Month: March 2022

3612-20-2, 1-Benzylpiperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1 -Benzyl-4-piperidone (1.89 g, 10 mmol) was dissolved in 15 ml acetone. Methyliodide (0.90 ml, 15 mmol) was slowly added over 5 min. After 2 hrs magnetic stirring additional Methyliodide (1.8 ml, 30 mmol) was added. After 1 hr magnetic stirring 20 ml diethyl-ether was added. Crude product was collected by filtration and washed with acetone/diethyl ether. White crystals were dried under vacuum giving 806 mg quartenary salt. TLC (10% methanol in dichloromethane): Rf =0.7. Partly dissolved salt in 5 ml water was added to 50 C. hot mixture of t-Butylamine (120 mg, 1.6 mmol) and Potassiumcarbonate (32 mg, 0.22 mmol) in 3 ml ethanol. The resulting mixture was stirred and heated to reflux (~80 C.) for 1 hr. After cooling water (20 ml) and dichloromethane (20 ml) were added. Phases were separated and aq. phase was re- extracted with dichloromethane and ethylacetate. Combined organic phases were dried over MgSO4 and concentrated on Rotavapor (40 C.) giving 496 mg 47AKU-47. TLC (10% methanol in dichloromethane): Rf=0.3. 1H-NMR (400 MHz, CDCl3): delta 2.82 (4H31); 2.41 (4H5 t); 1.12 (9H, s). 13C-NMR (CDCl3): delta 210.2, 54.3, 46.4, 42.4, 26.6. Crude product contained ~25% (1H-NMR) starting material (l-Benzyl-4-piperidone)., 3612-20-2

The synthetic route of 3612-20-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ACADIA PHARMACEUTICALS, INC.; WO2007/124136; (2007); 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.61995-20-8,Benzyl 3-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

crude purified product (770 mg) of benzyl 3-oxopiperidine-1-carboxylate, 2,2-dimethylpropan-1-amine (643 mg) and acetic acid (0.5 mL) were dissolved in THF (10 mL), and sodium triacetoxyborohydride (1563 mg) was added at room temperature. The mixture was stirred at room temperature for 1 hr, to the reaction mixture was added water at room temperature, and the mixture was extracted with ethyl acetate. The extract was washed with saturated brine, dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The obtained residue was dissolved in THF (10 mL), di-tert-butyl dicarbonate (1610 mg) and triethylamine (2.57 mL) were added at room temperature, and the mixture was stirred at 60 C. for 6 hr. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (ethyl acetate/hexane) to give the title compound (690 mg) as a colorless oil. (1235) 1H NMR (300 MHz, CDCl3) delta 0.89 (9H, brs), 1.31-1.53 (10H, m), 1.66-1.95 (2H, m), 2.10-3.82 (6H, m), 3.99-4.27 (2H, m), 4.99-5.22 (2H, m), 7.28-7.41 (5H, m)., 61995-20-8

The synthetic route of 61995-20-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; AIDA, Jumpei; YOSHITOMI, Yayoi; HITOMI, Yuko; NOGUCHI, Naoyoshi; HIRATA, Yasuhiro; FURUKAWA, Hideki; SHIBUYA, Akito; WATANABE, Koji; MIYAMOTO, Yasufumi; OKAWA, Tomohiro; TAKAKURA, Nobuyuki; MIWATASHI, Seiji; (199 pag.)US2016/115128; (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.1211587-42-6,Benzyl 4-((chlorosulfonyl)methyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Into a 50-mL round-bottom flask was placed 2-oxo-N-(piperidin-4-yl)-2,3- dihydro-1H-indole-5-carboxamide hydrochloride (80 mg, 0.27 mmol, 1.00 equiv) and NMP (16 mL). This was followed by the addition of TEA (82 mg, 0.81 mmol, 3.00 equiv) dropwise with stirring at 0oC. To this was then added benzyl 4- [(chlorosulfonyl)methyl]piperidine-1-carboxylate (135 mg, 0.41 mmol, 1.50 equiv) in several batches at 0oC. The resulting solution was stirred for 2 h at 20oC. The mixture was concentrated under vacuum. The residue was chromatographed on a silica gel column with dichloromethane/methanol (50:1-20:1). The collected fractions were combined and concentrated under vacuum. This resulted in 100 mg (67%) of benzyl 4- [[4-(2-oxo-2,3-dihydro-1H-indole-5-carboxamido)piperidine-1- sulfonyl]methyl]piperidine-1-carboxylate as a yellow solid

1211587-42-6, The synthetic route of 1211587-42-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Epizyme, Inc.; Poley, Megan Allen Clunan; Kunz, Kevin Wayne; Mills, James Edward John; Mitchell, Lona Helen; munckhof, Michael John; Harvey, Darren Martin; (303 pag.)KR2017/45749; (2017); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

10338-57-5, 4-(Piperidin-1-yl)benzaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A flame-dried sealed tube equipped with exo-cyclic enol ether (0.3mmol) and 18-crown-6 (23.8mg, 0.09mmol) was pumped to vacuum and exchanged with nitrogen for three times. Aldehyde (0.45mmol), solution of t-BuOK in THF (60muL) and DMF (1mL) were then added successively under nitrogen atmosphere. The mixture was stirred at 110C and the reaction was monitored by TLC. After completion of the reaction, the mixture was cooled and concentrated aqueous solution of NH4Cl was added to quench the reaction. The resulting mixture was extracted with CH2Cl2 and the organic phase was washed with concentrated brine and dried over Na2SO4. The solvent was evaporated under reduced pressure, and the residue was passed through column chromatography on silica gel to afford the desired product C., 10338-57-5

The synthetic route of 10338-57-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Shang, Xue Song; Li, Deng Yuan; Li, Nian Tai; Liu, Pei Nian; Dyes and Pigments; vol. 114; C; (2015); p. 8 – 17;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.72551-53-2,Ethyl 1-benzylpiperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

1.71 N-Benzyl-3-[(N-3-methoxyphenyl-N-phenylsulphonyl)aminomethyl] piperidine DIBAL (7.0 mL, 1.5 M in toluene, 10.5 mmol) was added (dropwise along the sides of the flask) to a solution of ethyl 1-benzylpiperidine-3-carboxylate in toluene (from Emka-Chemie, 1.01 g, 4.08 mmol) at -78 C. and the resulting solution was stirred at -78 C. for 3.5 hours. The reaction mixture was quenched by slow addition of ethyl acetate (10 mL) and methanol (5 mL) at -78 C. After 15 min, a solution of potassium sodium tartrate (1 M aqueous) was added and the resulting precipitate was stirred for ~1 hour, further diluted with ethyl acetate and filtered to remove the precipitate. The solvent was removed in vacuo, using methanol to aid azeotropic removal of the toluene at the end, providing 1 -benzylpiperidine-3-carboxaldehyde of sufficient purity for use below., 72551-53-2

As the paragraph descriping shows that 72551-53-2 is playing an increasingly important role.

Reference：
Patent; Egle, Ian R.; Frey, Jennifer; Isaac, Methvin B.; Slass, Abdelmalik; Begleiter, Leah E.; Edwards, Louise G.; Stefanac, Tomislav; Tehim, Ashok; Maddaford, Shewn P.; Tse, Hoi Lun Allan; US2003/176461; (2003); 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.914988-10-6,tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

914988-10-6, A mixture of tert-butyl 3-eyano-4-oxopiperidine- I -carboxylate (310 g, 1.38 mol) and hydrazine mono-hydrate (140 mL, 2.08 mol) in EtOH (1.5 L) was heated to 60 C for 2 h. The mixture was concentrated in vacuo to give the crude product that was dissolved inEtOAc (1 L) and washed with water (1 L x 2), The organic layer was dried over anhydrousNa2SO4, filtered and concentrated in vacuo to afford the title compound (230 g, 70%) as acolorless solid, ?H NMR (400 MHz, CD3OD) 6 4.28 (s, 211), 3.66 -3.63 (m, 211), 2.62 – 2.59(m, 211), 1.49 (s, 9H).

As the paragraph descriping shows that 914988-10-6 is playing an increasingly important role.

Reference：
Patent; GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC.; ROMERO, F. Anthony; MAGNUSON, Steven; PASTOR, Richard; TSUI, Vickie Hsiao-Wei; MURRAY, Jeremy; CRAWFORD, Terry; ALBRECHT, Brian, K.; COTE, Alexandre; TAYLOR, Alexander, M.; LAI, Kwong Wah; CHEN, Kevin, X.; BRONNER, Sarah; ADLER, Marc; EGEN, Jackson; LIAO, Jiangpeng; WANG, Fei; CYR, Patrick; ZHU, Bing-Yan; KAUDER, Steven; (0 pag.)WO2016/86200; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

