2,6-Dichloronicotinic acid (CAS: 38496-18-3) can be used in the preparation of AZD8055 (CAS: 1009298-09-2). AZD8055 has been utilized in clinical trials focused on the treatment of cancer, lymphomas, solid tumors, malignant glioma, and brainstem glioma, among others.
Application In Synthesis of [ 38496-18-3 ]
* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.
Reference：
[1] Bioorganic and Medicinal Chemistry Letters, 2013, vol. 23, # 5, p. 1212 - 1216
2
[ 38496-18-3 ]
[ 38025-90-0 ]
Yield
Reaction Conditions
Operation in experiment
88%
at 129℃; for 4 h;
Step a 2-chloro-6-oxo-1 ,6-dιhydropyrιdιne-3-carboxylιc acιd; ° A 500-mL round-bottom flask was charged with 2,6-dιchloronιcotιnιc acid (25 0 g 130 mmol), NaOH solution (325 ml_, 2N) and the solution was refluxed at 1290C for 4 hours The reaction mixture was cooled to room temperature and acidified with a 6N aq HCI solution The resulting precipitate was filtered and dried under reduced pressure yielding to the desired product (19 87g, 88percent)
4 g
Stage #1: at 120℃; for 4 h; Inert atmosphere Stage #2: With hydrogenchloride In water at 20℃;
2,6-Dichloronicotinic acid (6 g) was placed in a 250 mL round bottom flask, and sodium hydroxide solution (80 mL) was added.The mixture was heated to 120 ° C for 4 hours. After the reaction was completed, it was cooled to room temperature, acidified with 6N hydrochloric acid, and the solid was precipitated, filtered, and dried to give the title compound (4 g).
Reference：
[1] Patent: WO2010/108652, 2010, A1, . Location in patent: Page/Page column 97
[2] Patent: WO2008/125820, 2008, A1, . Location in patent: Page/Page column 33
[3] Patent: CN108314645, 2018, A, . Location in patent: Paragraph 0094; 0095; 0096; 0097
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