Reference of 2927-71-1, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 2927-71-1 as follows.
[0666] Synthesis of 4-(2-chloro-5-fluoropyrimidin-4-yl) morpholine: [0667] To a stirred solution of morpholine (260 mg, 2.99 mmol) in EtOH (10 mL) under argon atmosphere were added DIPEA (1.15 g, 8.98 mmol) and 2, 4-dichloro-5- fluoropyrimidine (500 mg, 2.99 mmol) at RT; heated to reflux and stirred for 1 h. The reaction was monitored by TLC; after completion of the reaction, the volatiles were removed in vacuo. The residue was diluted with water (20 mL) and extracted with EtOAc (2 x 30 mL). The combined organic extracts were dried over sodium sulphate, filtered and concentrated in vacuo to obtain the crude. The crude was purified through silica gel column chromatography using 15% EtOAc/ Hexanes to afford 4-(2-chloro- 5-fluoropyrimidin-4-yl) morpholine (550 mg, 85%>) as an off-white solid. [0668] 1H-NMR (CDCI3, 500 MHz): delta 7.96 (d, 1H), 3.82-3.76 (m, 8H); LC-MS: 99.56%; 218.1 (M++l); (column: X-Bridge C-18, 50 3.0 mm, 3.5 muiotaeta); RT 2.88 min. 0.05% TFA: ACN; 0.8 mL/min); TLC: 20% EtOAc/ Hexanes (R/. 0.3).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,2927-71-1, its application will become more common.
Reference:
Patent; ENVIVO PHARMACEUTICALS, INC.; RIPKA, Amy; SHAPIRO, Gideon; MCRINER, Andrew, J.; BURSAVICH, Matthew, Gregory; WO2013/142269; (2013); A1;,
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