With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.
109-07-9, {4- [5-BROMOTHIOPHEN-2-YL]-PYRIMIDIN-2-YL}- (2, 2,6, 6-TETRAMETHYL-PIPERIDIN-4-YL)-AMINE, (Step C of Example 5,395 mg, 1 MMOL), Pd (OAC) 2 (20 mg), R- (+)-BINAP (20 mg), 2- methylpiperazine (500 mg, 5 mmol) and NaOtBu (400 mg, 4 mmol) were dissolved in 1,4- dioxan (6 ml) and refluxed for 3 hours. The reaction mixture was poured on water and extracted 3 times with EtOAc. The combined organic phases were dried over sodium sulfate, filtered through a bed of silicagel (TBME/MeOH/ammonia : 90/10/1) and purified via preparative HPLC to give the title compound as yellow crystals. Yield: 10 mg (2%). MS (ESI): 415 [M+H] + LH-NMR (CDCI3) : No. (ppm) 8.12 (d, 1H), 7.43 (d, 1 H), 6.73 (d, 1H), 6.10 (d, 1H), 4. 88 (br d, 1 H), 4.45 (m, 1H), 3.48 (br d, 2H), 2.90-3. 17 (M, 5H), 2.59 (br t, 1H), 2.13 (br d, 2H), 1.41-1. 79 (m, 14H), 1.18 (d, 3H).
As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.
Reference:
Patent; NOVARTIS AG; NOVARTIS PHARMA GMHBH; WO2004/89913; (2004); A1;,
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