Heterocyclic Building Blocks-piperidine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3433-37-2,2-(Hydroxymethyl)piperidine,as a common compound, the synthetic route is as follows.,3433-37-2

Example 8; 2-Hydroxymethyl-piperidine-l-carboxylic acid tert-butyl ester; Di-tert-butyl dicarbonate (8.3 g, 38.2 mmol) was added to a stirred solution of piperidinemethanol (4. 0g, 37.4 mmol) in CH2C12 (50 mL) and 1N NaOH (50 mL, 50 mmol) was added. The mixture was stirred at room temperature overnight. Reaction mixture was diluted with CH2C12 and the aqueous phase was separated. The aqueous phase was extracted with dichloromethane (3X30 mL). The combined organic phase was washed with water (30 mL) and brine (30 mL), dried (sodium sulfate), filtered and concentrated in-vacuo to give the crude product which was triturated with hexane to afford the title compound as white solid (4.8 g, 64percent).

As the paragraph descriping shows that 3433-37-2 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2005/80386; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

22990-34-7, 2-(4-Piperidyl)-2-propanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 209 [0728] cis-Methyl 4-((E)-2-(4-fluorobenzoylimino)-6-((4-(2- hydroxypropan-2-yl)piperidin-l-yl)methyl)-2,3-dihydro-lH-benzo[d]imidazol-l- yl)cyclohexanecarboxylate. To a 0C cooled solution of cis-methyl 4-((E)-2-(4- fluorobenzoylimino)-6-(hydroxymethyl)-2,3-dihydro-lH-benzo[d]imidazol-l- yl)cyclohexanecarboxylate (1 g, 2.350 mmol) in DCM (25 mL) was added thionyl chloride (0.858 mL, 11.75 mmol) dropwise, and the reaction was stirred at 0C for 30 minutes. After 30 minutes, the solvent was removed at reduced pressure, and the residue was suspended in ACN (5 mL) and re-concentrated to remove residual thionyl chloride. The residue was resuspended in ACN (15 mL), cooled to 0C, and 2-(piperidin-4- yl)propan-2-ol (1.010 g, 7.05 mmol) and TEA (0.655 mL, 4.70 mmol) were added. The reaction was stirred overnight at RT. After 16 hours, the reaction mixture was concentrated and partitioned between EtOAc and water. The organic layer was concentrated and the residual product was purified by column chromatography, eluting with 0-100% (90:9:1 DCM/MeOH/NH4OH)/DCM to provide cis-methyl 4-((E)-2-(4- fluorobenzoylimino)-6-((4-(2-hydroxypropan-2-yl)piperidin-l-yl)methyl)-2,3-dihydro- lH-benzo[d]imidazol-l-yl)cyclohexanecarboxylate as a white powder (1.05 g, 81 % yield). .H NMR (400 MHz, DMSO-d6) delta ppm 1.03 (s, 6 H), 1.09 – 1.35 (m, 3 H), 1.56 – 1.91 (m, 8 H), 2.21 – 2.29 (m, 2 H), 2.53 – 2.64 (m, 2 H), 2.77 – 2.95 (m, 3 H), 3.50 (s, 2 H), 3.77 (s, 3 H), 3.99 (s, 1 H), 4.74 (br. s., 1 H), 7.14 (d, J=6.9 Hz, 1 H), 7.26 (dd, J=8.8 Hz, 8.8 Hz, 2 H), 7.37 – 7.58 (m, 2 H), 8.26 (dd, J=8.7, 5.9 Hz, 2 H), 12.77 (s, 1 H). MS, m/z (C31H39FN4O4): calcd, 550.3; found, 551.1 [M+H].

22990-34-7, As the paragraph descriping shows that 22990-34-7 is playing an increasingly important role.

