- Method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane
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The invention discloses a method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane, and belongs to the technical field of medical intermediate chiral ligands. The chiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the like in sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiral alcohol preparation is overcome, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adoptedin literature is avoided.
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Paragraph 0008; 0046-0050
(2021/03/23)
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- Method for synthesizing chiral nitrogen-phosphorus ligand L-8 containing pyridocycloheptane
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The invention discloses a method for synthesizing a chiral nitrogen-phosphorus ligand L-8 containing pyridocycloheptane, and belongs to the technical field of medical intermediate chiral ligands. Thechiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the likein sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiralalcohol preparation, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adopted in literature is avoided.
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Paragraph 0046-0050
(2021/03/23)
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