Some common heterocyclic compound, 82998-57-0, name is 3-Iodo-4-methylbenzoic acid, molecular formula is C8H7IO2, 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. 82998-57-0
General procedure: 1.10.5. General method K To a suspension of amine derivative (1 eq.), carboxylic acid (1.2 eq.), EDCI.HC1 (1.3 eq.) and HOBt (1.3 eq.) in DMF is added Et3N (2.6 eq.). The reaction mixture is stirred overnight at room temperature. After 48 h, water was added and the mixture is extracted with EtOAc. The organic layers are combined, dried over Na2S04, filtered and evaporated to dryness. The expected intermediate is purified by chromatography of silica gel (elution DCM/ MeOH: 95/5 or 90/10) or preparative LCMS.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 82998-57-0, its application will become more common.
Reference:
Patent; GALAPAGOS NV; SANIERE, Laurent Raymond Maurice; HUCK, Jacques; DYKES, Graeme James; SCHMITT, Benoit Antoine; BLANC, Javier; BUTLER, Anna Sara; BEAUMONT, Stephane Nicolas Alain; BONNATERRE, Florence Marie-Emilie; WO2015/24905; (2015); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com