With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.
Example 68 (3S)-1-{[6-(5-{1-[4-(cyclopropylsulfonyl)phenyl]-2-(tetrahydro-2H-pyran-4-yl)ethyl}-1H-pyrrol-2-yl)pyridin-3-yl]methyl}-3-methylpiperazine To a solution of 6-(5-{1-[4-(cyclopropylsulfonyl)phenyl]-2-(tetrahydro-2H-pyran-4-yl)ethyl}-1H-pyrrol-2-yl)pyridine-3-carbaldehyde (250 mg) in tetrahydrofuran (10 mL) was added (2S)-2-methylpiperazine (270 mg), and the mixture was stirred at room temperature for 30 min. To the reaction mixture was added sodium triacetoxyborohydride (230 mg), and the mixture was stirred overnight at room temperature. The reaction mixture was diluted with ethyl acetate, washed with saturated aqueous sodium hydrogen carbonate and saturated brine, dried (MgSO4) and concentrated. The residue was subjected to preparative HPLC to give the title compound (111 mg, yield 38%) as a colorless amorphous solid. MS:549(MH+). 1H NMR (300 MHz, CDCl3) 50.98 – 1.03 (2 H, m), 1.05 (3 H, d, J=6.2 Hz), 1.29 – 1.49 (5 H, m), 1.52 – 1.70 (3 H, m), 1.82 – 1.97 (2 H, m), 2.05 – 2.15 (2 H, m), 2.36 – 2.49 (1 H, m), 2.66 – 2.79 (2 H, m), 2.81 – 3.05 (3 H, m), 3.19 – 3.36 (2 H, m), 3.40 – 3.50 (2 H, m), 3.84 – 4.00 (2 H, m), 4.12 – 4.23 (1 H, m), 6.15 (1 H, t, J=3.0 Hz), 6.63 (1 H, dd, J=2.4, 3.5 Hz), 7.40 (2 H, d, J=8.3 Hz), 7.44 – 7.50 (1 H, m), 7.52 – 7.63 (1 H, m), 7.75 – 7.88 (2 H, m), 8.29 (1 H, d, J=1.5 Hz), 9.22 (1 H, brs)., 74879-18-8
As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.
Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP2149550; (2010); A1;,
Piperazine – Wikipedia
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