Application of 204257-72-7,Some common heterocyclic compound, 204257-72-7, name is Methyl 2-fluoro-4-iodobenzoate, molecular formula is C8H6FIO2, 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.
In a round-bottomed flask chiral(2S,3R,4S,5R)-4-(3-chloro-2-fluoro-phenyl)-3-(4-chloro-2-fluoro-phenyl)-2-(2,2-dimethyl-propyl)-5-hydroxymethyl-1-prop-2-ynyl-pyrrolidine-3-carbonitrile (30 mg, 61.1 mumol), methyl 2-fluoro-4-iodobenzoate (17.1 mg, 61.1 mumol, Eq: 1.00) were dissolved in toluene (1.2 ml) then cuprous iodide (2.33 mg, 12.2 mumol) dichlorobis(triphenylphosphine) palladium (II) (1.29 mg, 1.83 mumol) and triethylamine (6.16 mg, 8.51 mumol, 61.1 mumol) were added and stirred under nitrogen atmosphere at 25 C. for 16 hours (protect from light with aluminum foil around flask during reaction conditions). Work up by filtration through celite, wash with EtOAc, mixture concentrated under reduced vacuum to yield a crude oil. Purification by RP-HPLC (40-95% acetonitrile/water) to afford chiral methyl 4-(3-((2S,3R,4S,5R)-4-(3-chloro-2-fluorophenyl)-3-(4-chloro-2-fluorophenyl)-3-cyano-5-(hydroxymethyl)-2-neopentylpyrrolidin-1-yl)prop-1-ynyl)-2-fluorobenzoate (17.3 mg, 26.9 mumol, 44.0% yield) as an off-white foam. HRMS (ES+) m/z Calc for C26H26Cl2F2N2O+H[(M+)1+]: calc: 643.1737. found: 643.1735.
The synthetic route of 204257-72-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Liu, Jin-Jun; Ross, Tina Morgan; US2012/149660; (2012); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com