Synthesis Of Novel Thiophene-Bipyrimidine EGFR Inhibitors
DOI:
https://doi.org/10.54097/mvcs7314Keywords:
Novel thiophene bipyrimidines; EGFR inhibitors; synthesis.Abstract
Pyrimidine is a prevalent component in numerous antineoplastic medications. Herein, starting with Olmutinib, by applying the concept of skeleton transition, the thiopheno [3,2-d] pyrimidines were categorized into a thiophene bipyrimidine framework as the foundation, leading to the creation of a novel thiophene bipyrimidine compound. The target product was synthesized through nucleophilic substitution, Suzuki coupling, and reduction reactions employing 2-pyrrolidine-4-trichloropyrimidine as the raw material and triethylamine as the base, leading to the efficient synthesis of compound 7.The structure of compound 7 was confirmed by MS and 1H NMR spectrum and the total yield was high up to 65.7%.
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He, S., C. Xia, H. Li, et al. Cancer profiles in China and comparisons with the USA: a comprehensive analysis in the incidence, mortality, survival, staging, and attribution to risk factors [J]. Science China (Life Sciences), 2024, 67(01): 122-131.
Chen, P., Y. Liu, Y. Wen, et al. non-small cell lung cancer in China [J]. Cancer Communications, 2022.
D, M.K., N. Leticia, D. Theresa, et al. Cancer treatment and survivorship statistics, 2022 [J]. CA: a cancer journal for clinicians, 2022, 72(5): 409-436.
O'leary, K. New treatment option for early-stage lung cancer [J]. Nature Medicine, 2022.
Abu Rous, F., E.K. Singhi, A. Sridhar, et al. Lung Cancer Treatment Advances in 2022 [J]. Cancer Investigation, 2022.
Wang, R., H. Yan, A. Yu, et al. Cancer targeted biomimetic drug delivery system [J]. Journal of Drug Delivery Science and Technology, 2021.
Ferrarelli, L.K. Making cancer cells dependent on EGFR [J]. Science Signaling, 2016.
Momcilovic, M., S.T. Bailey, J.T. Lee, et al. Targeted Inhibition of EGFR and Glutaminase Induces Metabolic Crisis in EGFR Mutant Lung Cancer [J]. Cell Reports, 2017.
Ding, X., X. Liu, X. Song, et al. Chemotherapy Drug Response to the L858R-induced Conformational Change of EGFR Activation Loop in Lung Cancer [J]. Molecular Informatics, 2016.
Jia, Y., C.-H. Yun, E. Park, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors [J]. Nature, 2016.
Patel, H., R. Pawara, A. Ansari, et al. Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance [J]. European Journal of Medicinal Chemistry, 2017.
Singh, D., B.K. Attri, R.K. Gill, et al. Review on EGFR Inhibitors: Critical Updates [J]. Mini-Reviews in Medicinal Chemistry, 2016.
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