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Review on Synthetic Approaches toward Rivaroxaban (Xarelto), an Anticoagulant Drug
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2022-07-22 , DOI: 10.1021/acs.oprd.2c00188 Dmitry Y. Mladentsev 1 , Ekaterina N. Kuznetsova 2 , Maria N. Skvortsova 2 , Ratmir R. Dashkin 2
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2022-07-22 , DOI: 10.1021/acs.oprd.2c00188 Dmitry Y. Mladentsev 1 , Ekaterina N. Kuznetsova 2 , Maria N. Skvortsova 2 , Ratmir R. Dashkin 2
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Venous thromboembolism including deep vein thrombosis and pulmonary embolism is an abundant and dangerous disease with significant relapse probability and mortality. In pursuit of an effective treatment, Bayer created Rivaroxaban, nowadays known under the brand name Xarelto, that was approved by the FDA in 2011. By 2022, the number of main indications for the drug has been increased 10-fold as well as the drug’s prevalence in the field of thrombosis treatment. It is therefore apparent that with growing prescriptions new synthetic pathways are highly desirable, especially those utilizing inexpensive and safe reagents in environmentally benign protocols. The present work reviews the literature concerning Rivaroxaban preparation with an emphasis on the applicability of synthetic pathways on a large scale. Within the synthetic sequences, common intermediates are discussed in detail and relevant comparisons are made. Our main purpose is to provide an overview of the subject in its current state, paying attention to advances made and suggesting possible directions for further development.
中文翻译：
抗凝药物利伐沙班（拜瑞妥）的合成方法综述
包括深静脉血栓形成和肺栓塞在内的静脉血栓栓塞是一种多发且危险的疾病，具有显着的复发概率和死亡率。为了追求有效的治疗，拜耳创造了利伐沙班，现在以 Xarelto 的品牌而闻名，该品牌于 2011 年获得 FDA 的批准。到 2022 年，该药物的主要适应症数量以及该药物的数量增加了 10 倍在血栓治疗领域的流行。因此很明显，随着处方的增加，非常需要新的合成途径，尤其是那些在环境友好的协议中使用廉价和安全试剂的途径。目前的工作回顾了有关利伐沙班制剂的文献，重点是大规模合成途径的适用性。在合成序列中，对常见的中间体进行了详细讨论并进行了相关比较。我们的主要目的是概述该主题的当前状态，关注已取得的进展并提出进一步发展的可能方向。
更新日期：2022-07-22
中文翻译：
抗凝药物利伐沙班（拜瑞妥）的合成方法综述
包括深静脉血栓形成和肺栓塞在内的静脉血栓栓塞是一种多发且危险的疾病，具有显着的复发概率和死亡率。为了追求有效的治疗，拜耳创造了利伐沙班，现在以 Xarelto 的品牌而闻名，该品牌于 2011 年获得 FDA 的批准。到 2022 年，该药物的主要适应症数量以及该药物的数量增加了 10 倍在血栓治疗领域的流行。因此很明显，随着处方的增加，非常需要新的合成途径，尤其是那些在环境友好的协议中使用廉价和安全试剂的途径。目前的工作回顾了有关利伐沙班制剂的文献，重点是大规模合成途径的适用性。在合成序列中，对常见的中间体进行了详细讨论并进行了相关比较。我们的主要目的是概述该主题的当前状态，关注已取得的进展并提出进一步发展的可能方向。
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