DirectMultiStep: Direct Route Generation for Multistep Retrosynthesis
Traditional computer-aided synthesis planning (CASP) methods rely on iterative single-step predictions, leading to exponential search space growth that limits efficiency and scalability. We introduce a series of transformer-based models that leverage a mixture of experts approach to directly generate multistep synthetic routes as a single string, conditionally predicting each transformation based on all preceding ones. Our DMS Explorer XL model, which requires only target compounds as input, outperforms state-of-the-art methods on the PaRoutes dataset with 1.9x and 3.1x improvements in Top-1 accuracy on the n<sub>1</sub> and n<sub>5</sub> test sets, respectively. Providing additional information, such as the desired number of steps and starting materials, enables both a reduction in model size and an increase in accuracy, highlighting the benefits of incorporating more constraints into the prediction process. The top-performing DMS-Flex (Duo) model scores 25-50% higher on Top-1 and Top-10 accuracies for both n<sub>1</sub> and n<sub>5</sub> sets. Additionally, our models successfully predict routes for the FDA-approved drugs not included in the training data, demonstrating strong generalization capabilities. While the limited diversity of the training set may affect performance on less common reaction types, our multistep-first approach presents a promising direction toward fully automated retrosynthetic planning.
Authors
- Yu Shee (ORCID: https://orcid.org/0000-0002-3728-0021)
- Haote Li (ORCID: https://orcid.org/0000-0002-8146-5066)
- Anton Morgunov (ORCID: https://orcid.org/0009-0004-6245-0354)
- Víctor S. Batista (ORCID: https://orcid.org/0000-0002-3262-1237)
Institutions
- Yale University (US)
Publication Details
- Journal
- Journal of Chemical Information and Modeling
- Published
- 2025-04-08
- DOI
- https://doi.org/10.1021/acs.jcim.4c01982
- Citations
- 8
- Primary Topic
- Genomics and Phylogenetic Studies
- Type
- article
- Field-Weighted Citation Impact
- 6.45
Funders
- Division of Chemistry