5464-12-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.
(S)-2-( tert-Butoxy)-2-( 4-(4, 4-dimethylpiperidin-l-yl)-2, 6-dimethyl-5-( 4-( 2-( 4- methylpiperazin-l-yl)ethoxy)phenyl)pyridin-3-yl)acetic acid. To a stirred solution of (S)- ethyl 2-(tert-butoxy)-2-(4-(4,4-dimethylpiperidin-l-yl)-5-(4-hydroxyphenyl)-2,6- dimethylpyridin-3-yl)acetate (20 mg, 0.043 mmol), 2-(4-methylpiperazin-l-yl)ethanol (30.8 mg, 0.213 mmol) and Ph3P-resin (33.6 mg, 0.128 mmol) in THF (5 mL) was added DEAD (0.020 mL, 0.128 mmol) at rt. After 18 h, mixture was filtered to remove polymer, concentrated and treated with IN NaOH (0.854 mL, 0.854 mmol) in MeOH (1 mL) at 75 °C for 16 h. Mixture was then cooled and purified by prep-HPLC to afford (S)-2-(tert-butoxy)-2-(4-(4,4-dimethylpiperidin-l-yl)-2,6-dimethyl-5-(4-(2-(4- methylpiperazin-l-yl)ethoxy)phenyl)pyridin-3-yl)acetic acid (2.1 mg, 3.71 mupiiotaomicron, 8.68 percent yield). 1H MR (500MHz, DMSO-d6) delta 7.21 (d, J=8.4 Hz, 1H), 7.05 – 7.00 (m, 3H), 5.80 (s, 1H), 4.22 – 4.04 (m, 2H), 3.36 (br. s., 1H), 2.84 – 2.76 (m, 1H), 2.70 (t, J=5.7 Hz, 2H), 2.43 (s, 3H), 2.33 (br. s., 3H), 2.16 (s, 3H), 2.06 (s, 3H), 1.49 (br. s., 1H), 1.30 (br. s., 1H), 1.17 (d, J=11.4 Hz, 1H), 1.12 (s, 9H), 1.02 (d, J=12.5 Hz, 1H), 0.85 (s, 3H), 0.61 (s, 3H). 8H of piperidine were not resolved. LCMS (M+H) = 567.5
As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.
Reference：
Patent; VIIV HEALTHCARE UK (NO.5) LIMITED; KADOW, John F.; NAIDU, B. Narasimhulu; PATEL, Manoj; SIVAPRAKASAM, Prasanna; (60 pag.)WO2017/6260; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics