{
  "abstract": "*Email: nowmiracle@zjnu.edu.cn; dengwp827@zjnu.edu.cn ABSTRACT: Pyrazines and piperazines are privileged 1,4-diaza motifs, yet neither combines conformational rigidity with a stereochemically defined three-dimensional shape. Here we report the first catalytic enantioselective formal (3 + 3) cycloaddition of 1-azabicyclo[1.1.0]butanes (ABBs), providing direct access to enantioenriched 1,4diazabicyclo[3.1.1]heptanes—rigid, C(sp3)-rich scaffolds that serve as chiral three-dimensional complements to these classical motifs. Relay Dy/Ir catalysis merges Dy(OTf)3-promoted ABB strain release with iridium-catalyzed asymmetric allylic amination of allylamine-derived N,C,C synthons, extending ABB chemistry beyond conventional strain-release functionalization and previously reported racemic cycloadditions. The method furnishes 50 examples in up to 93% yield and 99% ee, with broad functional-group tolerance and compatibility with drug- and natural-product-derived substrates. Control experiments, 1H NMR studies, and DFT calculations support a staged mechanism involving carbonyl-assisted N,O-bidentate activation of the ABB by Dy(OTf)3. Preparative-scale synthesis, orthogonal product diversification, and access to pyrazineand piperazine-related drug analogues demonstrate the synthetic versatility and scaffold-hopping potential of this platform.",
  "abstract_shown": true,
  "affiliations": [],
  "article_type": null,
  "arxiv": null,
  "author_total": 5,
  "authors": [
    {
      "name": "Jun-Cheng Jin"
    },
    {
      "name": "Jian Zhang",
      "orcid": "0009-0006-1201-5228"
    },
    {
      "name": "Qi-Guo Zheng"
    },
    {
      "name": "Hanliang Zheng"
    },
    {
      "name": "Wei-Ping Deng"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/31ntz40ae6dte.bib",
  "cited_by": 0,
  "doi": "10.26434/chemrxiv.15009675/v1",
  "fulltext_url": null,
  "id": "31ntz40ae6dte",
  "issns": [],
  "landing_url": "https://chemrxiv.org/doi/full/10.26434/chemrxiv.15009675/v1",
  "language": null,
  "licence": "CC-BY",
  "licence_label": "CC BY",
  "licence_source": "journal",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "openalex",
      "1605|Asymmetric Synthesis and Catalysis"
    ]
  ],
  "openalex": "W7214931735",
  "pdf_url": "https://chemrxiv.org/doi/pdf/10.26434/chemrxiv.15009675/v1",
  "pmcid": null,
  "pmid": null,
  "published": "2026-09-29",
  "publisher": "American Chemical Society (ACS)",
  "ris": "https://research.draconitic.com/paper/31ntz40ae6dte.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:17:21Z",
      "native_id": "10.26434/chemrxiv.15009675",
      "source": "chemrxiv",
      "url": "https://chemrxiv.org/doi/full/10.26434/chemrxiv.15009675/v1"
    }
  ],
  "subjects": [
    {
      "field": "chemistry",
      "origin": "openalex:1605|Asymmetric Synthesis and Catalysis",
      "subfield": "organic"
    }
  ],
  "title": "Enantioselective Strain-Release Formal (3 + 3) Cycloaddition of 1-Azabicyclo[1.1.0]butanes to Chiral 1,4-Diazabicyclo[3.1.1]heptanes via Relay Dy/Ir Catalysis",
  "title_text": "Enantioselective Strain-Release Formal (3 + 3) Cycloaddition of 1-Azabicyclo[1.1.0]butanes to Chiral 1,4-Diazabicyclo[3.1.1]heptanes via Relay Dy/Ir Catalysis",
  "type": "preprint",
  "updated_at": "2026-10-30T12:17:21Z",
  "url": "https://research.draconitic.com/paper/31ntz40ae6dte",
  "venue": "ChemRxiv",
  "versions": []
}