Development of Practical and Scalable Synthetic Route for 1-(2,2,2-Trifluoroethyl)cyclopropane-1-carboxylic Acid

Organic Process Research & Development 2026

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Authors: Sukhen Karmakar, Rajaram Ayothiraman, Sundar Nandhagopal, Zulelal Dolas, Arundutt Silamkoti, Alla Venu, Srinivasarao Jami, Arvind Venkataramani, Thirumalai Lakshminarasimhan, Sabuj Mukherjee, Anuradha Gupta, Arvind Mathur
+4 more Jeishla L. M. Matos, Ian Charles Hale, Martin D. Eastgate, Francisco González‐Bobes
DOI: 10.1021/acs.oprd.5c00371
Cited by: 0
References: 33

Abstract

An efficient, scalable, and safe synthesis of 1-(2,2,2-trifluoroethyl)cyclopropane-1-carboxylic acid (compound 1 ) was developed, starting from the inexpensive and readily available trifluoro-iodopropane 18 . This was accomplished through detailed optimization of the conditions for the key Simmons–Smith cyclopropanation reaction. The optimized process was used to prepare multi-kilograms of this intermediate, supporting early development activities of a pharmaceutical candidate.

Fields of Study & Subjects

Cyclopropane Reaction Mechanisms Asymmetric Synthesis and Catalysis Synthetic Organic Chemistry Methods

Publication details

Journal / source
Organic Process Research & Development
Volume
30
Issue
1
Pages
155–163
Publication date
5 January 2026
Language
EN