Brief introduction of 55121-99-8

55121-99-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

3,5-Dibromopyridine (249 mg, 1.05 mmol), [l-(tert-butoxycarbonyl)-H-indol-2- yl]boronic acid (302 mg, 1.16 mmol), Pd(PPh3J4 (61 mg, 0.05 mmol) and Na- HCO3 (309 mg, 3.68 mmol) in DME/water (3.5: 1, 4.5 mL) was irradiated with microwaves at 120 0C for 5 minutes, followed by 180 0C for 12 minutes. The reaction mixture was extracted with DCM (2×10 mL) and water (10 mL). The organic layers were combined, dried (Na2SO4), filtered and concentrated. The residue was purified by preparative HPLC (YMC ODS-AQ, 0.1% TFA-MeCN) to give 2-(5-bromopyridin-3-yl)-lH-indole. 2-(5-bromopyridin-3-yl)-lH-indole (10 mg, 0.04 mmol), {4-[(4-methylpiperazin-l-yl)carbonyl]phenyl}amine (12 mg, 0.06 mmol), Pd(OAc)2 (2 mg, 0.01 mmol), NaOtBu (12 mg, 0.13 mmol) and Xantphos (9 mg, 0.018 mmol) in toluene /tBuOH (5: 1, ImL) was irradiated with micro waves at 160 0C for 20 minutes. Additional Pd(OAphi (5 mg, 0.02 mmol) was added and the resulting mixture was irradiated with micro waves for a further 20 min at 160 0C. The crude mixture was extracted with EtOAc and 1 M aq NaOH and the product precipitated and was filtered off. The crude product was purified by preparative HPLC (ACE C8, 0.1% TFA, MeCN) followed by (XTerra C 18, 5OmM NH4HCO3 pH 10, MeCN). This gave the title compound as a white solid (0.7 mg). MS (ESI+) for C25H25N5O m/z 412 (M+H)+. HPLC 100%(System A), 96%(System B).

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BIOVITRUM AB (PUBL); WO2007/147874; (2007); A1;,
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