Synthetic Approaches toward Dabigatran Etexilate, an Oral Anticoagulant Drug

• Published in: Organic process research & development Vol. 28; no. 9; pp. 3509 - 3523
• Main Authors: Kalam, Abdul, Mahammad Ghouse, Shaik, Joshi, Swanand Vinayak, Tamang, Nitesh, Sahu, Nived Rajesh, Yaddanapudi, Madhavi Venkata, Nanduri, Srinivas
• Format: Journal Article
• Language: English
• Published: American Chemical Society 20-09-2024
• Subjects: synthesis; dabigatran etexilate; anticoagulant; process development; impurities
• ISSN: 1083-6160; 1520-586X
• DOI: 10.1021/acs.oprd.4c00233

Thromboembolic disorders affect millions of people worldwide. Anticoagulant drugs, such as Dabigatran etexilate, Rivaroxaban, Argatroban, Enoxaparin, and Fondaparinux, are commonly used in treating most of these diseases. Dabigatran etexilate (PRADAXA), the first oral direct thrombin inhibitor of its kind, has become a leading anticoagulant therapy for various thromboembolic disorders. Numerous efforts have been made to synthesize API and its intermediates. This review comprehensively examines the diverse methodologies employed for the synthesis of the Key Starting Materials (KSMs), Key Intermediates, and the final API of Dabigatran etexilate. The review also details the various impurities generated during the process. For the reader’s convenience, the review is organized into sections that separately describe each of the Key Starting Materials and Intermediates’ synthetic processes. This review of recent advancements serves as a valuable resource for researchers, chemists, and pharmaceutical scientists engaged in the development and optimization of synthetic routes to produce Dabigatran etexilate.