This chapter describes the discovery and development of Ru(II)-tethered catalysts for the asymmetric transfer hydrogenation of ketones and imines. Aspects of catalyst design and activity are described, as are the applications of the catalysts, notably to industrially relevant targets. This class of catalyst has enjoyed a significant amount of interest from researchers worldwide and offers exciting prospects as a practical reagent in both industrial and academic laboratories.

Tethered Ruthenium(II) Catalysts in Asymmetric Transfer Hydrogenation

The invention discloses a method for synthesizing chiral trans-carbocyclic pyrimidine nucleoside, belonging to the field of asymmetric syntheses in the organic chemistry. The method comprises the following steps: with racemic alpha-pyrimidine ring ketone 1 as a raw material, adding formic acid and triethylamine in the presence of a chiral ruthenium catalyst, and carrying out an asymmetric hydrogentransfer reaction to obtain cis-carbocyclic pyrimidine nucleoside 2 having two chiral centers; then, performing hydroxylation to form methanesulfonyl ester; and then reacting methanesulfonyl ester with sodium azide or potassium acetylthiolate or directly reacting methanesulfonyl ester with DAST to obtain the trans-carbocyclic pyrimidine nucleoside 3. The chiral trans-carbocyclic pyrimidine nucleoside compound prepared by using the method of the invention has good stereoselectivity, moderate-to-good yield and high diastereoselectivity and enantioselectivity, and enriches pyrimidine nucleosidederivatives.

Method for synthesizing chiral trans-carbocyclic pyrimidine nucleoside

The present invention relates to a method for preparing a droxidopa intermediate (2S,3R)-3-(3,4-dibenzyloxyphenyl)-2-dibenzylamino-3-hydroxypropionate, comprising carrying out asymmetric hydrogenation to 3-(3,4-dibenzyloxyphenyl)-2-dibenzylamino-3-oxo-propionate in an organic solvent under the catalysis of a ruthenium catalyst in the presence of a hydrogen donor reagent and an organic base. The reaction highly stereoselectively introduces two chiral centres of droxidopa in a high yield in one step. Furthermore, on the basis of the reaction, a method for preparing droxidopa is designed. The method has a simple and short process, and can stereoselectively synthesize droxidopa.

Method for preparing droxidopa and intermediate thereof

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Method for preparing droxidopa and intermediate thereof