Introduction of a new synthetic route about 517-21-5

With the rapid development of chemical substances, we look forward to future research findings about 517-21-5.

517-21-5, A common compound: 517-21-5, name is Sodium 1,2-dihydroxyethane-1,2-disulfonate,molecular formula is C2H4Na2O8S2, it can change the direction of chemical reaction, and react with certain compounds to generate new functional products. A new synthetic method of this compound is introduced below.

Example 4 Preparation of compound Varenicline (I) A solution prepared dissolving a compound of formula (IV) (30.0 g, 0.12 mols) in 440 mL of tetrahydrofuran is loaded in a 1L flask. 33 g of Pd/C (containing 58.5% w/w of water, 3.97 mmols of Pd, 3% molar) are added, maintaining the reaction mixture under stirring. The reaction environment is saturated with hydrogen at atmospheric pressure and left to react for 48 h at room temperature. The suspension is filtered on celite and the panel is first washed with tetrahydrofuran and then with water. The collected organic phases are directly transferred in a 2L flask, whereas the aqueous phase is first treated with the glyoxal sodium bisulphite adduct (VI) (34.3 g, 0.13 mols) and then added to the organic phase. The so obtained biphasic mixture is heated at 55C and maintained under strong stirring for two hours. The phases are separated and the organic one is concentrated under reduced pressure. The obtained residue is added to the aqueous phase previously removed. The aqueous mixture is treated with a solution of 30% NaOH till it is actually basic. The product is extracted more times with dichloromethane and the organic phases are collected and dried with anhydrous sodium sulphate, filtered off and the solvent is removed by distillation under reduced pressure. Solid Varenicline (I) (20.5 g) is obtained with a yield of 70% in two steps starting from the compound of formula (IV).

With the rapid development of chemical substances, we look forward to future research findings about 517-21-5.

Reference:
Patent; Dipharma Francis S.r.l.; Attolino, Emanuele; Rossi,Roberto; Allegrini, Pietro; EP2551269; (2013); A1;,
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