With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1187173-43-8,2,7-Diazaspiro[4.5]decan-1-one hydrochloride,as a common compound, the synthetic route is as follows.
7-{[2-Methyl-5-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one (2,7-Diazaspiro[4.5]decan-1 -one (200 mg, 1.297 mmol) was dissolved in a mixture of triethylamine (0.542 mL, 3.89 mmol) and dichloromethane (10 mL), and 2-bromo-5- (trifluoromethyl)benzenesulfonyl chloride (503 mg, 1 .556 mmol) was added. The reaction mixture was stirred for 16 h and the reaction mixture was concentrated in vacuo. The resulting yellow solid 7-{[2-bromo-5-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one (829 mg, impure) was used in the next reaction without further purification. MS ES+ve m/z 443 (M+H).7-{[2-Bromo-5-(trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (829 mg, impure) and potassium carbonate (269 mg, 1.946 mmol) was suspended in 1 ,4- dioxane (20 mL). Trimethylboroxine (0.271 mL, 1.946 mmol) and Pd(PPh3)4 (150 mg, 0.130 mmol) were then added and the reaction mixture was heated to 100 C. After 20 h, the reaction was cooled, filtered through a hydrophobic frit, and concentrated in vacuo. The resulting residue was purified by silica column chromatography on SP4 (gradient elution: 0 – 20% MeOH – DCM). The resulting brown residue was further purified on MDAP to give 7-{[2-methyl-5-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one (152 mg, 0.400 mmol, 31 % yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .52 (s, 3 H) 1.63 – 1 .76 (m, 1 H) 1 .91 (t, J=6.88 Hz, 2 H) 2.56 – 2.72 (m, 5 H) 3.04 – 3.20 (m, 2 H) 3.34 – 3.37 (m, 1 H) 3.62 (d, J=1 1 .62 Hz, 1 H) 7.69 – 7.76 (m, 2 H) 7.98 (d, J=8.00 Hz, 1 H) 8.01 (s, 1 H). MS ES+ve m/z 377 (M+H).
1187173-43-8, The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; GLEAVE, Robert James; HACHISU, Shuji; PAGE, Lee William; BESWICK, Paul John; WO2011/141728; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem