Heterocyclic Building Blocks-piperidine

72752-52-4, 2-Piperidinobenzonitrile is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2; 3-methyl-1-(2-(1-piperidinyl)phenyl)butylamine; This amine was obtained from the nitrile intermediate according to protocol B. It was isolated by silica gel chromatography (dichloromethane/methanol 95/5). Yield: 79%

72752-52-4, As the paragraph descriping shows that 72752-52-4 is playing an increasingly important role.

Reference：
Patent; GENFIT; US2006/79696; (2006); A1;,
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Piperidine | C5H11N – PubChem

92926-63-1,92926-63-1, 6-Chloro-1,2-dihydro-2-oxospiro[4H-3,1-benzoxazin-4,4′-piperidine] is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 520 2-(5-{3-[6-chloro-1,2-dihydro-2-oxo-spiro[4H-3,1-benzoxazin-4,4′-piperidin]-1-yl]-propylidene}-5,11-dihydro-10-oxa-1-aza-dibenzo[a,d]cyclohepten-7-yl)-propan-2-ol A solution of 6-chloro-1,2-dihydro-2-oxo-spiro[4H-3,1-benzoxazin-4,4′-piperidine] (Made by the procedure of Bock, et al. GB2,355,465, 0.25 g, 0.7 mmol) in isopropanol (5 mL) was treated with 2-[5-(3-Bromo-propylidene)-5,11-dihydro-10-oxa-1-aza-dibenzo[a,d]cyclohepten-7-yl]-propan-2-ol (0.19 g, 0.50 mmol) and catalytic potassium iodide. The solution was stirred at 80 C. for 5 hr, and evaporated in vacuo. The residue was purified by reverse-phase preparative HPLC to yield 0.029 g (10%) of the title compound, 1H-NMR (CD3OD) delta: 1.50 (3H, s), 2.18 (2H, brs), 2.95-3.2 (6H, m), 5.30 (2H, brs), 6.18 (1H, t), 6.79 (1H, m), 6.92 (1H, m), 7.12 (1H, m), 7.38 (2H, m), 7.48 (2H, m), 7.81 (2H, m), 8.31 (1H, m), 8.55 (1H, d). ESI-MS m/z: 546 [M+1].

92926-63-1 6-Chloro-1,2-dihydro-2-oxospiro[4H-3,1-benzoxazin-4,4′-piperidine] 13116154, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Millennium Pharmaceuticals, Inc.; Kyowa Hakko Kirin Co., Ltd.; LULY, Jay R.; NAKASATO, Yoshisuke; OHSHIMA, Etsuo; HARRIMAN, Geraldine C.B.; CARSON, Kenneth G.; GHOSH, Shomir; ELDER, Amy M.; MATTIA, Karen M.; (190 pag.)US2016/31908; (2016); A1;,
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25137-01-3, (R)-Ethyl piperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2-(3-(3-methylphenyl)-3-phenyl-2-propen-1-yloxy)ethanol (16 g, 60 mmol) and triethylamine (15.1 g, 149 mmol) in dry toluene (75 ml) kept under a nitrogen atmosphere was cooled to 5 C. and a solution of methanesulphonyl chloride (13.7 g, 119 mmol) in dry toluene (75 ml) was added dropwise keeping the temperature below 10 C. When addition was complete the reaction mixture was stirred for 1.5 h at 5 C. Water was added (100 ml) and the mixture was stirred at room temperature for 0.5 h. The phases were separated and the aqueous phase was extracted with a small portion of toluene. The combined organic extracts was washed with brine, dried over sodium sulphate and filtered. To the filtrate was added ethyl (R)-3-piperidinecarboxylate (10.3 g, 66 mmol) and potassium carbonate (9.9 g, 72 mmol) and the mixture was heated at reflux temperature for 6 days. Another portion of ethyl (R)-3-piperidinecarboxylate (5.3 g) was added and the mixture was heated at reflux temperature for another 24 h. The reaction mixture was poured into ice water (200 ml) and extracted with ethyl acetate (2*200 ml). The combined organic extracts was washed with a sodium citrate buffer solution (2*100 ml, pH 5) and then extracted with a 5% aqueous citric acid solution (4*100 ml). Toluene (120 ml) was added to the combined acidic extracts and sodium hydroxide pellets was added to the mixture until the pH was measured at 8.5. The phases were separated and the organic phase was dried over sodium sulphate. The solvent was evaporated in vacuo to give 9.4 g (39%) of (R)-N-(2-(3-(3-methylphenyl)-3-phenyl-2-propen-1-yloxy)ethyl)-3-piperidinecarboxylic acid ethyl ester as an oil. TLC: rf=0.50 (SiO2; dichloromethane/methanol/acetic acid=20:2:1).

25137-01-3, 25137-01-3 (R)-Ethyl piperidine-3-carboxylate 185582, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Novo Nordisk A/S; US5198451; (1993); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

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

4- r(E)-2-(4-nitrophenyl)ethenyl1piperidinium Chloride Step A: fert-Butyl 4-r(E)-2-(4-nitrophenyl)ethenyl1piperidine-l-carboxylate tert-Butyl 4-ethenylpiperidine- 1 -carboxylate (0.50 g, 2.4 mmol), tra/?s-dichlorobis(tri-o- tolylphosphine) palladium (II) (0.050 g, 0.064 mmol), l-bromo-4-nitrobenzene (0.57 g, 2.8 mmol), and triethylamine (1.6 mL, 12 mmol) were added to a microwave tube, diluted with DMF (2 mL) and degassed under a stream of nitrogen. The tube was sealed and heated in the microwave to 130 C for 30 min. The resulting mixture was diluted with diethyl ether and washed successively with saturated sodium bicarbonate, water (2x), 1 N hydrochloric acid, and brine, then dried (MgS04), filtered and concentrated. The resulting tert-butyl 4-[(E)-2-(4- nitrophenyl)ethenyl]piperidine-l -carboxylate was used directly in the next step. LC/MS: [(M+l)]+ = 333.

180307-56-6, The synthetic route of 180307-56-6 has been constantly updated, and we look forward to future research findings.

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; WO2013/39802; (2013); A1;,
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534595-51-2, 1-Boc-4-(isopropylamino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 10; N-Isopropyl-N-piperidin-4-yl-3-trifluoromethylbenzenesulfonamide (19); [0258] NaB(OAc)3H (14 g, 66 mmol, Aldrich) was added to a mixture of compound 14 (10 g, 50 mmol, Aldrich), compound 15 (3 g, 52.5 mmol, Aldrich), molecular sieves (4A beads, 2Og, Aldrich) in DCE (200 ml) at 0 0C. The resulting mixture was stirred at room temperature for 24 hours. The reaction mixture was quenched with MeOH (2ml), filtered over celite, washed with water, 2N NaOH and concentrated under vacuum to afford crude compound 16 as a colorless oil. Compound 17 (12 g, 49 mmol, Aldrich) was added to a mixture of the above crude compound 16, TEA (10 ml) and DCM (10 ml) at room temperature. The resulting mixture was heated and stirred at 37 0C for 2 days. The reaction mixture was then cooled to room temperature, washed with water (10 ml), brine, concentrated and purified by column (silica gel, EtOAc/hexanes 3/7) to obtain compound 18 as a sticky oil (10 g, yield 45% in two steps), which was dissolved in 100 ml of 1,4-dioxane. HCl (10 ml, concentrated aq.) was added to the 1,4-dioxane solution at room temperature. The resulting mixture was stirred at room temperature for 48 hours, and concentrated under vacuum. The residue was washed with ethyl ether, and dried to obtain the title compound 19 as HCl-salt, which was suspended in EtOAc, and neutralized with IN NaOH aq, concentrated and dried under vacuum to give compound 19 as colorless oil (5 g, yield 65%).

