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This content will become publicly available on July 1, 2026

Title: N-Alkylation by Hydrogen Borrowing: Pharmaceutical Applications and Comparison to Other Methods
Formation of C-N bonds is a quintessential transformation in organic synthesis. Among the various methods to access them, hydrogen borrowing catalysis offers a green, atom economical, and cost-effective approach with water as the sole by-product. In this reaction, amines are alkylated with alcohol coupling partners in the presence of a transition metal catalyst. Several catalytic systems have been developed and employed in the synthesis of pharmaceutical intermediates and complex natural products, replacing conventional amination reactions with hydrogen borrowing reactions that deliver improved selectivity and yield. In this short review, we compare hydrogen borrowing N-alkylation with other classical and modern C-N bond forming reactions and discuss applications in pharmaceutical synthesis.  more » « less
Award ID(s):
1856395
PAR ID:
10617643
Author(s) / Creator(s):
;
Publisher / Repository:
Thieme
Date Published:
Journal Name:
Synthesis
ISSN:
0039-7881
Subject(s) / Keyword(s):
N-alkylation hydrogen borrowing amine alkylation C-N bond formation natural products pharmaceutical intermediates catalysis
Format(s):
Medium: X
Sponsoring Org:
National Science Foundation
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