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.
2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (2.314 g, 12.14 mmol) was dissolved in dichloromethane (50 ml_), and triethylamine (8 ml_, 57.4 mmol) was added. The reaction mixture was cooled to 0 C and 4- (trifluoromethyl)benzenesulfonyl chloride (3.27 g, 13.35 mmol) was added. After 2 h, the reaction mixture was washed with aqueous 1 M HCI followed by aqueous 1 M NaOH, the organic layer was passed through a hydrophobic frit, and concentrated in vacuo. The resulting residue was purified by silica column chromatography on SP4 (gradient elution: 0 – 20% DCM – MeOH). The early colourless fractions led to 7-{[4- (trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (360 mg, 0.984 mmol, 8% yield) as a white solid. The later orange fractions were combined, and concentrated in vacuo. The resulting residue was recrystallised from methanol to give 3 batches of white crystals: 1 st batch 7-{[4-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one (1 .506 g, 4.1 1 mmol, 33% yield), 2nd batch 7-{[4- (trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (400 mg, 1 .093 mmol, 9% yield), and 3rd batch 7-{[4-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one (324 mg, 0.885 mmol, 7% yield). 1 H NMR (250 MHz, DMSO-d6) 5 ppm 1.31 – 1.76 (m, 4 H) 2.00 (qt, J=13.25, 6.60 Hz, 2 H) 2.18 – 2.32 (m, 2 H) 3.20 (t, J=6.86 Hz, 2 H) 3.34 (d, J=1 1 .49 Hz, 1 H) 3.64 (d, J=1 1 .59 Hz, 1 H) 7.77 (s, 1 H) 7.96 (d, J=8.37 Hz, 2 H) 8.04 (d, J=8.44 Hz, 2 H). MS ES+ve m/z 363 (M+H).
1187173-43-8, 1187173-43-8 2,7-Diazaspiro[4.5]decan-1-one hydrochloride 45074126, apiperidines compound, is more and more widely used in various fields.
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