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1.
ACS Cent Sci ; 9(4): 836-843, 2023 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-37122445

RESUMO

We describe the development of the practical manufacturing of Ensitrelvir, which was discovered as a SARS-CoV-2 antiviral candidate. Scalable synthetic methods of indazole, 1,2,4-triazole and 1,3,5-triazinone structures were established, and convergent couplings of these fragments enabled the development of a concise and efficient scale-up process to Ensitrelvir. In this process, introducing a meta-cresolyl moiety successfully enhanced the stability of intermediates. Compared to the initial route at the early research and development stage, the overall yield of the longest linear sequence (6 steps) was improved by approximately 7-fold. Furthermore, 9 out of the 12 isolated intermediates were crystallized directly from each reaction mixture without any extractive workup (direct isolation). This led to an efficient and environmentally friendly manufacturing process that minimizes waste of organic solvents, reagents, and processing time. This practical process for manufacturing Ensitrelvir should contribute to protection against COVID-19.

2.
Chem Asian J ; 13(4): 409-412, 2018 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-29327427

RESUMO

Transition-metal-free synthesis of ß-alkoxy monohydroperoxides via aerobic photooxidation using an acridinium photocatalyst was developed. This method enables the synthesis of some novel hydroperoxides. The peroxide source is molecular oxygen, which is cost-effective and atomically efficient. Magnesium oxide plays an important role as a base in the catalytic system.

3.
Org Lett ; 18(1): 8-11, 2016 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-26654114

RESUMO

The intermolecular cyclopropanation of aromatic olefins with activated methylene compounds using iodine and visible light irradiation was described. This reaction proceeds under rare-metal-free conditions. Styrenes with various substituted groups (alkyl and electron-withdrawing groups) provided corresponding cyclopropanes in moderate to good yields.


Assuntos
Carbono/química , Ciclopropanos/química , Iodo/química , Estirenos/química , Catálise , Estrutura Molecular
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