Application of 57641-67-5 ,Some common heterocyclic compound, 57641-67-5, molecular formula is C6H13BrO3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
2-[2-(2-bromoethoxy)ethoxy]ethanol (0.12 g, 0.547 mmol, 2 mL) was added to a solution of rapamycin (0.5 g, 0.547 mmol) and p-toluenesulfonic acid hydrate (0.5 g, 2.73 mmol) in THF (7 mL) at room temperature and the resulting mixture was stirred for 2 hours. Ice cold NaHCO3 aqueous solution was then added and the mixture was extracted with EtOAc (30 mL ¡Á 3). The organic phase was then dried over Na2SO4, filtered, and concentrated in vacuo. The resulting crude material was purified by reverse phase chromatography (CH3CN/pure water = 7:3) to obtain (21E,23E,25E,26E,34R,35S,36R,37R, 39R,41S,44S,45R,46R,55S)-43-[2-[2-(2-bromoethoxy)ethoxy]ethoxy]-45,55-dihydroxy-44- [(1S)-2-[(1S,3R,4R)-4-hydroxy-3-methoxy-cyclohexyl]-1-methyl-ethyl]-46-methoxy-34,35, 36,37,47,48-hexamethyl-65,66-dioxa-56-azatricyclohexatriaconta-21,23,25(47),26(48)- tetraene-49,50,51,52,53-pentone (0.2 g, 33.4% yield, 1HNMR shows a rapamycin impurity) as a white solid. MS (EI+, m/z): 1116.4 [M+Na] +.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,57641-67-5, its application will become more common.
Reference:
Patent; NAVITOR PHARMACEUTICALS, INC.; SAIAH, Eddine; O’NEILL, David, John; KANG, Seong Woo Anthony; (366 pag.)WO2019/241789; (2019); A1;,
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