Reference£º
Patent; AMGEN INC.; BODE, Christiane, M.; CHENG, Alan, C.; CHOQUETTE, Deborah; LEWIS, Richard, T.; POTASHMAN, Michele, H.; ROMERO, Karina; STELLWAGEN, John, C.; WHITTINGTON, Douglas, A.; WO2012/18668; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

64051-79-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.64051-79-2,3-Hydroxypiperidine Hydrochloride,as a common compound, the synthetic route is as follows.

10 Step 4: preparation of 3-Hydroxy-piperidine-1-carboxylic acid benzyl ester. Tosuspension of piperidin-3-ol hydrochloride (134 g, 0.974 mol) and triethylamine (276 mL, 1.98 mol) in dichloromethane (2 L) at 0 C was added a solution of benzyl chloroformate (140 mL, 0.981 mol) in dichloromethane (100 mL) drop wise over 2.5 h. The reaction was allowed to stir for an additional 30 mm at 0 C, then allowed to warm15 to ambient temperature over 16 h, after which it was quenched with 1 N hydrochloric acid (3 L) and allowed to stir for 30 mm. The organic layer was separated, dried over sodium sulfate, and concentrated in vacuo to afford the title compound (218 g, 95 %).1H-NMR (CDCI3) 67.29-7.41 (m, 5H), 5.14 (s, 2H), 3.59-3.85 (m, 3H), 3.13-3.27 (m, 2H), 2.18 (bs, 1H), 1.74-1.94 (m, 2H), 1.38-1.61 (m, 2H).

64051-79-2 3-Hydroxypiperidine Hydrochloride 2723962, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER INC.; SPRINGER, John Robert; DEVADAS, Balekudru; GARLAND, Danny James; GRAPPERHAUS, Margaret Lanahan; HAN, Seungil; HOCKERMAN, Susan Landis; HUGHES, Robert Owen; SAIAH, Eddine; SCHNUTE, Mark Edward; SELNESS, Shaun Raj; WALKER, Daniel Patrick; WAN, Zhao-Kui; XING, Li; ZAPF, Christoph Wolfgang; SCHMIDT, Michelle, Ann; WO2014/68527; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

625471-18-3, (S)-tert-Butyl 3-aminopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Fluorophenylisocyanate (137 mg, 1 rnrnol) was slowly dropped into a solution of (S)-3-amino-l-N-Boc-piperidine (200 mg, 1 mmol) in DCM (2 mL). The reaction mixture was stirred at ambient temperature for 2h and then the solvent was evaporated under reduced pressure to afford a residue oil (337 mg), which was used for the next step without further purification. Yield: 100percent; LCMS (RT): 7.9 min (Method B); MS (ES+) gave m/z: 338.1., 625471-18-3

The synthetic route of 625471-18-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ADDEX PHARMACEUTICALS SA; WO2006/123244; (2006); A2;,
Piperidine – Wikipedia
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41373-39-1,41373-39-1, (S)-Piperidin-2-ylmethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4-((6-ethoxy-6-oxohexyl)oxy)-5-methoxy-2-nitrobenzoic acid (16 ) (2.00 g, 5.60 mmol) in dichloromethane (40 mL) was charged with trimethyl amine (4.70 mL, 33.8 mmol) and 0-(7-azabenzotriazole-i-yl)-A V,A V-tetramethyluronium hexafluoro- phosphate (2.20 g, 5.90 mmol) and the resulting mixture was stirred for 2 h at room temperature. A solution of (S,)-piperidin-2-ylmethanol (647 mg, 5.63 mmol) in dichloromethane (10 mL) was then added and the resulting mixture was stirred for 16 h at room temperature. The reaction was quenched with a saturated aqueous solution of sodium hydrogen carbonate (40 mL), the phases were separated and the aqueous layer was further extracted with dichloromethane (20 mL). The combined organic extracts were washed with brine (40 mL), dried over magnesium sulfate, filtered and (1451) concentrated to give an amber oil. Purification was carried out by column (1452) chromatography (silica), eluting with ethyl acetate/ hexane (from 0percent to 100percent), to give the title compound (1.20 g, 48percent) as a colourless oil. (1453) NMR (400 MHz, CDCI3) delta 7.63-7.6o (m, iH), 6.77-6.75 (m, iH), 4.13-4.02 (m, 4H), 3-93 (s, 3H), 3-78-3-70 (m, iH), 3-68-3-39 (m, iH), 3-i8-3-H (m, 3H), 2.32 (t, J=7-6 Hz, 2H), 1.91-1.83 (m, 2H), 1.72-1.39 (m, 11H), 1.26 (t, J=7-i Hz, 3H); MS M/Z (EIMS) = 453 (M+H)+; LCMS (Method B): tR = 3.63 min.

