- 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; 0041-0045
(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 0041-0045
(2021/03/23)
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- Construction of 5,6-ring-fused 2-pyridones: An effective annulation tactic achieved in water
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An efficient protocol to annulate the 5,6-fused 2-pyridone ring system, exploiting a tandem condensation of propiol-amide and cyclic -keto methyl esters in water, followed by acid- or base-promoted intramolecular ring closure and decarboxylation, has been
- Smith III, Amos B.,Atasoylu, Onur,Beshoreb, Douglas C.
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experimental part
p. 2643 - 2646
(2010/01/16)
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- A Simplified Route to a Key Intermediate in the Synthesis of the Chinese Nootropic Agent Huperzine A
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An efficient one-pot, three-component process for the preparation of 2-pyridones from a carbonyl compound, ammonia, and methyl propiolate has been found which provides ready access to a key intermediate in the synthesis of huperzine A.
- Kozikowski, Alan P.,Reddy, E. Rajarathnam,Miller, Chris P.
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p. 195 - 197
(2007/10/02)
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