The enantioselective total synthesis of ROCK-inhibitor ( S )-Netarsudil (Rhopressa) via asymmetric organocatalysis Full article
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Organic & Biomolecular Chemistry
ISSN: 1477-0520 , E-ISSN: 1477-0539 |
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| Output data | Year: 2026, Volume: 24, Pages: 1137-1142 Pages count : 6 DOI: 10.1039/d5ob01899d | ||
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Funding (1)
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Abstract:
A new efficient and waste-free approach to synthesize (S)-Netarsudil, a blockbuster drug for the treatment of glaucoma and increased intraocular pressure (IOP), has been developed. It is based on the use of terephthalic dialdehyde as a commercially available starting compound and an asymmetric organocatalytic Michael reaction as the key step responsible for the creation of a stereogenic center with the required (S)-configuration. The advantages of the proposed methodology over the currently known one are the higher overall yield of the target drug, use of a reusable organocatalyst, mild and green reaction conditions, and the elimination of labor-intensive and time-consuming stages for the isolation of auxiliary groups.
Cite:
Kovalevsky R.A.
, Kucherenko A.S.
, Zlotin S.G.
The enantioselective total synthesis of ROCK-inhibitor ( S )-Netarsudil (Rhopressa) via asymmetric organocatalysis
Organic & Biomolecular Chemistry. 2026. V.24. P.1137-1142. DOI: 10.1039/d5ob01899d WOS Scopus OpenAlex
The enantioselective total synthesis of ROCK-inhibitor ( S )-Netarsudil (Rhopressa) via asymmetric organocatalysis
Organic & Biomolecular Chemistry. 2026. V.24. P.1137-1142. DOI: 10.1039/d5ob01899d WOS Scopus OpenAlex
Dates:
| Submitted: | Dec 4, 2025 |
| Published online: | Jan 8, 2026 |
Identifiers:
| Web of science: | WOS:001666073900001 |
| Scopus: | 2-s2.0-105027754207 |
| OpenAlex: | W7118872067 |
Citing:
| DB | Citing |
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| Scopus | Нет цитирований |
| OpenAlex | Нет цитирований |