153243-81-3Relevant academic research and scientific papers
Method for synthesizing chiral 4-hydroxy amino acid derivative
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Paragraph 0118; 0123-0128, (2021/09/26)
The invention discloses a method for synthesizing a chiral 4-hydroxy amino acid derivative, which comprises the following steps: by taking a diphosphine dinitrogen chiral ruthenium complex as a catalyst, a racemic allyl alcohol compound and glycine imino ester as substrates, quaternary ammonium salt and 18-crown ether-6 as additives and cesium carbonate and the like as alkali, synthesizing the chiral 4-hydroxy amino acid derivative in an inert gas atmosphere through an asymmetric hydrogen borrowing strategy, and realizing stereoselective control of two remote chiral centers. According to the method, the substrate is cheap and easy to obtain, an oxidizing agent and a reducing agent do not need to be additionally added, atom economy is high, reaction conditions are mild, operation is easy and convenient, the obtained chiral compound is good in yield and high in stereoselectivity, the chiral compound with the (2R, 5S) configuration or the (2S, 5R) configuration serves as the main component, the substrate can be further converted into a chiral amino alcohol, a chiral diol and a chiral heterocyclic compound, the method is a green method for synthesizing the chiral 4-hydroxy amino acid derivative.
Application of asymmetric phase-transfer catalysis in the enantioselective synthesis of cis-5-substituted proline esters
Lygo, Barry,Beynon, Christopher,McLeod, Michael C.,Roy, Claude-Eric,Wade, Charles E.
experimental part, p. 8832 - 8836 (2011/01/04)
A simple, highly stereoselective three-step sequence for the enantioselective synthesis of cis-5-substituted proline esters is described. This sequence features an asymmetric PTC Michael addition, followed by acid catalysed imine exchange and catalytic hydrogenation. Application of this chemistry in the synthesis of the nonpeptide cholecystokinin antagonist (+)-RP-66803 11 is also described.
Pyrrolidine and thiazolidine derivatives, their preparation and medicaments containing them
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, (2008/06/13)
This invention relates to compositions of formula: STR1 and their salts, their preparation and the medicaments containing them.
