DACH-Ph Trost Ligand
SYNLETT(2022)
摘要
An improved chemical process has been developed for the synthesis of (S,S)-DACH-Ph Trost ligand. The amidation of 2-diphenylphosphinylbenzoic acid and (S,S)-diaminocyclohexarie is promoted by stoichiometric CDI and catalytic imidazole hydrochloride. The resulting product, (S,S)-DACH-Ph Trost ligand, is isolated as a white solid in 80% yield with >99% ee by simple filtration without column chromatography. The current facile process is also demonstrated on kilogram scale.
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关键词
Trost ligand, DACH-Ph, coupling, 2-diphenylphosphinyl-benzoic acid, chiral diaminocyclohexane, CDI, imidazole hydrochloride, kilogram
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