Noyori-Ikariya-type ruthenium(II)-catalysts for asymmetric transfer hydrogenation (ATH) have been known for 25 years and have proved as a well-behaved and user-friendly platform for the synthesis of chiral secondary alcohols. A progress has been made in the past five years in understanding the asymmetric reduction of complex ketones, where up to four stereocenters can be controlled in a single chemical transformation. Intriguing multi-chiral molecular architectures are therefore available in few well understood and robust synthetic steps from commercially available building blocks and possess handles for additional functionalization. The aim of this Review is to showcase the availability of three-dimensional scaffolds and homochiral lead-like compounds via ATH and inspire their direct use in drug discovery endeavors. Basic mechanistic insights are provided to demystify the stereo-chemical outcomes, as well as examples of diastereoselective transformations of enantiopure alcohols to give a feeling of how these rigid non-planar molecules can be further elaborated.

https://chemistry-europe.onlinelibrary.wiley.com/doi/pdf/10.1002/chem.202180162

Escaping from Flatland: Stereoconvergent Synthesis of Three-Dimensional Scaffolds via Ruthenium(II)-Catalyzed Noyori–Ikariya Transfer Hydrogenation

A catalytic protocol for the enantio- and diastereoselective reduction of α-substituted-β-keto carbonitriles is described The reaction involves a DKR-ATH process with the simultaneous construction of β-hydroxy carbonitrile scaffolds with two contiguous stereogenic centers A wide range of α-substituted-β-keto carbonitriles were obtained in high yields (94%-98%) and excellent enantio- and diastereoselectivities (up to >99% ee, up to >99:1 dr) The origin of the diastereoselectivity was also rationalized by DFT calculations Furthermore, this methodology offers rapid access to the pharmaceutical intermediates of Ipenoxazone and Tapentadol

Asymmetric Transfer Hydrogenation of α-Substituted-β-Keto Carbonitriles via Dynamic Kinetic Resolution.

Based on the ever-increasing demand for enantiomerically pure compounds, the development of efficient, atom-economical, and sustainable methods to produce chiral alcohols and amines is a major concern. Homogeneous asymmetric catalysis with transition-metal complexes including asymmetric hydrogenation (AH) and transfer hydrogenation (ATH) of ketones and imines through dynamic kinetic resolution (DKR) allowing the construction of up to three stereogenic centers is the main focus of the present short review, emphasizing the development of new catalytic systems combined to new classes of substrates and their applications as well. 1 	Introduction 2 	Asymmetric Hydrogenation via Dynamic Kinetic Resolution 2.1 	α-Substituted Ketones 2.2	α-Substituted β-Keto Esters and Amides 2.3 	α-Substituted Esters 2.4 	Imine Derivatives 3 	Asymmetric Transfer Hydrogenation via Dynamic Kinetic Resolution 3.1 	α-Substituted Ketones 3.2 	α-Substituted β-Keto Esters, Amides, and Sulfonamides 3.3 	α,β-Disubstituted Cyclic Ketones 3.4 	β-Substituted Ketones 3.5 	Imine Derivatives 4. 	Conclusion

Recent Progress and Applications of Transition-Metal-Catalyzed Asymmetric Hydrogenation and Transfer Hydrogenation of Ketones and Imines through Dynamic Kinetic Resolution

trans-Diastereoselective Ru(II)-Catalyzed Asymmetric Transfer Hydrogenation of α-Acetamido Benzocyclic Ketones via Dynamic Kinetic Resolution

Rhodium-mediated asymmetric transfer hydrogenation: a diastereo- and enantioselective synthesis of syn-α-amido β-hydroxy esters

Highly Enantioselective Synthesis of syn-β-Hydroxy α-Dibenzylamino Esters via DKR Asymmetric Transfer Hydrogenation and Gram-Scale Preparation of Droxidopa

The present invention relates to a sacubitril intermediate and a preparation method thereof, the sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound; In addition, the intermediate can be used as a raw material to synthesize sacubitril The method disclosed herein has advantages of easily obtained raw materials, simple preparation process, low cost and environment friendly, and so on, which is very suitable for industrial production

Sacubitril intermediate and preparation method thereof

The invention provides a novel intermediate with the structure represented by formula (IV), and its preparation method, and also provides an improved method for preparing besifloxacin hydrochloride (I). The method for preparing besifloxacin hydrochloride (I) comprises the following steps: carrying out a reaction on a compound represented by formula (II), a compound represented by formula (III) and a salt of the compound represented by formula (III) in a lower boiling point solvent in the presence of an alkaline reagent at a relatively low temperature, adding an organic solution of hydrochloric acid or hydrochloric acid after the reaction, and stirring. The preparation methods have the advantages of simple operation, low reaction temperature and less energy consumption.

Preparation method of fluoroquinolone antibiosis medicine

Handle everyday research tasks with reliable, citation-backed results

Your personal Research Agent to handle research tasks with citation-backed results

Popular Tasks used by Researchers

How can I help with your research?

Meet SciSpace

Get more enhanced response by uploading the PDFs you want me to reference.

No relevant PDFs in your library

SciSpace is the AI research assistant for academics. Run systematic literature reviews on 280M+ papers, and write papers with cited sources. Trusted by 1M+ students, PhDs & researchers.

SciSpace | AI for Research

Analyze PDFs

Code & Manuscripts

Funding & Grants

Literature & Patents

Medical & Clinical Data

Systematic Review

Visualize & Present

Web & Data

Build a Google Scholar-like website for your research.

Build a website

Create charts and images for your research

Create a Chart

Write a paper for submission to a journal

Draft a manuscript

Patent Search

Design eye-catching scientific posters in minutes.

Scientific Poster Generation

Systematic Literature Review

One task is running at the moment. Your messages will be shown right after.

Drag and drop or click here to browse

Loved by <highlight>1 million+</highlight> researchers

Extract a list of specific topics and their sources from unstructured text

Topics

Compare and analyze relevant papers that matches with your search

Papers

Get insights from PDFs and bookmarked papers from your library

My library

Recent searches

Try searching for:

Catch AI-generated content in scholarly and non-scholarly content

{ai} Detector

Ai Writer

Get PDF Summaries, highlighted text explanations 

Chat with PDF

Effortlessly create in-text citations and bibliographies in APA and 2,500 other formats

Citation generator

Get explanations, summaries, and answers on academic papers

Ease up your research workflow with {scispace}'s cohort of exciting AI tools

Elevate your academic writing skills and convey your ideas the way you want

Paraphraser

Explore our range of reading and writing tools

Your file is being prepared and should be ready in a few minutes. If it's a large file, it might take a bit longer. You can close this window, and we'll email you the file when it's done.

You have reached a maximum limit of <strong>{limit}</strong> columns in the table. Remove at least <strong>1</strong> column to add or create another one.

Chen Lei

Author Tools

Chat about Author

Papers

Highly Enantioselective Synthesis of syn-β-Hydroxy α-Dibenzylamino Esters via DKR Asymmetric Transfer Hydrogenation and Gram-Scale Preparation of Droxidopa

Sacubitril intermediate and preparation method thereof

Preparation method of fluoroquinolone antibiosis medicine