The effect of the change of 1,1-Dioxo-isothiazolidine synthetic route on the product

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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

5908-62-3, A flask was charged under nitrogen with 3-bromo-5-iodo-benzoic acid tert-butyl ester D8b (1 g, 2.6 mmol, 1 equiv), Cs2CO3 (1.26 g, 3.9 mmol, 1.5 equiv), tris (DIBENZYLIDENEACETONE) DIPALLADIUM (0) (12 mg, 0.013 mmol, 0.005 equiv), Xantphos (22 mg, 0.038 mmol, 0.015 equiv) and toluene (20 ML). ISOTHIAZOLIDINE 1,1-dioxide (D22a) (350 mg, 2.9 mmol, 1.1 equiv) was then added and the resulting mixture was stirred at 100C for 16 h then cooled to room temperature and diluted with AcOEt. The organic phase was washed with saturated aqueous NAHC03 solution, dried over MGS04 and concentrated in vacuo. The residue was triturated with Et20 to give 3-BROMO-5-(1, 1-DIOXO-116-ISOTHIAZOLIDIN-2-YL)-BENZOIC acid tert-butyl ester (D17) (350 mg 38%) as a white solid.

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Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/50619; (2004); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com