Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 1214377-42-0, name is 5-Bromo-2-methoxy-3-(trifluoromethyl)pyridine. A new synthetic method of this compound is introduced below., Product Details of 1214377-42-0
Alternative synthesis for intermediate 24:To a glass flask was added (S)-3-(5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino)- pyrrolidine-1-carboxylic acid tert-butyl ester (intermediate 23) (6.331 g, 15.86 mmol), 5- bromo-2-methoxy-3-(trifluoromethyl)pyridine (intermediate 1 ) (4.465 g, 17.442 mmol), sodium tert-butoxide (2.29 g, 23.78 mmol), tris(dibenzylideneacetone)dipalladium(0) (0.726 g, 0.793 mmol), di-tert-butyl(2′-methylbiphenyl-2-yl)phosphine (0.297 g, 0.951 mmol) and anhydrous ferf-butanol (30 mL). The flask was flushed with a stream of nitrogen for 15 sec and capped. The mixture was heated with stirring for 4h under reflux. The mixture was allowed to cool to rt and partitioned between EtOAc (100 mL) and water (20 mL). The biphasic mixture was filtered the through a celite pad. The organic layer was separated and concentrated in vacuo to give crude (S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)- 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidine-1 -carboxylic acid tert-butyl ester as a yellow foam (7.46 g, 95% yield).
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Reference:
Patent; NOVARTIS AG; FERNANDES GOMES DOS SANTOS, Paulo Antonio; HOeGENAUER, Klemens; HOLLINGWORTH, Gregory; SOLDERMANN, Nicolas; STOWASSER, Frank; TUFILLI, Nicola; ZECRI, Frederic; WO2013/1445; (2013); A1;,
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