Reference of 2077-19-2 ,Some common heterocyclic compound, 2077-19-2, molecular formula is C9H11BrO, 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.
General Palladium Mediated Coupling Procedure; The following general procedure illustrates the method used for Pd mediated N-arylation of the pyrrolidin-2-one moiety with the corresponding aryl bromide: To a sealed tube was added 3- [5-fluoro-2- (4-methyl-piperazin-1-yl)-benzyl]-pyrrolidin-2-one (Preparation 13), aryl bromide (1.2 equiv), dipalladium tris (dibenzylideneacetone) (0.05 equiv), 9, 9-dimethyl-4, 5- bis (diphenylphosphino) xanthene (XANTPHOS) (0.15 equiv), cesium carbonate (1.5 equiv), and dioxane (7 volumes). The mixture was heated at 100 C for 12 to 24 hours. After cooling to room temperature, the mixture was concentrated in vacuo and was purified by silica gel chromatography. The following compounds were prepared via the general procedure above:; Example 1; 3-r5-Fluoro-2-(4-methyl-piperazin-1-vl)-benzvil-1-14-(1-hvdroxv-1-methyl-ethyl)-phenvll-pyrrol idin- 2-one:; 3- [5-Fluoro-2- (4-methyl-piperazin-1-yl)-benzyl]-1- [4- (1-hydroxy-1-methyl-ethyl)-phenyl]- pyrrolidin-2-one : 13C NMR (100 MHz, CDCI3) d 24.8, 31.9, 32. 5, 44. 7, 46.0, 46.9, 52.9, 55.7, 72.4, 113.9, 114.1, 116.8, 117.1, 119.7, 1222.4, 122.5, 125.2, 137.8, 137. 9, 138.2, 145.6, 147. 9, 158. 6, 161.1, 175.5 ; MS (AP/CI) 426.3 (M+H) +. The enantiomers were separable by HPLC (90/10 heptane/ethanol ; Chiralcel OD, 10 cm x 50 cm; 275 mL/minute). Approximate retention times: t1 = 12.7 minutes; t2 = 14.8 minutes
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 2077-19-2, 2-(4-Bromophenyl)propan-2-ol, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; PFIZER PRODUCTS INC.; WO2005/90300; (2005); A1;,
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts