Preparation method of chiral amino cyanide containing pyrazolidone structure

The invention discloses a preparation method of a chiral amino cyanide containing a pyrazolidone structure. The method is characterized by: taking annular hydrazone as a reactant, under the catalysis of a chiral thiourea catalyst, adopting trimethylsilyl cyanide as a cyanation reagent, employing mes...

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Hauptverfasser: LI NAIKAI, WANG XINGWANG
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The invention discloses a preparation method of a chiral amino cyanide containing a pyrazolidone structure. The method is characterized by: taking annular hydrazone as a reactant, under the catalysis of a chiral thiourea catalyst, adopting trimethylsilyl cyanide as a cyanation reagent, employing mesitylene as a solvent, and leaving the materials to react for 10-144h under -15DEG C, thus obtaining the chiral amino cyanide. The catalyst used in the invention is prepared from industrial, cheap and easily available raw materials. The adopted cyanation reagent has low toxicity and a low price. The involved reaction condition is mild, the post-treatment is simple and convenient, and the reaction is free of an N-N bond fracture process and generates no imine by-product. The range of substrates applicable to the invention is wide, the functional group compatibility is high, and the stereoselectivity is good or excellent, so that the invention provides an efficient method for synthesis of the chiral amino cyanide with