The synthetic route of 41373-39-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; FEMTOGENIX LIMITED; JACKSON, Paul Joseph Mark; THURSTON, David Edwin; RAHMAN, Khondaker Mirazur; (243 pag.)WO2017/194960; (2017); A1;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.908245-03-4,Methyl 6-methylpiperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

908245-03-4, To a dichloromethane solution (40 mL) of methyl 6-methylpiperidine-3-carboxylate (3.90 g) obtained in Step 1, triethylamine (2.64 g) was added, then, a dichloromethane solution (5 mL) of Boc2O (5.68 g) was added while stirring at room temperature. After stirred for 70 hours at room temperature, the reaction mixture was washed with 1 mol/L hydrochloric acid (100 mL). The organic layer was dried with anhydrous sodium sulfate, and filtered. The filtrate was concentrated under reduced pressure, the residue was purified with silica gel column chromatography (hexane/ethyl acetate=100/0 to 13/87) to give 1-tert-butyl 3-methyl-cis-6-methylpiperidine-1,3-dicarboxylate (2.66 g, low polarity) and 1-tert-butyl 3-methyl-trans-6-methylpiperidine-1,3-dicarboxylate (1.39 g, high polarity) respectively as an oil. cis-isomer, 1H NMR (300 MHz, CDCl3) delta 1.13 (d, 3H), 1.46 (s, 9H), 1.50-1.95 (m, 4H), 2.30-2.45 (m, 1H), 2.80-3.00 (m, 1H), 3.69 (s, 3H), 4.15 (br, 1H), 4.40 (br, 1H); trans-isomer, 1H NMR (300 MHz, CDCl3) delta 1.14 (d, 3H), 1.30-1.40 (m, 1H), 1.46 (s, 9H), 1.72-1.96 (m, 2H), 1.96-2.06 (br, 1H), 2.58 (br, 1H), 3.04-3.10 (m, 1H), 3.68 (s, 3H), 4.30-4.45 (m, 2H)

908245-03-4 Methyl 6-methylpiperidine-3-carboxylate 42628698, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SUMITOMO CHEMICAL COMPANY, LIMITED; SUMITOMO DAINIPPON PHARMA CO., LTD.; FUSANO, Akira; KOBAYASHI, Tomonori; SAITO, Yasuhiro; KANAI, Toshio; (55 pag.)US2016/221948; (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.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

Example 1683-(4-Cyclohexylamino-1H-pyrazolo[4,3-c]pyridin-3-yl)-1-(4,4-drfluoro-piperidin-1-yl)-propan-1-oneTo a solution of Intermediate 23 (35 mg, 0.12 mmol) in DMF (1.5 ml) was added HATU (48 mg, 0.13 mmol) and Lambda/,Lambda/-diisopropylethylamine (126 mul, 0.73 mmol). 4,4-difluoro0 piperidine (19 mul, 0.18 mmol) was then added and the resulting solution was left to stir at room temperature overnight. The volatiles were removed under reduced pressure and the crude product was re-dissolved in 10percent MeOH/DCM and eluted though an Isolute-NH2 cartridge. The crude product purified by flash chromatography eluting with 10percent MeOH/DCM to give a yellow gum (28 mg, 61percent). 1H NMR (400 MHz, DMSO-Cf6) delta ppm-5 1.14 – 1.26 (m, 1 H), 1.30 – 1.46 (m, 4 H), 1.60 – 1.72 (m, 1 H), 1.71 – 2.01 (m, 8 H), 2.87 (t, 2 H), 3.21 (t, J=6.4 Hz, 2 H), 3.49 – 3.60 (m, 4 H), 4.01 (br. s., 1 H), 6.67 (br. s., 1 H), 7.62 (d, J=6.0 Hz, 1 H); m/z (ES+APCl)+: 392 [M + H]+., 21987-29-1

As the paragraph descriping shows that 21987-29-1 is playing an increasingly important role.

Reference£º
Patent; MEDICAL RESEARCH COUNCIL TECHNOLOGY; MCIVER, Edward, Giles; SMILJANIC, Ela; HARDING, Denise, Jamilla; HOUGH, Joanne; WO2010/106333; (2010); 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.19395-41-6,Ritalinic acid,as a common compound, the synthetic route is as follows.

Example 8 Conjugation of RA to BTG To a solution of RA (29.6mg, 0.135mmol) in DMF (1.0ml) was added N,N-dicyclohexylcarbodiimide (DCC) (31.0mg, 0.149mmol) and N-hydroxysuccinimide (17.13mg, 0.149mmol) and the mixture was stirred at room temperature overnight. The dicyclohexylurea formed was removed by filtration and the solution was added dropwise to a solution of BTG (150mg) in 50mM sodium bicarbonate solution (pH 8.5) (10ml)., 19395-41-6

19395-41-6 Ritalinic acid 86863, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Randox Laboratories Ltd.; Benchikh, Elouard; Fitzgerald, Peter; Lowry, Philip; McConnell, Ivan; EP2769994; (2014); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1123-40-6, 4,4-Dimethylpiperidine-2,6-dione is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A suspension of LiAlH4 (5.5 g, 145 mmol) in diethyl ether (300 ML) was treated in portions with 3,3-dimethylglutarimide (8.5 g, 57.7 mmol), heated to reflux, stirred overnight, cooled to room temperature, and treated with 1N NaOH (70 ML).The solution was decanted and the remaining solid was washed with diethyl ether (3*200 ML).The combined organic washes were washed with brine, dried (Na2SO4), filtered, and concentrated to a volume of 200 ML. The solution was treated with 2M HCl in diethyl ether (50 ML) and the mixture was filtered and the filter cake was washed with diethyl ether (3*150 ML) to provide the desired product (6.58 g, 76%). MS (CI) m/e 114 (M+H)+., 1123-40-6

As the paragraph descriping shows that 1123-40-6 is playing an increasingly important role.

Reference£º
Patent; Elmore, Steven W.; Park, Cheol-Min; Wang, Xilu; US2003/236247; (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.6859-99-0,Piperidin-3-ol,as a common compound, the synthetic route is as follows.

6859-99-0, A solution of di-tert-butyl dicarbonate (5.83 g, 26.7 mmol) in dichloromethane (10 ml) was added to a solution of 3-hydroxypiperidine (3.0 g, 29.7 mmol) in dichloromethane (30 ml) at room temperature and stirred for 15 hours. The reaction solution was concentrated, diluted with ethyl acetate, and then washed with a saturated aqueous sodium hydrogencarbonate solution, a 0.5M-aqueous potassium hydrogensulfate solution, a saturated aqueous sodium hydrogencarbonate solution and then a saturated aqueous sodium chloride solution. The organic layer was dried over anhydrous magnesium sulfate and distilled under reduced pressure to remove the solvent, and the resulting residue was crystallized by the addition of hexane, filtered, and then dried to obtain tert-butyl 3-hydroxy-1-piperidinecarboxylate (5.17 g, 87percent).1H-NMR (DMSO-d6) delta; 1.46 (9H, s, 1.99 (2H, m), 3.34-3.49 (4H, m), 4.45 (1H, m).

The synthetic route of 6859-99-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Pharmaceuticals Company, Limited; EP1403255; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem