On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin

MedChemComm ◽  
2013 ◽  
Vol 4 (1) ◽  
pp. 101-111 ◽  
Author(s):  
Vincent Mascitti ◽  
Benjamin A. Thuma ◽  
Aaron C. Smith ◽  
Ralph P. Robinson ◽  
Thomas Brandt ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Drug Discovery ◽  
Organic Synthesis ◽  
Medicinal Chemistry ◽  
Critical Role ◽  
Antidiabetic Agent ◽  
Synthetic Organic Chemistry

The discovery of antidiabetic agent ertugliflozin is described. In this article, emphasis is placed on the critical role that organic synthesis played in influencing our medicinal chemistry strategy.

Ethenesulfonyl Fluoride (ESF) and Its Derivatives in SuFEx Click Chemistry and More

Synthesis ◽  
2019 ◽  
Vol 52 (05) ◽  
pp. 673-687 ◽  
Author(s):  
Yan-Ping Meng ◽  
Shi-Meng Wang ◽  
Wan-Yin Fang ◽  
Zhi-Zhong Xie ◽  
Jing Leng ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Click Chemistry ◽  
Exchange Reaction ◽  
Organic Synthesis ◽  
Medicinal Chemistry ◽  
Materials Science ◽  
Click Reaction ◽  
Chemical Properties ◽  
Chemical Transformations ◽  
Absolute Reliability

The sulfur(VI) fluoride exchange reaction (SuFEx), developed by Sharpless and co-workers in 2014, is a new category of click reaction that creates molecular connections with absolute reliability and unprecedented efficiency through a sulfur(VI) hub. Ethenesulfonyl fluoride (ESF), as one of the most important sulfur(VI) hubs, exhibits extraordinary reactivity in SuFEx click chemistry and organic synthesis. This review summarizes the chemical properties and applications of ESF in click chemistry, organic chemistry, materials science, medicinal chemistry and in many other fields related to organic synthesis.1 Introduction2 Chemical Transformations of ESF3 Chemical Transformations of 2-Arylethenesulfonyl Fluorides4 Novel SuFEx Reagents Derived from ESF5 Applications of ESF Derivatives in Medicinal Chemistry6 Applications of ESF Derivatives in Materials Science7 Conclusion

scholarly journals Electrocatalysis as an enabling technology for organic synthesis

2021 ◽  
Author(s):  
Luiz F. T. Novaes ◽  
Jinjian Liu ◽  
Yifan Shen ◽  
Lingxiang Lu ◽  
Jonathan M. Meinhardt ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Organic Synthesis ◽  
Enabling Technology ◽  
Synthetic Organic Chemistry

Electrochemistry has recently gained increased attention as a versatile strategy for achieving challenging transformations at the forefront of synthetic organic chemistry.

Triflic Anhydride (Tf2O)-Activated Transformation of Amides, Sulfoxides and Phosphorus Oxides via Nucleophilic Trapping

Synthesis ◽  
2021 ◽  
Author(s):  
Hai Huang ◽  
Jun Yong Kang
Keyword(s):  
Organic Chemistry ◽  
Organic Synthesis ◽  
Phosphorus Oxide ◽  
Synthetic Organic Chemistry ◽  
The Past ◽  
Mechanistic Pathway ◽  
Trifluoromethanesulfonic Anhydride ◽  
Wide Range ◽  
Electrophilic Activation ◽  
Nucleophilic Trapping

Trifluoromethanesulfonic anhydride (Tf2O) has found a wide range of applications in synthetic organic chemistry as a strong electrophilic activator leading to the transient generation of a triflate intermediate. This versatile triflate intermediate undergoes nucleophilic trapping with diverse nucleophiles to yield novel compounds. In this review, we describe the features and applications of triflic anhydride in organic synthesis reported in the past decade, especially in amide, sulfoxide, and phosphorus oxide chemistry through electrophilic activation. A plausible mechanistic pathway of each important reaction is also discussed.

scholarly journals Fragment-based drug discovery: opportunities for organic synthesis

2021 ◽  
Author(s):  
Jeffrey D. St. Denis ◽  
Richard J. Hall ◽  
Christopher W. Murray ◽  
Tom D. Heightman ◽  
David C. Rees
Keyword(s):  
Organic Chemistry ◽  
Drug Discovery ◽  
Organic Synthesis ◽  
Fragment Based Drug Discovery

Herein is described the concept of fragment sociability and the opportunities for organic chemistry to address the challenges of fragment elaboration.

scholarly journals Application of Complexes of Group 13 Elements in Synthetic Organic Chemistry for Activation of Carbonyl Compounds

Vestnik RFFI ◽  
2019 ◽  
pp. 113-140
Author(s):  
Roman A. Novikov ◽  
Yury V. Tomilov
Keyword(s):  
Organic Chemistry ◽  
Coordination Chemistry ◽  
Organic Synthesis ◽  
Carbonyl Compounds ◽  
Group 13 ◽  
New Era ◽  
Synthetic Organic Chemistry ◽  
Main Emphasis ◽  
New Compounds

The main aspects of modern organic chemistry of the Group 13 elements – aluminum (Al), gallium (Ga), indium (In), and thallium (Tl) – are considered. Herewith, the main emphasis is placed on their use for the various carbonyl compounds activation in organic synthesis and reactions, which are specific for these elements. The 21th century marked a new era in the development of chemistry of the Group 13 elements; it is connected with the discovery of surprising and unexpected reactions and new compounds (primarily in the area of organic and coordination chemistry), defining various fields of these elements application.

scholarly journals Copper-boryl mediated organic synthesis

2018 ◽  
Vol 47 (19) ◽  
pp. 7477-7494 ◽  
Author(s):  
David Hemming ◽  
Russell Fritzemeier ◽  
Stephen A. Westcott ◽  
Webster L. Santos ◽  
Patrick G. Steel
Keyword(s):  
Organic Chemistry ◽  
Organic Synthesis ◽  
Synthetic Organic Chemistry

The diverse applications of copper-catalyzed borylation, which has become an essential strategy in modern synthetic organic chemistry, are reviewed and illustrated.

scholarly journals Synthesis of spirocyclic scaffolds using hypervalent iodine reagents

2018 ◽  
Vol 14 ◽  
pp. 1778-1805 ◽  
Author(s):  
Fateh V Singh ◽  
Priyanka B Kole ◽  
Saeesh R Mangaonkar ◽  
Samata E Shetgaonkar
Keyword(s):  
Organic Chemistry ◽  
Heavy Metals ◽  
Natural Product ◽  
Organic Synthesis ◽  
Stereoselective Synthesis ◽  
Natural Product Synthesis ◽  
Hypervalent Iodine ◽  
Toxic Heavy Metals ◽  
Synthetic Organic Chemistry ◽  
The Past

Hypervalent iodine reagents have been developed as highly valuable reagents in synthetic organic chemistry during the past few decades. These reagents have been identified as key replacements of various toxic heavy metals in organic synthesis. Various synthetically and biologically important scaffolds have been developed using hypervalent iodine reagents either in stoichiometric or catalytic amounts. In addition, hypervalent iodine reagents have been employed for the synthesis of spirocyclic scaffolds via dearomatization processes. In this review, various approaches for the synthesis of spirocyclic scaffolds using hypervalent iodine reagents are covered including their stereoselective synthesis. Additionally, the applications of these reagents in natural product synthesis are also covered.

Thieme–IUPAC Prize 2016 Call for Nominations

2015 ◽  
Vol 37 (5-6) ◽  
Keyword(s):  
Organic Chemistry ◽  
Organic Synthesis ◽  
International Union ◽  
Applied Chemistry ◽  
Synthetic Organic Chemistry ◽  
International Conference

Thieme Chemistry, IUPAC, and the Editors of SYNTHESIS, SYNLETT, SYNFACTS, and Science of Synthesis announce the Thieme–IUPAC Prize for 2016. This award is presented every two years on the occasion of the International Union of Pure and Applied Chemistry – International Conference on Organic Synthesis (IUPAC–ICOS). The 2016 ICOS will be held at IIT Bombay in Mumbai, India, 11-16 December 2016. The prize is awarded to a scientist under 40 years of age whose research has had a major impact in synthetic organic chemistry.

scholarly journals Rhodococcus as A Versatile Biocatalyst in Organic Synthesis

2019 ◽  
Vol 20 (19) ◽  
pp. 4787 ◽  
Author(s):  
Busch ◽  
Hagedoorn ◽  
Hanefeld
Keyword(s):  
Organic Chemistry ◽  
Organic Synthesis ◽  
Specific Enzyme ◽  
Close Attention ◽  
Comprehensive Overview ◽  
Whole Cell ◽  
Synthetic Organic Chemistry ◽  
Utilization Potential ◽  
Enzyme Class

The application of purified enzymes as well as whole-cell biocatalysts in synthetic organic chemistry is becoming more and more popular, and both academia and industry are keen on finding and developing novel enzymes capable of performing otherwise impossible or challenging reactions. The diverse genus Rhodococcus offers a multitude of promising enzymes, which therefore makes it one of the key bacterial hosts in many areas of research. This review focused on the broad utilization potential of the genus Rhodococcus in organic chemistry, thereby particularly highlighting the specific enzyme classes exploited and the reactions they catalyze. Additionally, close attention was paid to the substrate scope that each enzyme class covers. Overall, a comprehensive overview of the applicability of the genus Rhodococcus is provided, which puts this versatile microorganism in the spotlight of further research.

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