New downstream synthetic route of Isoindoline hydrochloride

The synthetic route of 32372-82-0 has been constantly updated, and we look forward to future research findings.

Reference of 32372-82-0, These common heterocyclic compound, 32372-82-0, name is Isoindoline hydrochloride, its 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.

To a solution of 2-chloropyridin-4-amine (0.5 g, 3.90 mmol) in toluene (12 ml) were added isoindoline hydrochloride (0.91 g, 5.85 mmol), BINAP (0.24 g, 0.39 mmol) and potassium tertbutoxide (2.07 g, 9.76 mmol) at rt. The mixture was degassed for 10 mm before addition of Pd2(dba)3 (0.178 g, 0.19 mmol). The reaction mixture was at 110C for 4 hrs. The resulting mixture was poured into cold water (200 ml) and combined with two other batches prepared by an identical method on the same scale. The resulting mixture was extracted with DCM (3 x 100 ml). The organic phase was collected, dried over Na2SO4, filtered and concentrated under reduced pressure. The resulting residue was purified by column chromatography (3% MeOH in DCM) yielding 2-(isoindolin-2-yl)pyridin-4- amine (1.2 g, 5.67 mmol). LCMS: Method C, 1.57 mi MS: ES+ 212.29.

The synthetic route of 32372-82-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MISSION THERAPEUTICS LIMITED; KEMP, Mark Ian; STOCKLEY, Martin Lee; MADIN, Andrew; (95 pag.)WO2017/103614; (2017); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem