---
OA_place: publisher
OA_type: hybrid
_id: '22370'
abstract:
- lang: eng
  text: We report a unified method for the synthesis of α-polyhalomethyl amines from
    alkenes and alkynes, enabled by readily available hemiaminal reagents. This operationally
    simple transformation allows for the introduction of not only well-established
    CF3 and CF2H groups, but also the synthetically (and medicinally) underexplored
    CF2Cl and CFClH motifs—thereby broadening access to previously inaccessible chemical
    space of halogenated amine scaffolds. The method displays broad substrate scope
    and functional-group tolerance while operating under mild conditions. Late-stage
    functionalization of drug-like derivatives of Oxaprozin, Erlotinib, and Ibuprofen
    (among others) is reported.
acknowledgement: "Funded by the European Union (ERC, C-HANCE, 101142915 to N.M.).
  Views and opinions expressed are, however, those of the author(s) only and do not
  necessarily reflect those of the European Union or the European Research Council.
  This research was funded in full or in part by the Austrian Science Fund (FWF, 10.55776/P37182
  to N.M.). The technical staff of the NMR Centre of the Faculty of Chemistry (University
  of Vienna) are acknowledged for crucial NMR measurements and expert advice with
  spectral analysis. The authors thank the Core Facility Crystal Structure Analysis
  (U. Vienna) for determination of the crystal structures. The authors are also grateful
  to the University of Vienna for its continued support of our research programs.\r\n\r\nOpen
  Access funding provided by Universität Wien."
article_number: e1233707
article_processing_charge: Yes (via OA deal)
article_type: original
author:
- first_name: Angela K.
  full_name: Hofmeister, Angela K.
  last_name: Hofmeister
- first_name: Giulia
  full_name: Iannelli, Giulia
  last_name: Iannelli
- first_name: Péter
  full_name: Angyal, Péter
  last_name: Angyal
- first_name: Augustin
  full_name: Malandain, Augustin
  last_name: Malandain
- first_name: Daniel
  full_name: Kaiser, Daniel
  last_name: Kaiser
- first_name: Boris
  full_name: Maryasin, Boris
  last_name: Maryasin
- first_name: Hanspeter
  full_name: Kählig, Hanspeter
  last_name: Kählig
- first_name: Matteo
  full_name: Barel, Matteo
  id: 8959927b-2236-11ed-bd6e-ea83d94ade0e
  last_name: Barel
- first_name: Gaia
  full_name: Novarino, Gaia
  id: 3E57A680-F248-11E8-B48F-1D18A9856A87
  last_name: Novarino
  orcid: 0000-0002-7673-7178
- first_name: Nuno
  full_name: Maulide, Nuno
  last_name: Maulide
citation:
  ama: Hofmeister AK, Iannelli G, Angyal P, et al. Unified synthesis of unconventional
    α-polyhalogenated amines through hydroaminoalkylation. <i>Angewandte Chemie International
    Edition</i>. 2026. doi:<a href="https://doi.org/10.1002/anie.1233707">10.1002/anie.1233707</a>
  apa: Hofmeister, A. K., Iannelli, G., Angyal, P., Malandain, A., Kaiser, D., Maryasin,
    B., … Maulide, N. (2026). Unified synthesis of unconventional α-polyhalogenated
    amines through hydroaminoalkylation. <i>Angewandte Chemie International Edition</i>.
    Wiley. <a href="https://doi.org/10.1002/anie.1233707">https://doi.org/10.1002/anie.1233707</a>
  chicago: Hofmeister, Angela K., Giulia Iannelli, Péter Angyal, Augustin Malandain,
    Daniel Kaiser, Boris Maryasin, Hanspeter Kählig, Matteo Barel, Gaia Novarino,
    and Nuno Maulide. “Unified Synthesis of Unconventional α-Polyhalogenated Amines
    through Hydroaminoalkylation.” <i>Angewandte Chemie International Edition</i>.
    Wiley, 2026. <a href="https://doi.org/10.1002/anie.1233707">https://doi.org/10.1002/anie.1233707</a>.
  ieee: A. K. Hofmeister <i>et al.</i>, “Unified synthesis of unconventional α-polyhalogenated
    amines through hydroaminoalkylation,” <i>Angewandte Chemie International Edition</i>.
    Wiley, 2026.
  ista: Hofmeister AK, Iannelli G, Angyal P, Malandain A, Kaiser D, Maryasin B, Kählig
    H, Barel M, Novarino G, Maulide N. 2026. Unified synthesis of unconventional α-polyhalogenated
    amines through hydroaminoalkylation. Angewandte Chemie International Edition.,
    e1233707.
  mla: Hofmeister, Angela K., et al. “Unified Synthesis of Unconventional α-Polyhalogenated
    Amines through Hydroaminoalkylation.” <i>Angewandte Chemie International Edition</i>,
    e1233707, Wiley, 2026, doi:<a href="https://doi.org/10.1002/anie.1233707">10.1002/anie.1233707</a>.
  short: A.K. Hofmeister, G. Iannelli, P. Angyal, A. Malandain, D. Kaiser, B. Maryasin,
    H. Kählig, M. Barel, G. Novarino, N. Maulide, Angewandte Chemie International
    Edition (2026).
das_tickbox: '1'
dataavailabilitystatement: The data that supports the findings of this study are available
  in the supplementary material of this article.
date_created: 2026-07-19T22:01:48Z
date_published: 2026-07-10T00:00:00Z
date_updated: 2026-07-21T07:19:26Z
day: '10'
ddc:
- '570'
- '540'
department:
- _id: GaNo
- _id: GradSch
doi: 10.1002/anie.1233707
external_id:
  pmid:
  - '42429166'
has_accepted_license: '1'
language:
- iso: eng
month: '07'
oa_version: Published Version
pmid: 1
publication: Angewandte Chemie International Edition
publication_identifier:
  eissn:
  - 1521-3773
  issn:
  - 1433-7851
publication_status: epub_ahead
publisher: Wiley
quality_controlled: '1'
researchdata_availability: no
scopus_import: '1'
status: public
supplementarymaterial: yes
title: Unified synthesis of unconventional α-polyhalogenated amines through hydroaminoalkylation
tmp:
  image: /images/cc_by.png
  legal_code_url: https://creativecommons.org/licenses/by/4.0/legalcode
  name: Creative Commons Attribution 4.0 International Public License (CC-BY 4.0)
  short: CC BY (4.0)
type: journal_article
user_id: 2DF688A6-F248-11E8-B48F-1D18A9856A87
year: '2026'
...