It has been brought to our attention by an alert medicinal chemist from the P. R. China that Scheme 3 and the Experimental section of this paper [1] had been copied from an earlier paper by Gong et al. [2], published in Chinese [3]. In addition, the m.p. of 119-120°C given for the final product Gefitinib (7) was also copied from an earlier publication [4], and later shown to be wrong [5]. The first listed author has subsequently provided us with another different melting point for Gefitinib (212-214°C) and informed us that the correct melting points for the intermediates methyl 5-(3-chloropropoxy)-4-methoxy-2-nitrobenzoate (18) and 6-(3-chloropropoxy)-4-chloro-7-methoxy-quinazoline (21) should be revised to 79-81°C and 128-130°C, respectively. In light of these serious factual errors and the apparent plagiarism, the Editorial Team and the Publisher have determined that the paper should be declared “Withdrawn”. We apologize to our readership for any inconvenience this may cause.
Dr. Derek J. McPhee, Editor-in-Chief, Molecules
Dr. Shu Kun Lin, Publisher, MDPI
Supplementary Files
References and Notes
- 1.Li M. D., Zheng Y. G., Ji M. Synthesis of Gefitinib from Methyl 3-Hydroxy-4-methoxy-benzoate. Molecules. 2007;12:673–678. doi: 10.3390/12030673. [DOI] [PMC free article] [PubMed] [Google Scholar] [Retracted]
- 2.Dr. Ping Gong, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, 110016 Shenyang, Liaoning, P. R. China; Fax: (+86) 24-23986426/23882925, Phone: (+86) 24-23986426, E-mail: gongpinggp@126.com.
- 3.Yuan L., Hao J.-H., Zhang Y., Wang Y.-Y., Wang H., Chen. J.-Y., Gong P. Synthesis of 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline (ZD1839) Chin. J. Med. Chem. 2005;15:39–41. [Google Scholar]
- 4.Gibson K.H. Quinazoline derivatives. WO9633980. 1996:24.
- 5.Recently a melting point of 194-198 °C was reported for Gefitinib; Gilday J. P., David M. Process for the preparation of 4-(3’-chloro-4’-fluoroanilino)-7-methoxy-6-(3-morpholino-propoxy)quinazoline. WO2004024703. 2006:12.
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