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.

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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

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article

DirectMultiStep: Direct Route Generation for Multistep Retrosynthesis

Yu Shee, Haote Li, Anton Morgunov, Víctor S. Batista
8 citations
Journal of Chemical Information and Modeling
Genomics and Phylogenetic Studies
6.45
article

DirectMultiStep: Direct Route Generation for Multistep Retrosynthesis

Yu Shee, Haote Li, Anton Morgunov, Víctor S. Batista
article en
8 citations

Abstract

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.

Journal of Chemical Information and ModelingVol. 65(8)
Yale University (US)
Division of Chemistry
Openalex Percentile: Top 3%
Genomics and Phylogenetic Studies
6.45
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