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Efinaconazole

CAT#: H 314247

CAS#: 164650-44-6

Description: Efinaconazole is a triazole antifungal. It is approved for use in Canada and the USA as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nail). Efinaconazole acts as a 14α-demethylase inhibitor. Efinaconazole inhibits fungal lanosterol 14α-demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes. Efinaconazole has been shown to be active against isolates of the following microorganisms, both in vitro and in clinical infections. Efinaconazole exhibits in vitro minimum inhibitory concentrations (MICs) of 0.06 μg/mL or less against most ( ≥ 90%) isolates of the following microorganisms: Trichophyton rubrum; Trichophyton mentagrophytes.

Synthetic Routes

Efinaconazole - Synthetic Route 1

Synthetic reference

Tamura, Keiji; Kumagai, Naoya; Shibasaki, Masakatsu. An Enantioselective Synthesis of the Key Intermediate for Triazole Antifungal Agents; Application to the Catalytic Asymmetric Synthesis of Efinaconazole (Jublia). ournal of Organic Chemistry. Volume 79. Issue 7. Pages 3272-3278. Journal; Online Computer File. (2014).

Efinaconazole - Synthetic Route 2

Synthetic reference

Karasawa, Tomoya; Oriez, Raphael; Kumagai, Naoya; Shibasaki, Masakatsu. anti-Selective Catalytic Asymmetric Nitroaldol Reaction of α-Keto Esters: Intriguing Solvent Effect, Flow Reaction, and Synthesis of Active Pharmaceutical Ingredients. Journal of the American Chemical Society. Volume 140. Issue 38. Pages 12290-12295. Journal; Online Computer File. (2018).

Efinaconazole - Synthetic Route 3

Synthetic reference

Ren, Wei. Method for preparing efinaconazole. CN 108383829. (2018).

Efinaconazole - Synthetic Route 4

Synthetic reference

Bertolini, Giorgio; Colli, Corrado; Sada, Mara; Colombo, Federica. Process for preparing intermediates useful in the synthesis of antifungal drugs. Assignee Olon S.p.A., Italy. WO 2017178909. (2017).

Efinaconazole - Synthetic Route 5

Synthetic reference

Wei, Yanjun; Jiang, Xianlong; Xing, Yanping. Preparation method of efinaconazole intermediate. Assignee Viwit Pharmaceutical Co., Ltd., Peop. Rep. China; Viwit Pharmaceuticals Ltd. CN 106608854. (2017).

Efinaconazole - Synthetic Route 6

Synthetic reference

Gopin, Anna; Rubnov, Shai; Zats, Galina; Marom, Ehud. Intermediate compounds and process for the preparation of efinaconazole. Assignee Mapi Pharma Ltd., Israel. WO 2016079728. (2016).

Efinaconazole - Synthetic Route 7

Synthetic reference

Wang, Hailong; Sun, Guodong; Zhang, Dexi. Process for preparation of Efinaconazole and intermediates thereof. Assignee Ruyuan Yao Autonomous County Dazhong Pharmaceutical Trading Co., Ltd., Peop. Rep. China. CN 105503826. (2016).

Efinaconazole - Synthetic Route 8

Synthetic reference

Bao, Jinyuan; Huang, Yange; Ding, Wei; Jiang, Yuwei; Zhang, Xiaoqing. Synthetic method of efinaconazole and intermediate thereof. Assignee Nanjing Huawei Pharmaceutical Science and Technology Development Co., Ltd., Peop. Rep. China. CN 104292214. (2015).