Category: 1187173-43-8

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.,1187173-43-8

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-3-(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 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 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-3- (trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (1.022 g, 2.316 mmol, 77% yield) as a white solid. 1 H NMR (250 MHz, CHLOROFORM-d) delta ppm 1 .59 – 1 .86 (m, 4 H) 2.00 – 2.14 (m, 1 H) 2.24 – 2.51 (m, 3 H) 3.31 – 3.51 (m, 2 H) 3.52 – 3.60 (m, 1 H) 3.86 (dd, J=10.39, 1.96 Hz, 1 H) 5.67 (br. s., 1 H) 7.72 (dd, J=8.30, 1 .92 Hz, 1 H) 7.90 (d, J=8.37 Hz, 1 H) 8.02 (d, J=2.13 Hz, 1 H). MS ES+ve m/z 443 (M+H).

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

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

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 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

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

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

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.,1187173-43-8

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 3,5-bis(trifluoromethyl)benzenesulfonyl chloride (144 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-{[3,5-bis(trifluoromethyl)phenyl]- sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (14 mg, 0.032 mmol, 8% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .32 – 1 .63 (m, 3 H) 1.66 – 1 .76 (m, 1 H) 1 .87 – 1 .97 (m, 1 H) 2.00 – 2.08 (m, 1 H) 2.35 – 2.47 (m, 2 H) 3.15 – 3.24 (m, 2 H) 3.47 (d, J=1 1 .45 Hz, 1 H) 3.71 (d, J=1 1 .67 Hz, 1 H) 7.75 (s, 1 H) 8.32 (s, 2 H) 8.55 (s, 1 H). MS ES+ve m/z 431 (M+H).

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

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

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 (150 mg, 0.973 mmol) was dissolved in a mixture of triethylamine (0.542 mL, 3.89 mmol) and dichloromethane (10 mL), and 3-chloro-4- [(trifluoromethyl)oxy]benzenesulfonyl chloride (344 mg, 1.167 mmol) was added. After 16 h the reaction mixture was concentrated in vacuo and the resulting residue was purified by silica column chromatography on SP4 (gradient elution: 0 – 20% MeOH – DCM) to give 7-({3-chloro-4-[(trifluoromethyl)oxy]phenyl}sulfonyl)-2,7- diazaspiro[4.5]decan-1 -one (350 mg, 0.839 mmol, 86% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .37 – 1.49 (m, 2 H) 1.49 – 1.65 (m, 1 H) 1.65 – 1 .76 (m, 1 H) 1.88 – 2.08 (m, 2 H) 2.27 – 2.40 (m, 2 H) 3.19 (t, J=6.63 Hz, 2 H) 3.36 (d, J=1 1 .51 Hz, 1 H) 3.64 (d, J=1 1 .62 Hz, 1 H) 7.77 (s, 1 H) 7.80 – 7.87 (m, 2 H) 8.06 (dd, J=1.59, 0.82 Hz, 1 H). MS ES+ve m/z 413 (M+H)., 1187173-43-8

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

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

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.

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 3-bromo-5-(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 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 iso- hexanes (3 column volumes), a gradient from 60 – 100% EtOAc (over 9 column volumes) then EtOAc (3 column volumes) to yield 7-{[3-bromo-5- (trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (798 mg, 1 .808 mmol, 60% yield) as a white solid. 1 H NMR (400 MHz, CHLOROFORM-d) delta ppm 1 .61 – 1 .88 (m, 4 H) 2.01 – 2.1 1 (m, 1 H) 2.35 (td, J=1 1 .37, 3.45 Hz, 1 H) 2.43 (td, J=8.69, 4.1 1 Hz, 1 H) 2.48 (dd, J=1 1 .48, 0.96 Hz, 1 H) 3.34 – 3.50 (m, 2 H) 3.57 (dt, J=1 1 .51 , 1 .78 Hz, 1 H) 3.89 (dd, J=1 1 .65, 1.56 Hz, 1 H) 5.77 (br. s., 1 H) 7.89 – 7.92 (m, 1 H) 7.99 (d, J=0.55 Hz, 1 H) 8.04 (t, J=1.45 Hz, 1 H). MS ES+ve m/z 441 (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

