Reference of 496-12-8, 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 496-12-8 as follows.
Example 17Synthesis of 5-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-2-(phenylsulfonyl)isoindolineReagents MW Reagent/raw material (g/mole) Quantity moles Isoindoline 119.16 0.5 g 4.2 benzenesulfonyl chloride 176.62 1.1 g 6.3 2-(phenylsulfonyl)isoindoline 259.32 0.54 g 2 sulfurochloridic acid 116.52 5 mL excess 2-(phenylsulfonyl)isoindoline-5- 357.83 0.05 g 0.139 sulfonyl chloride 2,3- 136.15 0.024 g 0.18 dihydrobenzo[b][1,4]dioxineAlCl3 133 0.037 0.27 Step 1: Isoindoline was dissolved in 5 mL dry pyridine, and benzenesulfonyl chloride was dropped in. The reaction was stirred overnight at room temperature and an intense red color developed. When complete as determined by HPLC using the protocol of Example 1, as well as by LCMS, the crude reaction mixture was poured into 100 mL cold 1M KHSO4, and extracted twice with 50 mL CH2Cl2. The organic phase was evaporated and the evaporation residue was purified by CombiFlash (PE/EtOAC) providing 1.1 g pure product (100% yield).
According to the analysis of related databases, 496-12-8, the application of this compound in the production field has become more and more popular.
Reference:
Patent; Becker, Oren M.; Shitrit, Alina; Schutz, Nili; Ben-Zeev, Efrat; Yacovan, Avihai; Ozeri, Rachel; Kehat, Tzofit; Mirilashvili, Sima; Aizikovich, Alex; Sherman, Daniel; Behar, Vered; Kashtan, Osnat; US2012/108631; (2012); A1;,
Indoline – Wikipedia,
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