The enantioselective total synthesis of ROCK-inhibitor ( S )-Netarsudil (Rhopressa) via asymmetric organocatalysis

The enantioselective total synthesis of ROCK-inhibitor ( S )-Netarsudil (Rhopressa) via asymmetric organocatalysis Full article

Journal

Organic and Biomolecular Chemistry
ISSN: 1477-0520 , E-ISSN: 1477-0539

Output data

Year: 2026, DOI: 10.1039/d5ob01899d

Authors

Kovalevsky Ruslan A. ¹ , Kucherenko Alexander S. ¹ , Zlotin Sergei G. ¹

Affiliations

1	N.D. Zelinsky Institute of Organic Chemistry, Russin Academy of Sciences, 47 Leninsky Prospect, 119991, Moscow, Russian Federation

Funding (1)

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.

Kovalevsky R.A. , Kucherenko A.S. , Zlotin S.G.
The enantioselective total synthesis of ROCK-inhibitor ( S )-Netarsudil (Rhopressa) via asymmetric organocatalysis
Organic and Biomolecular Chemistry. 2026. DOI: 10.1039/d5ob01899d WOS Scopus OpenAlex

Web of science:	WOS:001666073900001
Scopus:	2-s2.0-105027754207
OpenAlex:	W7118872067

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