Related Products of 1133123-02-0, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 1133123-02-0 as follows.
A mixture of Intermediate 177c (crude boronic ester, 60 mg, 0.107 mmol) and 4- bromo-2-iodobenzoic acid (35.0 mg, 0.107 mmol) in NMP/H20 (1:1, 1 mL) was treated with K2C03 (32.6 mg, 0.236 mmol) followed by Pd2(dba)3 (9.80 mg, 10.71 muiotaetaomicron). The resulting mixture was degassed with N2 for 2 min before the reaction vessel was sealed and irradiated in a microwave reactor at 120 C for 15 min. The mixture was cooled and filtered through celite and purified via preparative HPLC (Column: Phenomenex AXIA Luna 100 x 30mm 5u s; Mobile Phase A: 10:90 ACN: H20 with 10 mM TFA; Mobile Phase B: 90: 10 ACN: H20 with 10 mM TFA; Gradient: 0-100% B over 10 minutes, then a 2-minute hold at 100% B; Flow: 40 mL/min.) to afford the title compound (Intermediate 195a, 17 mg, 0.037 mmol, 34.5 % yield). LC-MS (Method A5): 2.27 min, [M + H]+=465.1 and 467.1. 1H NMR (500 MHz, CDCl3) delta 7.91 (br d, 7=8.0 Hz, IH), 7.76 (br s, IH), 7.65 (br d, 7=7.7 Hz, IH), 7.44 (br s, 2H), 5.84 (br s, 2H), 3.26 (br s, 2H), 2.72 – 2.54 (m, 6H), 1.38 (br s, 3H).
According to the analysis of related databases, 1133123-02-0, the application of this compound in the production field has become more and more popular.