Category: piperidines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

Step 2To a solution of 68 (13 g, 38.9 mmol) in DCM (5 mL) was added HCl/EA (20 mL). The mixturewas stirred at rt for 2 h. The mixture was filtered and filter cake was concentrated under vacuum to afford 69 (7.59 g, 83% yield).

220394-97-8, As the paragraph descriping shows that 220394-97-8 is playing an increasingly important role.

Reference：
Patent; SYROS PHARMACEUTICALS, INC.; PARAZA PHARMA, INC.; CIBLAT, Stephane; DEROY, Patrick; LEBLANC, Melissa; MARINEAU, Jason, J.; MOORE, Joel; ROY, Stephanie; SIDDIQUI, M., Arshad; SPROTT, Kevin; WINTER, Dana, K.; KABRO, Anzheliika; LEGER, Serge; MILLER, Tom; SCHMIDT, Darby; BRADLEY, Michael; WO2015/58163; (2015); A2;,
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180307-56-6, tert-Butyl 4-vinylpiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0077] In a 15 mL microwave tube was added 5-bromo-2,1,3-benzoxadiazole (0.94 g, 4.7 mmol), tert-butyl 4-ethenylpiperidine-1-carboxylate (1.0 g, 4.7 mmol), triethylamine (0.66 ml, 4.7 mmol), palladium (II) acetate (0.11 mg, 0.47 mmol)and DMF (5 mL). The solution was degassed and filled with nitrogen (3x), then heated to 100 C for 2 hr. The reactionwas diluted with ethyl acetate, washed with water, filtered through a pad of diatomaceous earth and a plug of silica gel.The organic phase was dried over MgSO4, concentrated and purified by MPLC (eluted with gradient 0->30% EtOAc/Hexane)to provide tert-butyl 4-[(E)-2-(2,1,3-benzoxadiazol-5-yl)ethenyl]piperidine-1-carboxylate as a mixture with the Zolefin.LC-MS (IE, m/z): 352 [M+Na]+.

180307-56-6, As the paragraph descriping shows that 180307-56-6 is playing an increasingly important role.

Reference：
Patent; Merck Sharp & Dohme Corp.; WALSH, Shawn; PASTERNAK, Alexander; CATO, Brian; FINKE, Paul, E.; FRIE, Jessica; FU, Qinghong; KIM, Dooseop; PIO, Barbara; SHAHRIPOUR, Aurash; SHI, Zhi-Cai; TANG, Haifeng; (136 pag.)EP2755656; (2016); B1;,
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4801-58-5, Piperidin-1-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 31.9 mg (0.15 mmol) of N,N-dibenzylhydroxylamines 1a was placed into a 4 mL vial equipped with a magnetic stirrer bar. 2 mL of dehydrated methanol was added and then stirred to obtain a solution. AuNPore (10 mol%, 2.96 mg) was put into the reaction solution, which was placed in the bottom of vial. Oxygen balloon was prepared and then attached into the vial through cap equipped with a septum to make an oxygen atmosphere. Reaction was allowed to proceed for 2 h at 60C. The formation of product(s) was monitored by TLC. After completion of reaction, the resulting solution was simply taken using a pipette while the vial was washed several times with methanol. Combined solution was concentrated under vacuum condition to give a residue. Obtained residue was purified by passing it through a basic silica column chromatography with ethyl acetate as the eluent to give 31.1 mg of 2a in 98% yield. All of products in Tables 1 and 2 are identified with the reported data in the literature: 2a,17a 2b,19 2c,12b 2d,20 2e,13j 2f,19 2g.13b

4801-58-5, 4801-58-5 Piperidin-1-ol 20935, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Yudha S, Salprima; Kusuma, Indra; Asao, Naoki; Tetrahedron; vol. 71; 37; (2015); p. 6459 – 6462;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.14813-01-5,1-Benzylpiperidin-3-ol,as a common compound, the synthetic route is as follows.

General procedure: The alcohol (1.0 equiv.) was dissolved in CH2Cl2 at room temperature.The solution was stirred, and isocyanate (1.2 equiv.) wasadded, followed by 4-DMAP (0.1 equiv.). After 24 h, the solvent wasevaporated and the crude product was purified by flash columnchromatography.

14813-01-5, As the paragraph descriping shows that 14813-01-5 is playing an increasingly important role.

Reference：
Article; ?akelj, Simon; Brazzolotto, Xavier; Gobec, Stanislav; Juki?, Marko; Knez, Damijan; Ko?ak, Urban; Kos, Janko; Nachon, Florian; Pi?lar, Anja; Stra?ek, Nika; Zahirovi?, Abida; European Journal of Medicinal Chemistry; vol. 197; (2020);,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.19099-93-5,1-Cbz-Piperidin-4-one,as a common compound, the synthetic route is as follows.

Benzyl 4-oxopiperidine-l-carboxylate (5g, 21 mmol) in THF (50 ml) was cooled to 0C. Sodium hydride (1.1 g, 43 mmol), then iodomethane (3.0 ml, 47 mmol) was added slowly. Mixture was stirred at 0C for 2 hours, then slowly warm up to room temperature and stirred overnight. Saturated aq. NH4C1 solution was added and the product was extracted with EtOAc. The extract was washed with brine, dried over anhydrous sodium sulfate, and concentrated. The crude product thus obtained was purified by column chromatography on a 100 gram-size silica gel column, eluting with gradient EtOAc/hexane to afford the titled product as colorless oil.

19099-93-5, The synthetic route of 19099-93-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; ALI, Amjad; LO, Michael Man-Chu; LIM, Yeon-Hee; STAMFORD, Andrew; KUANG, Rongze; TEMPEST, Paul; YU, Younong; HUANG, Xianhai; HENDERSON, Timothy J.; KIM, Jae-Hun; BOYCE, Christopher; TING, Pauline; ZHENG, Junying; METZGER, Edward; ZORN, Nicolas; XIAO, Dong; GALLO, Gioconda V.; WON, Walter; WU, Heping; WO2014/101373; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.140645-24-5,(S)-3-(Aminomethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.

To the solution of 5-bromothiazole-2-carboxylic acid (scheme 8-33 compound S1, 458 mg, 2.2mmol) and tert-butyl (S)-3-(aminomethyl)piperidine-1-carboxylate (scheme 8-33 compound S2, 429 mg, 2.0mmol) in DCM (15.0 mL) at 0 C, HATU (912 mg, 2.4mmol) was added, followed by addition of DIEA (3.6mmol). The mixture was stirred for 1 h. The volatiles were evaporated under reduced pressure. The residue was diluted with ethyl acetate (60mL) and washed with saturated NaHCO3, water and brine. The organic solution was dried over MgSO4. The solution was filtered and the filtrate was concentrated. The remaining material was purified to afford 513 mg of title product. LC (method A): tR = 2.30 min. LC/MS (EI) m/z: [M + H]+ 404.06, 406.09.

140645-24-5, As the paragraph descriping shows that 140645-24-5 is playing an increasingly important role.

Reference：
Patent; ACHILLION PHARMACEUTICALS, INC.; WILES, Jason, Allan; PHADKE, Avinash, S.; DESHPANDE, Milind; AGARWAL, Atul; CHEN, Dawei; GADHACHANDA, Venkat, Rao; HASHIMOTO, Akihiro; PAIS, Godwin; WANG, Qiuping; WANG, Xiangzhu; GREENLEE, William; (508 pag.)WO2017/35409; (2017); A1;,
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21168-72-9, 2-(4-(Aminomethyl)piperidin-1-yl)ethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

12 g of 2- (4- (aminomethyl) piperidin-1-yl) ethanol was added to150 ml of N, N-dimethylformamide,Add 18g bromoethane, then add 15g of potassium carbonate,Heated to reflux for 2 hours,Water and ethyl acetate were added, the mixture was extracted and separated, and the organic phase was collected, dried and concentrated. The residue was separated on a silica gel column to obtain 9 g2- (4 – ((ethylamino) methyl) piperidin-1-yl) ethanol., 21168-72-9

As the paragraph descriping shows that 21168-72-9 is playing an increasingly important role.

Reference：
Patent; Hunan Huateng Pharmaceutical Co., Ltd.; Bu Gonggaofamingren; (5 pag.)CN104557672; (2016); B;,
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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.32559-18-5,Methyl piperidine-2-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

1-(2-Oxo-2-thiophen-2-yl-acetyl)piperidine-2-carboxylic acid N’-(6-methyl-4-trifluoromethyl-pyridin-2-yl)-hydrazide A solution of methyl pipecolinate hydrochloride (7.2 g, 40 mmol) in dry DCM (100 mL) and TEA (8.3 g) was cooled to 0 C. The slurry was stirred for 1 h. Methyl oxalyl chloride was added. The mixture was stirred at 0 C. for 2 h. Water was added, and the organic phase was washed with a NaHCO3 solution, dried with MaSO4. Evaporation of the solvent and drying in vacuum gave a reddish oil; 9.1 g (99%); MS (m/z) 252 (M+Na).

32559-18-5, 32559-18-5 Methyl piperidine-2-carboxylate hydrochloride 13246231, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Sui, Zhihua; Macielag, Mark; Lanter, James; US2003/144262; (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.5810-56-0,4-Acetamidopiperidine,as a common compound, the synthetic route is as follows.

5810-56-0, Following the procedure of Example 74 using 5,5-Dioxo-2-(4-nitrobenzoxy-carbonylamino)dibenzothiophene (Example 24) and the appropriate amine the following compounds were prepared.

The synthetic route of 5810-56-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Block, Michael Howard; Donald, Craig Samuel; Brittain, David Robert; Foote, Kevin Michael; US2003/225097; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

20691-89-8, 1-Methyl-4-piperidinemethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of l-chloro-4-nitrobenzene (23) (2.37 g, 15.0 mmol), alcohol 22 (1.94 g, 15.0 mmol), and DMSO (25 mL) was treated portionwise with NaH (60% in mineral oil, 660 mg, 16.5 mmol) at 40 0C. The mixture was stirred at 70 0C for 3 h, poured into water (15O mL), and extracted with Et2O (5 x 10O mL). The combined organic fractions were washed with water (250 mL) and brine (250 mL), dried (MgSQ4), and the solvent was removed in vacuo. The resulting solid was recrystallized from Et2O to give 24 (3.12 g, 83%) as yellow needles. 1H NMR (300 MHz, CDCl3): delta = 1.36-1.56 (m, 2 H, 3-Hax, 5-Hax), 1.75-1.91 (m, 3 H, 3-Heq, 4-H, 5-Heq), 1.98 (dt, J= 11.9, 1.9 Hz, 2 H, 2-Hax, 6-Hax), 2.30 (s, 3 H, NMe), 2.85-2.98 (m, 2 H, 2-Heq, 6-Heq), 3.90 (d, J= 5.8 Hz, 2 H, OCH2), 6.94 (me, 2 H, 2′-H, 6′-H), 8.19 Cm0, 2 H, 3′-H, 5′-H) ppm. – 13C NMR (50.3 MHz, CDCl3): 6 = 28.9 (C-3, C-5), 35.1 (C-4), 46.4 (NMe), 55.3 (C-2, C-6), 73.3 (OCH2), 114.3 (C-21, C-6′), 125.8 (C-3′, C-5′), 141.3 (C-41), 164.1 (C-I’) ppm. -MS (70 eV, EI): m/z (%) = 250 (79) [M]+, 249 (100) [M-H]+. – Ci3H]8N2O3 (250.29): calcd. C 62.38, H 7.25; found C 62.25, H 7.40., 20691-89-8

The synthetic route of 20691-89-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SYNTARGA B.V.; GEORG-AUGUST-UNIVERSITAet GOeTTINGEN STIFTUNG OeFFENTLICHEN RECHTS (OHNE BEREICH HUMANMEDIZIN); WO2007/89149; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem