Synthesis of N -Linked Amino-Hexyl Fluorotryptophan for Enlicitide, Part 1: Route Scouting

Organic Process Research & Development 2026

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Authors: Jeffrey T. Kuethe, Byron K. Peters, Keywan A. Johnson, Kai‐Jiong Xiao, Yingju Xu, Stephen M. Dalby, Artis Klapars, Yonghee Lee, Weidong Tong, Erica L. Schwalm, Yongqian Zhang
DOI: 10.1021/acs.oprd.6c00255
Cited by: 1
References: 13

Abstract

Abstract One of the building blocks in the manufacture of the northern macrocycle of enlicitide decanoate is N-linked amino-hexylfluorotryptophan 1. An efficient, scalable, and protecting-group-free synthesis of this key building block is described. Hallmarks of the synthesis include the use of the Delépine reaction to prepare the required alkylating agent and the alkylation of unprotected fluorotryptophan.

Fields of Study & Subjects

Click Chemistry and Applications Chemical Synthesis and Analysis Fluorine in Organic Chemistry

Publication details

Journal / source
Organic Process Research & Development
Publisher
American Chemical Society (ACS)
Volume
30
Issue
9
Pages
2549–2556
Publication date
2 September 2026
Language
EN