10338-57-5, 4-(Piperidin-1-yl)benzaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of2-acetylbenzofuran (1) (1.6 g, 10 mmol) and 4-piperidinylbenzaldehyde(2) (1.89 g, 10 mmol) in ethanol (30 mL), 10%aqueous sodium hydroxide (10 mL) was added portion-wise atroom temperature for 10 min, the reaction mixture was furtherstirred for 3 h. The resulting solid was filtered, washed withwater, dried and crystallized from EtOH/DMF to afford chalcone3. orange powder; 85% yield; mp 178-179C; 1H-NMR(DMSO-d6) delta: 1.40-1.56 (6H, m, piperidine H), 2.98-3.26(4H, m, piperidine H), 6.70-6.72 (1H, d, J=14.0 Hz, -CO-CH=), 6.88-6.92 (2H, d, J=14.0 Hz, Ar-H), 7.52-7.54 (1H,d, J=14 Hz,=CH-Ar), 7.61-7.82 (6H, m, Ar-H), 8.16 (1H, s,benzofuran H). IR (KBr) cm-1: 3099 (CH-Ar), 1648 (C=O),1578 (CH olefinic). MS m/z: 331 (M+, 100), 330 (68), 274 (26),247 (28), 214 (56), 186 (27), 145 (87), 117 (7). Anal. Calcd forC22H21NO2: C, 79.73; H, 6.39; N, 4.23. Found: C, 79.56; H,6.21; N, 4.17., 10338-57-5

10338-57-5 4-(Piperidin-1-yl)benzaldehyde 291354, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Nassar, Ekhlass; El-Badry, Yaser Abdel-Moemen; Kazaz, Hagar El; Chemical and Pharmaceutical Bulletin; vol. 64; 6; (2016); p. 558 – 563;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1172500-91-2, 4-Benzenesulfonylpiperidine Hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 4-(phenylsulfonyl)piperidine hydrochloride (l .Og, 3.8 mmol), (S)-2-((tert-butoxycarbonyl)amino)-3-(3,5-difluoro-4-hydroxyphenyl)propanoic acid (l .lg, 3.5 mmol), DIPEA (1.8 mL, 10.4 mmol), DCM (16 mL) and DMF (4 mL) was treated with HATU (1.59 g, 4.2 mmol). The mixture was stirred for lh then the resulting solution was allowed to stand for 18 h. The mixture was diluted with dichloro methane (30 mL) and washed with saturated sodium hydrogen carbonate (aq.) (20 mL) then saturated brine (2 x 20 mL). The organic phase was dried (Na2S04) and concentrated in vacuo and purified by chromatography on a Si cartridge eluting with 0-20% DCM in ethyl acetate to give Intermediate 41 A (780 mg). LCMS (Method 3): Rt = 1.25 min. m/z 525.3 [M+H]+

1172500-91-2, The synthetic route of 1172500-91-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHIESI FARMACEUTICI S.P.A.; ACCETTA, Alessandro; RANCATI, Fabio; CAPELLI, Anna Maria; CLARK, David Edward; TISSELLI, Patrizia; EDWARDS, Christine; CHEGUILLAUME, Arnaud Jean Francois Auguste; BHALAY, Gurdip; (101 pag.)WO2020/16129; (2020); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

39514-19-7, Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3A 3-Oxo-piperidine-1,4-dicarboxylic Acid 1-tert-butyl Ester 4-ethyl Ester A mixture of commercially available ethyl-N-benzyl-3-oxo-4-piperidinecarboxylate hydrochloride (Aldrich, 75.4 g, 0.25 mol), di-t-butyl dicarbonate (58.5 g, 0.27 mol), Et3N (36 mL, 0.26 mol), and Pd(OH)2/C (7.5 g, 50percent in H2O) in 660 mL EtOH was put under 60 psi of H2 and was shaken for 25 min. The mixture was then filtered and the filtrate was concentrated under reduced pressure to provide the title compound which was used in the next step without further purification. MS (DCl/NH3) m/z 272 (M+H)+.

39514-19-7, As the paragraph descriping shows that 39514-19-7 is playing an increasingly important role.

Reference：
Patent; Basha, Anwer; Bunnelle, William H.; Dart, Michael J.; Gallagher, Megan E.; Ji, Jianguo; Li, Tao; Pace, Jennifer M.; Ryther, Keith B.; Tietje, Karin R.; Mortell, Kathleen H.; Nersesian, Diana L.; Schrimpf, Michael R.; US2005/101602; (2005); 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.61869-08-7,(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine,as a common compound, the synthetic route is as follows.,61869-08-7

0.8 g of oily paroxetine free base and 1.31 g of taurocholic acid were completely dissolved in a mixed solvent of purified water (5 mL) and ethanol (20 mL) while heating to 40 C. with shaking for one hour. After the solution was concentrated under reduced pressure until about 5 mL of the solvent was left, it was allowed to stand at -20 C.0 C. for 24 hours to precipitate a crystal, followed by filtration. The filtered residue was washed with cold methanol at 0 C. or less, and dried under vacuum to give 1.8 g of solid paroxetine taurocholate as a light gray powder.

The synthetic route of 61869-08-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Lee, Sang Joon; Shin, Hee Jong; Ki, Min Hyo; Lee, Su Kyoung; Kim, Bok Young; Lee, Hong Woo; US2006/63747; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem