1187173-43-8 | Page 2 of 3 | Heterocyclic Building Blocks-piperidine

Some tips on 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (80 mg, 0.420 mmol) was dissolved in dichloromethane (4 mL) and triethylamine (0.1 17 mL, 0.839 mmol) before the addition of 3-(trifluoromethyl)benzenesulfonyl chloride (1 13 mg, 0.462 mmol). After stirring for 20 h the reaction mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-{[3-(trifluoromethyl)phenyl]sulfonyl}- 2,7-diazaspiro[4.5]decan-1 -one (60 mg, 0.162 mmol, 39% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .35 – 1.46 (m, 2 H) 1.51 – 1.64 (m, 1 H) 1.66 – 1 .74 (m, 1 H) 1.90 – 1.98 (m, 1 H) 2.00 – 2.09 (m, 1 H) 2.20 – 2.31 (m, 2 H) 3.12 – 3.24 (m, 2 H) 3.37 (d, J=1 1 .40 Hz, 1 H) 3.67 (d, J=1 1 .24 Hz, 1 H) 7.76 (s, 1 H) 7.92 (t, J=7.87 Hz, 1 H) 7.98 (s, 1 H) 8.08 (d, J=7.95 Hz, 1 H) 8.14 (d, J=7.84 Hz, 1 H). MS ES+ve m/z 363 (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

Analyzing the synthesis route of 1187173-43-8

1187173-43-8, As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2,7-diazaspiro[4.5]decan-1 -one hydrochloride (0.572 g, 3mmol) and triethylamine (0.836 mL, 6.00 mmol) in dichloromethane (DCM) (15ml_), cooled in an ice-water bath, was added 4-bromo-2-(trifluoromethyl)benzenesulfonyl chloride (0.971 g, 3.00 mmol). The reaction was allowed to warm to room temperature and stirred for 18 hours.The reaction was diluted with DCM (35 ml), washed with water (30ml_), passed through a hydrophobic frit and reduced in vacuo. The residue was purified by silica chromatography (Biotage SP4) eluting with 60% EtOAc in iso-hexanes (3 column volumes), a gradient from 60-100% EtOAc (over 9 column volumes) then EtOAc (3 column volumes) to yield 7-{[4-bromo-2-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one as a white solid (0.826g, 62%)1H NMR (400 MHz, Chloroform-d) d ppm 1.61 – 1 .67 (m, 1 H) 1.69 – 1 .84 (m, 3 H) 2.05 (s, 1 H) 2.43 (s, 1 H) 2.59 – 2.67 (m, 1 H) 2.85 (d, J=12.7 Hz, 1 H) 3.32 – 3.45(m, 2 H) 3.67 (d, J=12.5 Hz, 1 H) 3.80 – 3.87 (m, 1 H) 5.72 (br. s., 1 H) 7.80 – 7.88 (m, 2 H) 8.01 (d, J=1.5 Hz, 1 H)

1187173-43-8, As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

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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.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 47: 7-[bis(4-fluorophenyl)methyl]-2,7-diazaspiro[4,5]decan-1-one (P47)Chlorobis(4-fluorophenyl)methane (0.174 m L, 0.934 mmol) was added to a stirred mixture of 2,7- diazaspiro[4.5]decan-l-one hydrochloride salt (0.15 g, 0.78 mmol) and K2C03(0.27 g, 1.95 mmol) in Acetonitrile (3 m L). The mixture was stirred for 3 hrs at reflux. The solution was diluted with EtOAc and water. The organic phase was dried and evaporated. The residue was purified by FC on silica gel (eluent: cHex to EtOAc) to afford 7-[bis(4-fluorophenyl)methyl]-2,7-diazaspiro[4.5]decan-l-one (p47, 165 mg, y= 59%) as white foam .MS (ES) (m/z): 357.2 [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; SHIRE INTERNATIONAL GMBH; SEMERARO, Teresa; TARSI, Luca; MICHELI, Fabrizio; LUKER, Tim; CREMONESI, Susanna; (122 pag.)WO2016/42451; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

Downstream synthetic route of 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.

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 (100 mg, 0.524 mmol) was dissolved in dichloromethane (10 mL) and triethylamine (0.219 mL, 1 .573 mmol). Then, 3-fluoro-5-(trifluoromethyl)benzenesulfonyl chloride (165 mg, 0.629 mmol) was added and stirred for 17 h. The mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-{[3-fluoro-5-(trifluoromethyl)phenyl]sulfonyl}- 2,7-diazaspiro[4.5]decan-1 -one (87.9 mg, 0.226 mmol, 43% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1.39 – 1 .49 (m, 2 H) 1.52 – 1 .64 (m, 1 H) 1.66 – 1 .75 (m, 1 H) 1.87 – 1.97 (m, 1 H) 1.99 – 2.09 (m, 1 H) 2.29 – 2.41 (m, 2 H) 3.14 – 3.24 (m, 2 H) 3.41 (d, J=1 1 .73 Hz, 1 H) 3.68 (d, J=1 1 .89 Hz, 1 H) 7.76 (s, 1 H) 7.84 (s, 1 H) 8.01 (d, J=7.84 Hz, 1 H) 8.16 (d, J=8.55 Hz, 1 H). MS ES+ve m/z 381 (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.

Brief introduction of 1187173-43-8

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Preparation 44: tert-butyl 1-oxo-2,7-diazaspiro[4,5]decane-7-carboxylate (P44)2,7-diazaspiro[4.5]decan-l-one hydrochloride (600 mg, 3.15 mmol), was dissolved in 30 m L of DCM. To this solution, TEA (1.98 mL, 14.18 mmol) and Boc20 (895 mg, 4.10 mmol) were added and the reaction mixture was stirred at RT for 4 hrs. Water was added and the two layers were separated; the organic layer was washed with NH4CI, dried and evaporated to obtain ferf-butyl l-oxo-2,7- diazaspiro[4.5]decane-7-carboxylate (p44, 830 mg, y= quant.), colourless oil.MS (ES) (m/z): 255.2 [M+H]+.

1187173-43-8, As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

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1187173-43-8 2,7-Diazaspiro[4.5]decan-1-one hydrochloride 45074126, apiperidines compound, is more and more widely used in various fields.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (80 mg, 0.420 mmol) was dissolved in dichloromethane (4 ml_). Then, triethylamine (0.1 17 ml_, 0.839 mmol) was added followed by 4-[(trifluoromethyl)oxy]benzenesulfonyl chloride (0.078 ml_, 0.462 mmol). After stirring for 20 h the reaction mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-({4-[(trifluoromethyl)oxy]- phenyl}sulfonyl)-2,7-diazaspiro[4.5]decan-1 -one (93 mg, 0.241 mmol, 57% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1.34 – 1 .47 (m, 2 H) 1.51 – 1 .64 (m, 1 H) 1.66 – 1.73 (m, 1 H) 1.90 – 1 .99 (m, 1 H) 2.00 – 2.08 (m, 1 H) 2.18 – 2.26 (m, 2 H) 3.19 (t, J=6.91 Hz, 2 H) 3.30 (s, 1 H) 3.62 (d, J=1 1 .35 Hz, 1 H) 7.64 (dd, J=8.85, 0.90 Hz, 2 H) 7.76 (s, 1 H) 7.86 – 7.90 (m, 2 H). MS ES+ve m/z 379 (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.

Simple exploration of 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

To a solution of 2,7-diazaspiro[4.5]decan-1 -one hydrochloride (0.572 g, 3 mmol) and triethylamine (0.836 mL, 6.00 mmol) in dichloromethane (15 mL), cooled in an ice- water bath, was added 4-bromo-2-[(trifluoromethyl)oxy]benzenesulfonyl chloride (1 .019 g, 3.00 mmol). The reaction was allowed to warm to room temperature and stirred for 18 hours. The reaction was diluted with dichloromethane (35 mL), washed with water (30 mL), passed through a hydrophobic frit and reduced in vacuo. The residue was purified by silica chromatography (Biotage SP4) eluting with 60% EtOAc in /’so-hexanes (3 column volumes), a gradient from 60 – 100% EtOAc (over 9 column volumes) then EtOAc (3 column volumes) to yield 7-({4-bromo-2-[(trifluoromethyl)oxy]phenyl}sulfonyl)-2,7-diazaspiro[4.5]decan-1 -one (0.936 g, 2.047 mmol, 68% yield) as a white solid. 1 H NMR (400 MHz, CHLOROFORM-d) delta ppm 1 .60 – 1 .82 (m, 4 H) 1.99 – 2.09 (m, 1 H) 2.43 (ddd, J=13.17, 8.18, 4.80 Hz, 1 H) 2.55- 2.65 (m, 1 H) 2.72 (dd, J=12.30, 0.96 Hz, 1 H) 3.30 – 3.46 (m, 2 H) 3.57 (dt, J=12.28, 1 .92 Hz, 1 H) 3.89 (ddd, J=12.32, 3.85, 1.81 Hz, 1 H) 5.68 (br. s., 1 H) 7.51- 7.59 (m, 2 H) 7.83 (d, J=8.71 Hz, 1 H). MS ES+ve m/z 459 (M+H)., 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

Brief introduction of 1187173-43-8

As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (100 mg, 0.524 mmol) was dissolved in dichloromethane (5 mL) and triethylamine (0.146 mL, 1 .047 mmol). Then 3-[(trifluoromethyl)oxy]benzenesulfonyl chloride (0.098 mL, 0.577 mmol) was added and stirred for 16 h. The reaction mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-({3-[(trifluoromethyl)oxy]phenyl}- sulfonyl)-2,7-diazaspiro[4.5]decan-1 -one (85 mg, 0.222 mmol, 42% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .32 – 1 .48 (m, 2 H) 1.50 – 1 .64 (m, 1 H) 1 .65 – 1 .75 (m, 1 H) 1.89 – 1 .98 (m, 1 H) 1.99 – 2.09 (m, 1 H) 2.18 – 2.28 (m, 2 H) 3.19 (t, J=7.10 Hz, 2 H) 3.30 – 3.37 (m, 1 H) 3.65 (d, J=1 1 .62 Hz, 1 H) 7.69 (s, 1 H) 7.73 – 7.85 (m, 4 H). MS ES+ve m/z 379 (M+H).

As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

New learning discoveries about 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.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (150 mg, 0.787 mmol) was dissolved in dichloromethane (4 mL) and triethylamine (0.219 mL, 1.573 mmol), and 2-chloro-4-(trifluoromethyl)benzenesulfonyl chloride (241 mg, 0.865 mmol) was added. After stirring for 18 h, the reaction mixture was concentrated in vacuo. The resulting residue was purified by MDAP to give 7-{[2-chloro-4-(trifluoromethyl)- phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (38.2 mg, 0.094 mmol, 12% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .37 – 1 .64 (m, 3 H) 1.65 – 1 .75 (m, 1 H) 1.84 – 2.02 (m, 2 H) 2.72 – 2.83 (m, 2 H) 3.09 – 3.18 (m, J=7.78, 7.51 Hz, 2 H) 3.40 (d, J=12.1 1 Hz, 1 H) 3.72 (d, J=12.93 Hz, 1 H) 7.74 (s, 1 H) 7.93 (d, J=9.54 Hz, 1 H) 8.18 (d, J=7.45 Hz, 2 H). MS ES+ve m/z 397 (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.

Some tips on 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (100 mg, 0.524 mmol) was dissolved in dichloromethane (10 mL) and triethylamine (0.219 mL, 1 .573 mmol), and 2,5-bis(trifluoromethyl)benzenesulfonyl chloride (197 mg, 0.629 mmol) was added. After stirring for 17 h the reaction mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-{[2,5-bis(trifluoromethyl)phenyl]- sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (96 mg, 0.221 mmol, 42% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .46 – 1 .63 (m, 3 H) 1.66 – 1 .75 (m, 1 H) 1 .85 – 2.03 (m, 2 H) 2.72 – 2.78 (m, 1 H) 2.80 (d, J=12.28 Hz, 1 H) 3.1 1 – 3.19 (m, 2 H) 3.47 (d, J=12.28 Hz, 1 H) 3.71 (d, J=1 1 .78 Hz, 1 H) 7.75 (s, 1 H) 8.24 (s, 1 H) 8.26 – 8.33 (m, 2 H). MS ES+ve m/z 431 (M+H)., 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.