Reference of 672-57-1, A common heterocyclic compound, 672-57-1, name is 1-Chloro-2-iodo-4-(trifluoromethyl)benzene, molecular formula is C7H3ClF3I, 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.
Compound 1 : 5-(2-chloro-5-trifluoromethyl-phenyl)-thiophene-2-carboxylic acid (2,6-difluoro-phenyl)-amide; Step 1; A mixture of 1-chloro-2-iodo-4-trifluoromethyl-benzene (a, 6 mmol), 5- (dihydroxyboryl)-2-thiophenecarboxylic acid (b, 6 mmol), bis(triphenylphosrhohine) palladium(ll) dichloride catalyst (0.30 mmol), potassium carbonate (1 g) in dry 1-methyl-2-pyrrolidinone (NMP) (6 mL) was heated at 120 0C for 4 h. Alternatively, 0.30 mmol of Pd(BnCI)(PPh3)2 may be used instead of bis(triphenylphosphine) palladium(ll) dichloride. The mixture was taken up with ethyl acetate (EtOAc) (100 mL), washed with water (2×100 mL) and dried over Na2SO4. The oil obtained on concentration was passed through silica gel and crystallized from EtOAc/hexanes to give c as a white solid (0.98 g).
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; SYNTA PHARMACEUTICALS CORP.; WO2006/81389; (2006); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com