Synthesis of Siphonazole B Through Domino Cycloisomerization-Oxazolonium Ion Rearrangements
(2025) In Chemistry – A European Journal 31(40). p.202501394-202501394- Abstract
- 4-Alkenyl- and 4-acyloxazoles represent important substructures across a diverse array of bioactive molecules. Practical methods to synthesize these motifs are, therefore, of considerable interest. Here, we develop a novel domino process wherein a cycloisomerization is followed by a 1,2-rearrangement via an oxazolonium ion to yield 4-alkenyloxazoles from an abundant β-chloro-N-benzyl propargylamine and acyl chlorides. The synthetic utility of the method is highlighted by its application to both oxazole units of siphonazole B, leading to a concise convergent total synthesis of this natural product. © 2025 The Author(s). Chemistry – A European Journal published by Wiley-VCH GmbH.
- Abstract (Swedish)
- Abstract 4-Alkenyl- and 4-acyloxazoles represent important substructures across a diverse array of bioactive molecules. Practical methods to synthesize these motifs are, therefore, of considerable interest. Here, we develop a novel domino process wherein a cycloisomerization is followed by a 1,2-rearrangement via an oxazolonium ion to yield 4-alkenyloxazoles from an abundant β-chloro-N-benzyl propargylamine and acyl chlorides. The synthetic utility of the method is highlighted by its application to both oxazole units of siphonazole B, leading to a concise convergent total synthesis of this natural product.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/84e11b1a-cdbb-4cd4-8ae2-d0122bdd3be3
- author
- Paulsen, Filip
LU
; Clementson, Sebastian
LU
; von Wachenfeldt, Henrik LU ; Antoszczak, Michał ; Fridolf, Simon LU and Strand, Daniel LU
- organization
- publishing date
- 2025
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- domino reactions, natural product synthesis, oxidative amidation, rearrangements
- in
- Chemistry – A European Journal
- volume
- 31
- issue
- 40
- pages
- 202501394 - 202501394
- publisher
- Wiley-Blackwell
- external identifiers
-
- pmid:40536015
- scopus:105009212201
- DOI
- 10.1002/chem.202501394
- language
- English
- LU publication?
- yes
- id
- 84e11b1a-cdbb-4cd4-8ae2-d0122bdd3be3
- date added to LUP
- 2025-08-06 19:49:00
- date last changed
- 2025-08-18 09:06:21
@article{84e11b1a-cdbb-4cd4-8ae2-d0122bdd3be3, abstract = {{4-Alkenyl- and 4-acyloxazoles represent important substructures across a diverse array of bioactive molecules. Practical methods to synthesize these motifs are, therefore, of considerable interest. Here, we develop a novel domino process wherein a cycloisomerization is followed by a 1,2-rearrangement via an oxazolonium ion to yield 4-alkenyloxazoles from an abundant β-chloro-N-benzyl propargylamine and acyl chlorides. The synthetic utility of the method is highlighted by its application to both oxazole units of siphonazole B, leading to a concise convergent total synthesis of this natural product. © 2025 The Author(s). Chemistry – A European Journal published by Wiley-VCH GmbH.}}, author = {{Paulsen, Filip and Clementson, Sebastian and von Wachenfeldt, Henrik and Antoszczak, Michał and Fridolf, Simon and Strand, Daniel}}, keywords = {{domino reactions; natural product synthesis; oxidative amidation; rearrangements}}, language = {{eng}}, number = {{40}}, pages = {{202501394--202501394}}, publisher = {{Wiley-Blackwell}}, series = {{Chemistry – A European Journal}}, title = {{Synthesis of Siphonazole B Through Domino Cycloisomerization-Oxazolonium Ion Rearrangements}}, url = {{http://dx.doi.org/10.1002/chem.202501394}}, doi = {{10.1002/chem.202501394}}, volume = {{31}}, year = {{2025}}, }