Scalable Diboron-Catalyzed Amidation for the Synthesis of Amide-Based APIs
In this study, we explored the application of the tetrahydroxydiboron [B 2 (OH) 4 ] catalyst for the synthesis of amide-based active pharmaceutical ingredients (APIs), a key starting material (KSM), and amide derivatives of the drug, with water as the only byproduct. Notably, the protocol allows a simple acid–base workup for isolation of the pure amide derivatives, highlighting its practical and industrial relevance. Furthermore, the successful scale-up of challenging aromatic APIs from 1 to 10 g demonstrated the robustness and practical applicability of this methodology.
Authors
- Dinesh N. Sawant (ORCID: https://orcid.org/0000-0003-2064-1692)
- Amit Vinayak Gavit (ORCID: https://orcid.org/0009-0000-2354-8819)
- Nayan Koli
- Nutan Rajendra Darandale (ORCID: https://orcid.org/0009-0005-0558-4417)
- Aarif Shaikh
- Buddhabhushan Anil Kamble
- Pooja Dattatray Parit (ORCID: https://orcid.org/0009-0003-6959-0272)
- Ghanshyamkumar Dineshbhai Patel
Institutions
- National Chemical Laboratory (IN)
- Clinical Research Solutions (US)
- Laboratoire de Synthèse Organique (FR)
- Academy of Scientific and Innovative Research (IN)
Publication Details
- Journal
- Organic Process Research & Development
- Published
- 2026-06-17
- DOI
- https://doi.org/10.1021/acs.oprd.5c00516
- Primary Topic
- Chemical Synthesis and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Department of Science and Technology, Ministry of Science and Technology, India
- Council of Scientific and Industrial Research, India
- National Chemical Laboratory