* 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.
With triethylamine; acetyl chloride In tetrahydrofuran at 0 - 20℃; for 0.5 h;
Step A: 6-Nitroindoline (3.0 g, 18.3 mmol) was dissolved in THF (45 mL) and Et3N (3.4 mL, 24.4 mmol) at O0C. Acetyl chloride (1.5 mL, 21 mmol) was added drop wise. The mixture was stirred at room temperature for 30 minutes. The mixture was partitioned between EtOAc and aqueous HCl. The organic layer was dried and concentrated to yield l-acetyl-6-nitroindoline (3.8 g, 100percent) as a yellow solid.
Reference：
[1] Patent: WO2006/19831, 2006, A1, . Location in patent: Page/Page column 447
[2] Zhurnal Obshchei Khimii, 1959, vol. 29, p. 2541,2550; engl. Ausg. S. 2504, 2511
[3] Heterocycles, 1998, vol. 48, # 12, p. 2481 - 2484
2
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Reference：
[1] Heterocycles, 2005, vol. 65, # 8, p. 1939 - 1946
[2] Chemical and Pharmaceutical Bulletin, 2005, vol. 53, # 10, p. 1277 - 1290
[3] European Journal of Medicinal Chemistry, 2005, vol. 40, # 2, p. 167 - 172
With triethylamine; acetyl chloride; In tetrahydrofuran; at 0 - 20℃; for 0.5h;
Step A: 6-Nitroindoline (3.0 g, 18.3 mmol) was dissolved in THF (45 mL) and Et3N (3.4 mL, 24.4 mmol) at O0C. Acetyl chloride (1.5 mL, 21 mmol) was added drop wise. The mixture was stirred at room temperature for 30 minutes. The mixture was partitioned between EtOAc and aqueous HCl. The organic layer was dried and concentrated to yield l-acetyl-6-nitroindoline (3.8 g, 100%) as a yellow solid.
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