Introduction of a new synthetic route about 5-Bromo-2,3-dihydro-1H-inden-1-amine

Synthetic Route of 185122-74-1, 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 185122-74-1 as follows.

At 0 0C and under protective atmosphere, a solution of 2-propanesulfonyl chloride (1 1.87 mL, 121 mmol) in DCM (121 mL) was added gradually to a solution of 5-bromo-2,3- dihydro-7/-/-inden-1 -amine (12.8 g, 60.4 mmol) and 1 ,8-diazabicyclo[5.4.0]undec-7-ene (4.83 mL, 32.1 mmol) in dichloromethane (300 mL). The reaction was stirred at rt overnight. The reaction mixture was washed with 1 N KHSO4 (1x) and sat NaHCOs (2x) before being dried on IS^SO4 and solvent evaporated in vacuo to afford a green oil. Purification by column chromatography (25% EtOAc in hept) afforded the title compound as a white solid (6.0 g, 18.9 mmol, 31 %). MS (ESI) : m/z [M – H]”317.0.

According to the analysis of related databases, 185122-74-1, the application of this compound in the production field has become more and more popular.

Reference:
Patent; N.V. ORGANON; WO2009/147167; (2009); A1;,
Bromide – Wikipedia,
bromide – Wiktionary