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 (90 mg, 0.584 mmol) was dissolved indichloromethane (10 mL) and triethylamine (0.163 ml_, 1 .167 mmol), and 3,5- dichlorobenzenesulfonyl chloride (158 mg, 0.642 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-[(3,5-dichlorophenyl)sulfonyl]-2,7-diazaspiro[4.5]decan-1 – one (130.5 mg, 0.352 mmol, 60% yield) as a white solid. 1 H NMR (400 MHz, DMSO- d6) delta ppm 1 .35 – 1 .50 (m, 2 H) 1.50 – 1 .65 (m, 1 H) 1.65 – 1 .76 (m, 1 H) 1.87 – 1 .98 (m, 1 H) 1.98 – 2.09 (m, 1 H) 2.30 (d, J=1 1 .56 Hz, 1 H) 2.33 – 2.41 (m, 1 H) 3.12 – 3.24 (m, 2 H) 3.38 (d, J=1 1.51 Hz, 1 H) 3.65 (d, J=1 1 .51 Hz, 1 H) 7.69 – 7.82 (m, 3 H) 8.04 (t, J=1.89 Hz, 1 H). MS ES+ve m/z 363 (M+H)., 1187173-43-8

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

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

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 (430 mg, 2.255 mmol) was dissolved in dichloromethane (4 mL), and triethylamine (0.628 mL, 4.53 mmol) was added followed by 2-bromo-4-(trifluoromethyl)benzenesulfonyl chloride (804 mg, 2.484 mmol). After stirring for 20 h the reaction mixture was concentrated in vacuo. The resulting residue was redissolved in EtOAc, washed with aqueous 1 M HCI followed by washing by saturated aqueous Na2C03. The organic layer was passed through a hydrophobic frit, concentrated in vacuo and recrystallised from methanol to give 7-{[2-bromo-4-(trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (395 mg, 0.877 mmol, 38% yield). The mother liquor was concentrated in vacuo to give the following impure material: 7-{[2-bromo-4-(trifluoromethyl)phenyl]sulfonyl}- 2,7-diazaspiro[4.5]decan-1 -one (419 mg, 0.548 mmol, 57.7% purity by mass, 24% yield), a mixture of desired product and 2-bromo-4-(trifluoromethyl)benzenesulfonyl chloride (1 :1 by molar equivalence). 1 H NMR (400 MHz, DMSO-c/6) delta ppm 1.46 – 1 .63 (m, 3 H) 1.65 – 1.74 (m, 1 H) 1.87 – 1.99 (m, 2 H) 2.74 – 2.80 (m, 1 H) 2.83 (d, J=12.50 Hz, 1 H) 3.05 – 3.20 (m, 2 H) 3.43 (d, J=12.39 Hz, 1 H) 3.72 (d, J=1 1.40 Hz, 1 H) 7.74 (s, 1 H) 7.97 (dd, J=8.28, 1.21 Hz, 1 H) 8.18 (d, J=8.00 Hz, 1 H) 8.29 (d, J=1.15 Hz, 1 H). MS ES+ve m/z 441 (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

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.

To a solution of 2,7-diazaspiro[4.5]decan-1-one hydrochloride (1.0 g, 5.26 mmol) in DCM (10 mL), benzaldehyde (0.53 mL, 5.26 mmol) was added and the mixture was stirred at RT for 15 mm, then NaBH(OAc)3 (1.67 g, 7.89 mmol) was added and the mixture was left stirring at RT overnight. Thereaction was quenched with saturated NaHCO3 solution, then phases were separated and aqueous one was backextracted with DCM twice. Combined organics were washed with brine, dried and concentrated under reduced pressure. Crude material was purified by FC on NH column (eluent: Cy to 50% AcOEt) affording 7-benzyl-2,7-diazaspiro[4.5]decan-1-one (p139, 890 mg, y= 69%) as white solid. MS (ES) (m/z): 245.2 [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; SHIRE INTERNATIONAL GMBH; CREMONESI, Susanna; LUKER, Tim; SEMERARO, Teresa; MICHELI, Fabrizio; (257 pag.)WO2016/42452; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

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

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