Brief introduction of 5382-16-1

5382-16-1 4-Piperidinol 79341, 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.5382-16-1,4-Piperidinol,as a common compound, the synthetic route is as follows.,5382-16-1

b. 1-(Carbobenzyloxy)piperidin-4-ol A solution of 4-hydroxypiperidine (25.0 g, 0.247 mol) in methylene chloride (2000 mL) was cooled to 0 C. under nitrogen with overhead stirring. Triethylamine (86.1 mL, 0.618 mol, 2.5 eq) was added followed by benzyl chloroformate (35.3 mL, 0.247 mol, 1.0 eq). The reaction was warmed to room temperature over 1 h and maintained at this temperature for 5 h. A significant amount of amine hydrochloride precipitates in the course of the procedure. The organic phase was washed with 3N HCl (3*250 mL), dried over anhydrous sodium sulfate and filtered. The solvent was removed in vacuo to yield 47.0 g (81%) of the title compound as an oil. The product did not require any addition purification prior to the Swern oxidation. TLC analysis (Rf 0.17, 50% ethyl acetate in hexane). MS (CI, CH4) m/z 236 (M+1,42), 218 (4), 192 (10), 181 (9), 174 (15), 91 (100).

5382-16-1 4-Piperidinol 79341, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Zeneca Limited; US5512575; (1996); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Analyzing the synthesis route of 5382-16-1

As the paragraph descriping shows that 5382-16-1 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5382-16-1,4-Piperidinol,as a common compound, the synthetic route is as follows.

Example 2 Preparation of 4-Hydroxy-Piperidine-1-Carboxylic Acid Isopropyl Ester Intermediate (2) To a stirred mixture of 4-hydroxypiperidine (53.8 g, 1.000 eq), triethylamine (71.8 g, 1.334 equivalents), and ethyl acetate (498.8 g) was added neat isopropyl chloroformate (78.0 g, 1.1966 equivalents) at a rate sufficiently slow to maintain the reaction mixture temperature at 10-17 C. with reactor jacket cooling. After the addition had been completed, the reaction mixture was stirred at 20 C. for 18 hours. Then water (100 g) was added, and the resulting mixture was stirred for 15 minutes before the phases were separated. The organic phase was washed with two 100-gram-portions of 20 wt % aqueous NaCl by stirring for 15 min at 150 rpm before separating the aqueous wash. After a final wash with water (100 g), the organic phase was concentrated by distillation on a rotary evaporator at reduced pressure to provide product (2) (91.1 g, 92.0% yield) as light amber oil of 96.8% purity by GC.

As the paragraph descriping shows that 5382-16-1 is playing an increasingly important role.

Reference£º
Patent; Gharbaoui, Tawfik; Fritch, John R.; Krishnan, Ashwin M.; Throop, Beverly Wolgast; Kato, Naomi S.; US2006/155129; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Brief introduction of 5382-16-1

The synthetic route of 5382-16-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5382-16-1,4-Piperidinol,as a common compound, the synthetic route is as follows.

4-chloronitrobenzene (31.5 g, 200 mmol) was dissolved in N,N-dimethylacetamide (80 ml), and potassium carbonate (35.9 g, 260 mmol) and 4-hydroxypiperidine (22.3 g, 220 mmol) were added thereto, followed by stirring under heat at 130 C. for 3 hours. After cooling to room temperature, water was added to the mixture, and the precipitate was collected by filtration. The obtained solid was dried under reduced pressure, thereby obtaining 4-hydroxy-N-(4-nitrophenyl)piperidine (41.3 g, 93%) as a yellow solid.1H-NMR (CDCl3): delta (ppm) 1.52-1.74 (m, 2H), 1.92-2.04 (m, 2H), 3.14-3.35 (m, 2H), 3.73-4.08 (m, 3H), 6.82 (d, J=9.6 Hz, 2H), 8.11 (d, J=9.6 Hz, 2H)

The synthetic route of 5382-16-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TAIHO PHARMACEUTICAL CO., LTD.; US2011/319413; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Brief introduction of 5382-16-1

The synthetic route of 5382-16-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5382-16-1,4-Piperidinol,as a common compound, the synthetic route is as follows.

Step: 3A-1Synthesis of l-(4-Nitro-phen -piperidin-4-ol.Procedure:K2C03 (2.44g, 0.0177mol) followed by l-Fluoro-4-nitro-benzene (lg, 0.00708mol) was added to a stirred solution of Piperidin-4-ol (0.86g, 0.00850mol) in DMF (5ml) and stirred at RT. The resulting reaction mixture was heated at 60C. The reaction was monitored by the TLC (50% EtOAc: hexane). The reaction mixture was cooled to RT, and ice was added into it to precipitate a solid which was collected to afford 1.45g (92% yield) of l-(4- Nitro-phenyl)-piperidin-4-ol.

The synthetic route of 5382-16-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AURIGENE DISCOVERY TECHNOLOGIES LIMITED; SENGUPTA, Saumitra; RAJAGOPALAN, Srinivasan; BELAVAGI, Ningaraddi; RAMACHANDRA, Muralidhara; WO2012/59932; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Simple exploration of 5382-16-1

5382-16-1 4-Piperidinol 79341, apiperidines compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5382-16-1,4-Piperidinol,as a common compound, the synthetic route is as follows.

REFERENCE EXAMPLE 6 Synthesis of 1-amino-4-hydroxypiperidine In 10 ml of water was dissolved 0.6 g(6 mmol) of hydroxylamine-O-sulfonic acid and 1.82 g(1.8 mmol) of 4-hydroxypiperidine was added thereto. After refluxing for 1 hour, the reaction mixture was cooled to 5 C. and 0.84 g(6.1 mmol) of potassium carbonate was added thereto. The reaction mixture was stirred for 10 min and the precipitate was filtered off. The filtrate was concentrated under the reduced pressure and 15 ml of dry ethanol was added to give precipitate, which was filtered off. While cooling the filtrate to 5~10 C., 0.85 ml of 57% HI was slowly added and the mixture was stirred at the same temperature for 30 min. To the reaction mixture was added 50 ml of petroleum ether. The filtrate was washed with acetone to give 1.41 g of the desired compound(34%). m.p.=117-119 C. NMR (DMSO-d6, delta) 1.12~1.98 (m, 4H), 2.41~2.86 (m, 2H) 2.86~3.24 (m, 2H), 3.40~3.79 (m, 1H) 5.23 (br, 2H, NH2)

5382-16-1 4-Piperidinol 79341, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Dae Woong Pharmaceutical Co., Ltd.; US5336673; (1994); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem