Journal
MOLECULAR DIVERSITY
Volume 26, Issue 5, Pages 2981-3002Publisher
SPRINGER
DOI: 10.1007/s11030-022-10406-8
Keywords
Total synthesis; Anti-angiogenesis receptor tyrosine kinase inhibitors; Cancer therapy; Pazopanib; Regorafenib; Lenvatinib
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Angiogenesis is an important scientific subject in the field of malignant tumors, with current research focusing on the role of blood microvessels in cancer cell proliferation, tumor growth, and metastasis. Tyrosine kinases have been identified as therapeutic targets that influence angiogenesis in tumor growth. This review aims to track the advancements in the total synthesis of three receptor tyrosine kinase inhibitors and examines the purification process of these anticancer medicines. Notably, different patents may report varying procedures and yields for the synthesis of the desired drugs and their intermediates.
Angiogenesis is an important and interesting scientific subject in the area of malignant tumours. Current research importance and interest are directed in connection to blood microvessels in cancer cell proliferation, tumour growth, and metastasis. Tyrosine kinases have been intensely implicated as therapeutic targets that affect the angiogenic process in tumour growth. In the last decades, targeting angiogenesis has led to achievements in the therapy of different carcinomas by different mechanisms, such as the utilization of anti-angiogenic small molecule receptor tyrosine kinase inhibitors. In the current review, we aim to track the advancements in the total synthesis of three receptor tyrosine kinase inhibitors (pazopanib, regorafenib and lenvatinib). This review surveys different synthetic routes for these three approved drugs (pazopanib, regorafenib and lenvatinib) which were previously published as patents (2014-2021). The purity of medicines is a very important factor during manufacturing so we have decided to review the purification process of these anticancer medicines as well. It should be noted that the different patents may have reported some procedures with different yields and purities for the synthesis of desired drug and their intermediates. In order to simplify the understanding of the contents of this review article, only the best results reported in each of these patents are reported for the synthesis of desired drug and their intermediates.
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