Category: 98977-34-5

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.98977-34-5,1-tert-Butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.,98977-34-5

1 -(1 , 1 -Dimethylethyl) 3-ethyl 4-oxo-1 ,3-piperidinedicarboxylate (Intermediate 1 , 380.48 g, 1.40 moles) was dissolved in toluene (2.97 Kg). The solution was stirred for 10 mins and then cooled to -7 0C and then treated with N,N-diisopropylethylamine (271.56 g, 2.10 mol) while maintaining the reaction below -7 0C. After stirring the reaction mixture for approximately 10 minutes, trifluoromethanesulfonic anhydride (436.29 g, 1.55 mol) was added while maintaining the temperature below 5 0C. The reaction mixture was stirred at 1 0C for 31 minutes. The product was used in the next step without purification (see preparation of Intermediate 3); HPLC: Rt= 2.69 min (HPLC instrument Agilent 1 100 Series analysis performed on a Agilent Zorbax SB C18 (50×3.0 mm, 1.8um), mobile phase: water:acetonitrile:TFA (0.05%), gradient from 0 to 95% in 2.5 min, hold for 0.2 min, then re-equilibrate; T=60; flow= 1.5 mL/min)

The synthetic route of 98977-34-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2009/109608; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

98977-34-5,98977-34-5, 1-tert-Butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

NaH 60percent in oil (0.62g, 15.48mmol) was added portionwise to a solution of 1,3-(4-oxo-piperidine)-dicarboxylic acid, 1-(1,1-dimethylethyl) 3-ethyl ester (2g, 7.37mmol) suspended in THF (20ml) cooled at 0¡ãC. The mixture was stirred for 30 minutes at 0¡ãC and then allowed to warm to ambient temperature and stirred for a further 1 hour. 3- fluorobenzylbromide (1.36ml, 11.06mmol) was added and the resulting solution was stirred at room temperature overnight. Water and then EtOAc were added. The organic layer was extracted, washed with brine, dried over MgS04, filtrered and concentrated. The residue (2.78g) was purified by Normal phase on irregular SiOH (15-40muiotaeta, 300g); mobile phase (85percent heptane, 15percent EtOAc). The pure fractions were collected and the solvent was evaporated, yielding lg (35.7percent) of intermediate 88.

As the paragraph descriping shows that 98977-34-5 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; GUILLEMONT, Jerome, Emile, Georges; MOTTE, Magali, Madeleine, Simone; LANCOIS, David, Francis, Alain; THOMAS, Sebastien, Robert, Gaston; BALEMANS, Wendy, Mia, Albert; WO2013/160431; (2013); 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.98977-34-5,1-tert-Butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

98977-34-5, To a stirred solution of 4-oxo-piperidine-1 ,3-dicarboxylic acid 1-tert-butyl ester 3-ethyl ester (14 g) in MeOH (300 mL) was added NaBhU (12 g) in 12 lots over 1 h period. After completion of addition, the reaction mixture was stirred for 30 min. Removed solvent under reduced pressure, to the residue was added saturated NH4CI solution (300 mL) and was extracted with EtOAc (300 mL). The organic layer was dried, filtered and concentrated under reduced pressure. The residue was purified by flash silica gel column chromatography by eluting with ethyl acetate to give 4-hydroxy-3-hydroxymethyl- piperidine-1-carboxylic acid tert-butyl ester (10.1 g, cis/trans mixture).

As the paragraph descriping shows that 98977-34-5 is playing an increasingly important role.

Reference£º
Patent; TRANSTECH PHARMA, INC.; GOHIMUKKULA, Devi, Reddy; JONES, David; QABAJA, Ghassan; ZHU, Jeff, Jiqun; COOPER, Jeremy, T.; BANNER, William, Kenneth; SUNDERMANN, Kurt; BONDLELA, Muralidhar; RAO, Mohan; WANG, Pingzhen; GOWDA, Raju, Bore; ANDREWS, Robert, C.; GUPTA, Suparna; HARI, Anitha; WO2011/103091; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

98977-34-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.98977-34-5,1-tert-Butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

1-(tert-Butyl) 3-ethyl 4-oxopiperidine-1,3-dicarboxylate (10 g, 36.86 mmol) was suspended in EtOH (200 mL) and cooled to 0¡ãC under a nitrogen atmosphere. Sodiumborohydride (0.7 g, 18.43 mmol) was then added portionwise over 15 minutes and the reaction mixture was stirred for 0.5 h at 25¡ãC. The mixture was evaporated to dryness, the residue was partitioned between EtOAc (200 mL) and saturated aqueous sodium bicarbonate solution (200 mL), then the aqueous layer was washed with EtOAc (2 x 100 mL). The combined organic layers were washed with brine (200 mL), dried overmagn1-(tert-Butyl) 3-ethyl 4-oxopiperidine-1,3-dicarboxylate (10 g, 36.86 mmol) was suspended in EtOH (200 mL) and cooled to 0¡ãC under a nitrogen atmosphere. Sodiumborohydride (0.7 g, 18.43 mmol) was then added portionwise over 15 minutes and the reaction mixture was stirred for 0.5 h at 25¡ãC. The mixture was evaporated to dryness, the residue was partitioned between EtOAc (200 mL) and saturated aqueous sodium bicarbonate solution (200 mL), then the aqueous layer was washed with EtOAc (2 x 100 mL). The combined organic layers were washed with brine (200 mL), dried overmagnesium sulfate and concentrated. The residue was purified by FCC, eluting with 0-100percent EtOAc in heptane, to afford the title compound (7.26 g, 85percent) as a clear yellow oil.OH (500 MHz, CDC13) 4.32-4.25 (m, 1H), 4.19 (q, J7.12 Hz, 2H), 4.13-3.85 (m, 1H), 3.71(dt, J 13.35, 3.62 Hz, 1H), 3.51-3.34 (m, 1H), 3.21-2.82 (m, 1H), 2.67-2.56 (m, 1H), 1.89-1.76 (m, 1H), 1.73-1.60 (m, 1H), 1.46 (s, 9H), 1.28 (t,J7.17 Hz, 3H).esium sulfate and concentrated. The residue was purified by FCC, eluting with 0-100percent EtOAc in heptane, to afford the title compound (7.26 g, 85percent) as a clear yellow oil.OH (500 MHz, CDC13) 4.32-4.25 (m, 1H), 4.19 (q, J7.12 Hz, 2H), 4.13-3.85 (m, 1H), 3.71(dt, J 13.35, 3.62 Hz, 1H), 3.51-3.34 (m, 1H), 3.21-2.82 (m, 1H), 2.67-2.56 (m, 1H), 1.89-1.76 (m, 1H), 1.73-1.60 (m, 1H), 1.46 (s, 9H), 1.28 (t,J7.17 Hz, 3H).

The synthetic route of 98977-34-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; UCB PHARMA S.A.; BENTLEY, Jonathan Mark; BROOKINGS, Daniel Christopher; BROWN, Julien Alistair; CAIN, Thomas Paul; CHOVATIA, Praful Tulshi; FOLEY, Anne Marie; GALLIMORE, Ellen Olivia; GLEAVE, Laura Jane; HEIFETZ, Alexander; HORSLEY, Helen Tracey; HUTCHINGS, Martin Clive; JACKSON, Victoria Elizabeth; JOHNSON, James Andrew; JOHNSTONE, Craig; KROEPLIEN, Boris; LECOMTE, Fabien Claude; LEIGH, Deborah; LOWE, Martin Alexander; MADDEN, James; PORTER, John Robert; QUINCEY, Joanna Rachel; REED, Laura Claire; REUBERSON, James Thomas; RICHARDSON, Anthony John; RICHARDSON, Sarah Emily; SELBY, Matthew Duncan; SHAW, Michael Alan; ZHU, Zhaoning; WO2014/9295; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem