A5015818002- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- vaccines and immunoinformatics approaches
- Molecular spectroscopy and chirality
- Axial and Atropisomeric Chirality Synthesis
- Computational Drug Discovery Methods
- Asymmetric Synthesis and Catalysis
- SARS-CoV-2 and COVID-19 Research
- Bacterial Genetics and Biotechnology
- Oral microbiology and periodontitis research
- Cyclization and Aryne Chemistry
- Innovative Microfluidic and Catalytic Techniques Innovation
- Medical Research and Treatments
- Quinazolinone synthesis and applications
- Diverse Scientific Research Studies
- Pediatric health and respiratory diseases
- Algebraic structures and combinatorial models
- Cyclopropane Reaction Mechanisms
- Catalytic C–H Functionalization Methods
- Chemical synthesis and alkaloids
- Bacterial biofilms and quorum sensing
Futaba (Japan)
2022-2023
Shionogi (Japan)
2022-2023
Kyoto University Institute for Chemical Research
2016-2017
Kyoto University
2016-2017
Kyoto Bunkyo University
2016-2017
Kyoto Pharmaceutical University
2016
Instituto de Investigaciones Químicas
2016
Osaka Prefecture University
2012
The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome 2 (SARS-CoV-2), has resulted in millions of deaths and threatens public health safety. Despite the rapid global spread COVID-19 vaccines, effective oral antiviral drugs are urgently needed. Here, we describe discovery S-217622, first noncovalent, nonpeptidic SARS-CoV-2 3CL protease inhibitor clinical candidate. S-217622 was discovered via virtual screening followed biological an in-house compound...
Abstract The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome 2 (SARS-CoV-2), has resulted in millions of deaths and threatens public health safety. Despite the rapid global spread COVID-19 vaccines, effective oral antiviral drugs are urgently needed. Here, we describe discovery S-217622, first non-covalent, non-peptidic SARS-CoV-2 3CL protease inhibitor clinical candidate. S-217622 was discovered via virtual screening followed biological an in-house...
We describe the development of practical manufacturing Ensitrelvir, which was discovered as a SARS-CoV-2 antiviral candidate. Scalable synthetic methods indazole, 1,2,4-triazole and 1,3,5-triazinone structures were established, convergent couplings these fragments enabled concise efficient scale-up process to Ensitrelvir. In this process, introducing meta-cresolyl moiety successfully enhanced stability intermediates. Compared initial route at early research stage, overall yield longest...
Ensitrelvir, SARS-CoV-2 3CL protease inhibitor, has been discovered for the treatment of coronavirus disease 2019 (COVID-19). Ensitrelvir is structurally composed from three main units, which are indazole unit, triazole unit and triazinone unit. Synthetic strategies where these units employed at latter steps in synthesis made it possible to construct a highly productive convergent route. In addition, lean manufacturing process was also established through optimization based on SELECT...
A method for asymmetric α-arylation of α-amino acid derivatives via memory chirality has been developed. Addition axially chiral enolates, generated from derivatives, to in situ arynes, followed by intramolecular C-acylation the resulting aryl metallic species, gave benzocyclobutenones with a tetrasubstituted carbon retention configuration up 99% ee.
Enantioselective intramolecular conjugate addition reactions of short-lived C-O axially chiral enolates have been developed. The proceeded with inversion the configuration and provided dihydrobenzofurans contiguous tetra- trisubstituted carbon centers in up to 96% enantiomeric excess (ee).
We describe the development of practical manufacturing Ensitrelvir, which was discovered as a SARS-CoV-2 antiviral candidate. Scalable synthetic methods indazole, 1,2,4-triazole and 1,3,5-triazinone structures were established, convergent couplings these fragments enabled concise efficient scale-up process to Ensitrelvir. In this process, introducing meta-cresolyl moiety successfully enhanced stability intermediates. Compared initial route in medicinal stage, overall yield longest linear...
Recently, the direct functionalization of unactivated C(sp3)-H bonds have been well developed. Despite their numerous efforts, controlling site-selectivity in these transformations is still challenging because a multitude C-H has close dissociation energies. In this mini-review, successful examples to control C(sp3)-activation reaction by changing reagents or catalysts described.
Abstract The products are formed with high diastereomeric and enantiomeric excesses.