Total synthesis: an enabling science

  1. editorImage
  1. Editor: Prof. Bastien Nay
    École Polytechnique

This thematic issue focuses on total synthesis as an enabling science. Total synthesis is the science of constructing molecules from simple starting materials and often deals with complex architectures that require a retrosynthetic problem-solving analysis. Total synthesis and the discovery of original synthetic methodologies have always been intimately linked. Old and recent achievements show that connections to other disciplines are important to the success of total synthesis and can be a source of new discoveries. Indeed, as a science allowing the preparation of useful functional compounds, it is strongly connected to biological and medicinal studies, while the development of natural-product-based tools for chemical biology often requires the construction of complex molecules (biology-driven total synthesis). Incidentally, the term "total synthesis" is not limited to natural products but also, sometimes, involves complex drugs. Furthermore, it is possible to test biosynthetic hypotheses concerning natural products through synthetic approaches (biomimetic synthesis). In addition, total syntheses have also been achieved with enzymes, strengthening the links to biology.

Total synthesis is not limited to academic laboratories but rather also pursued in industry, where a particular efficiency and economy of tasks is paramount. This requires permanent technological progress. Thus, the recent boom of machine learning and computational chemistry for retrosynthetic analyses and beyond foreshadows a renew interests to harvest increasingly complex synthetic strategies for industrial processes. In terms of discoveries in organic chemistry, total synthesis is a fruitful feed, and serendipity has well been exploited. Even dead ends, yet always heartbreaking for synthetic chemists, still provide a wealth of useful information for the chemical community. Finally, this is not to forget that organic chemistry, which is above all an experimental science, is performed daily by researchers in the laboratory, and some of these life stories can be truly inspiring to current and future generations. This thematic issue anticipates articles covering any of these remarks in the form of original research papers and reviews. In addition, submissions that highlight key topics and provide accounts and insights, or even biographical articles based on scientific data and/or evidence, are welcome.

Submission deadline: Nov 30, 2022

Synthesis of tryptophan-dehydrobutyrine diketopiperazine and biological activity of hangtaimycin and its co-metabolites

  1. Houchao Xu,
  2. Anne Wochele,
  3. Minghe Luo,
  4. Gregor Schnakenburg,
  5. Yuhui Sun,
  6. Heike Brötz-Oesterhelt and
  7. Jeroen S. Dickschat
  • Letter
  • Published 07 Sep 2022
Graphical Abstract

Beilstein J. Org. Chem. 2022, 18, 1159–1165, doi:10.3762/bjoc.18.120

  • Review
  • Published 15 Sep 2022

  • PDF
Graphical Abstract

Beilstein J. Org. Chem. 2022, 18, 1236–1248, doi:10.3762/bjoc.18.129

Enantioselective total synthesis of putative dihydrorosefuran, a monoterpene with an unique 2,5-dihydrofuran structure

  1. Irene Torres-García,
  2. Josefa L. López-Martínez,
  3. Rocío López-Domene,
  4. Manuel Muñoz-Dorado,
  5. Ignacio Rodríguez-García and
  6. Miriam Álvarez-Corral
  • Full Research Paper
  • Published 19 Sep 2022

  • PDF

  • Supp. Info
Graphical Abstract

Beilstein J. Org. Chem. 2022, 18, 1264–1269, doi:10.3762/bjoc.18.132

  • Full Research Paper
  • Published 04 Oct 2022

  • PDF
Graphical Abstract

Beilstein J. Org. Chem. 2022, 18, 1385–1395, doi:10.3762/bjoc.18.143

Solid-phase total synthesis and structural confirmation of antimicrobial longicatenamide A

  1. Takumi Matsumoto,
  2. Takefumi Kuranaga,
  3. Yuto Taniguchi,
  4. Weicheng Wang and
  5. Hideaki Kakeya
  • Full Research Paper
  • Published 18 Nov 2022
Graphical Abstract

Beilstein J. Org. Chem. 2022, 18, 1560–1566, doi:10.3762/bjoc.18.166

Formal total synthesis of macarpine via a Au(I)-catalyzed 6-endo-dig cycloisomerization strategy

  1. Jiayue Fu,
  2. Bingbing Li,
  3. Zefang Zhou,
  4. Maosheng Cheng,
  5. Lu Yang and
  6. Yongxiang Liu
  • Letter
  • Published 23 Nov 2022
Graphical Abstract

Beilstein J. Org. Chem. 2022, 18, 1589–1595, doi:10.3762/bjoc.18.169

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