One of the major reasons is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level.7025-19-6, name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, introduce a new downstream synthesis route. , 7025-19-6
To a solution of 6-(6-fluoro-4-iodo-2-pyridyl)-5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H- pyrido[4,3-d]pyrimidine (the product of step 1 in Example 96, 100 mg, 223 muiotaetaomicron) in dioxane ( 3mL) was added isothiazolidine-1,1-dioxide (54.1 mg, 446 muiotaetaomicron), cesium carbonate (145 mg, 446 muetaiotaomicron), Xantphos (25.8 mg, 44.6 muetaiotaomicron) and Pd(OAc)2(5.01 mg, 22.3 muetaiotaomicron). After being heated at 100 C with stirring for 20 hrs under argon, the resulting reaction mixture was then filtered and the filtrate was concentrated in vacuo. The residue was purified by prep-HPLC to give 2-[2-fluoro-6-(5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl)-4- pyridyl]-1,2-thiazolidine-1,1-dioxide (8 mg) as a light yellow solid. 1H NMR (400MHz, DMSO- d6) delta ppm: 8.99 (d, 2H), 8.95 (s, 1H), 7.64 (t, 1H), 6.32 (s, 1H), 6.15 (s, 1H), 5.69-5.64 (m, 1H), 4.47-4.36 (m, 1H), 3.89 – 3.79 (m, 2H), 3.68-3.59(m, 2H), 3.54 – 3.43 (m, 1H), 3.14 – 2.98 (m, 2H), 2.42-2.37 (m, 2H), 1.52 (d, 3H). MS obsd (ESI) [(M+H)+]: 442.
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Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; HAN, Xingchun; JIANG, Min; WANG, Jianhua; WANG, Yongguang; YANG, Song; (211 pag.)WO2018/1952; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com