Some common heterocyclic compound, 6579-54-0, name is 2,6-Dichlorobenzenesulfonyl chloride, molecular formula is C6H3Cl3O2S, 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. Recommanded Product: 6579-54-0
fer?-Bu1yl 4-[(7i?)-7-amino-4-methyl-5,6,7,8-tetrahydronaphthalen-l-yl]piperazine-l- carboxylate (87 mg, 0.25 mmol) was dissolved in dichloromethane (2 ml) and DIPEA (52 mul, 0.30 mmol) and 2,6-dichlorobenzenesulfonyl chloride (68 mg, 0.28 mmol) were added. The mixture was stirred for 4 h. The solvent was evaporated and the residue was dissolved in dichloromethane (2 ml) and TFA (0.24 ml) was added. The mixture was stirred at ambient temperature for 15 h. The mixture was concentrated and EtOAc was added. The mixture was washed with aqueous sodium hydroxide (pH 8-9), dried (Na2SO4), filtered and the solvent was evaporated. The residue was purified by preparative HPLC to give a dry film (6.5 mg, 5%).1H NMR (400 MHz, MeOD-^) delta ppm 7.58 (2 H, d) 7.48 (1 H, d) 6.97 (1 H, d) 6.81 (1 H, d) 3.53 – 3.61 (1 H, m) 3.01 – 3.17 (5 H, m) 2.91 – 2.98 (2 H, m) 2.74 – 2.88 (3 H, m) 2.54 – 2.63 (2 H, m) 2.14 (3 H, s) 1.96 – 2.04 (1 H, m) 1.74 – 1.85 (1 H, m); ESI-MS m/z M+H1″ 454, 456, 458.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 6579-54-0, its application will become more common.
Reference:
Patent; ASTRAZENECA AB; WO2007/108742; (2007); A1;,
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