534595-51-2, The synthetic route of 534595-51-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EURO-CELTIQUE S.A.; SHIONOGI & CO., LTD.; WO2007/118854; (2007); A1;,
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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: Chalcones analogs were synthesized by Claisen-Schmidt condensation reaction using appropriate equimolar amounts of substituted acetophenones and benzaldehydes in MeOH. NaOH was dissolved in the least amount of water and added dropwise (3mmol) (Scheme 1). Reactions were stirred overnight. All reactions were monitored by TLC using appropriate solvent or mixture of solvents. When the reaction was complete, the obtained precipitate was filtered, washed with cold methanol and dried under vacuum. The crude products were crystallized from different solvent systems based on their solubility or purified by column chromatography to give pure crystalline compounds., 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; Elkhalifa, Dana; Siddique, Abu Bakar; Qusa, Mohammed; Cyprian, Farhan S.; El Sayed, Khalid; Alali, Feras; Al Moustafa, Ala-Eddin; Khalil, Ashraf; European Journal of Medicinal Chemistry; vol. 187; (2020);,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.236406-22-7,1-Boc-4-(Aminomethyl)-4-methylpiperidine,as a common compound, the synthetic route is as follows.

Step 4. Synthesis of 4-benzyloxycarbonylaminomethyl-1-t-butoxycarbonyl-4-methylpiperidine To 6 ml of a tetrahydrofuran solution of 4-aminomethyl-1-t-butoxycarbonyl-4-methylpiperidine, obtained by Step 3, 1 ml of diisopropylehtylamine and 0.3 ml of benzyloxycarbonyl chloride were added successively, followed by stirring for 1 hour at the same temperature. The reaction mixture was diluted with ethyl acetate, washed successively with water and brine, and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and 324 mg of the crude title compound was obtained by purifying the resulting residue by silica gel column chromatography (eluding solvent: hexane/ethyl acetate=5/1~2/1)., 236406-22-7

236406-22-7 1-Boc-4-(Aminomethyl)-4-methylpiperidine 23282898, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Banyu Pharmaceutical Co Ltd; US6140333; (2000); A;,
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 3 Alternative synthesis of (3R,37?,4 ‘S)-l’-(6-amino-5-fluoropyrimidin-4-yl)-3-((3-chloro-5- (trifluoromethyl) phenyl)amino)-2-oxo- [ 1 ,3 ‘-bipiperidine] -4 ‘-carboxamide. [0101] In addition to the methods described in Example 2, (3R,3’R,4’S)- -(6-amino-5- fluoropyrimidin-4-yl)-3-((3-chloro-5-(trifluoromethyl) phenyl)amino)-2-oxo-[ 1 ,3 ‘-bipiperidine] – 4’-carboxamide (compound 1-1) was also synthesized according to Scheme 6. Scheme 6 3-1 3-2 [0102] 1-tert- utyl 4-ethyl 3-oxopiperidine-l,4-dicarboxylate 3-2. To a solution of 3-1 (5.0 kg, 19.1 mol, 1.0 equiv) in EtOH (50 L) under N2 was added (Boc)20 (4.2 kg, 19.1 mol, 1.0 equiv), Et3N (1.9 kg, 19.1 mol, 1.0 equiv) and 10percent Pd(OH)2/C (250 g, 10percentw/w). After evacuated and refilled with hydrogenation three times, the mixture was stirred under 1 atm of hydrogen at 50 °C for 15 hr. LC-MS indicated completely consumption of 3-1. After the mixture was cooled to ambient temperature, the catalyst was filtered through a layer of celite and washed with EtOH (2.5 L). The filtrate was concentrated in vacuo to afford crude 3-2 (5.2 kg) as an oil, which was used in next step without further purification.

39514-19-7, 39514-19-7 Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate 419705, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian T.; CONLON, Patrick; CHAN, Timothy R.; JENKINS, Tracy J.; CAI, Xiongwei; HUMORA, Michael; SHI, Xianglin; MILLER, Ross A.; THOMPSON, Andrew; WO2013/185084; (2013); A1;,
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161975-39-9, tert-Butyl 4-(((methylsulfonyl)oxy)methyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(cyanomethyl)piperidine-1-carboxylate tert-Butyl 4-{[(methylsulfonyl)oxy]methyl}piperidine-1-carboxylate (15.3 g) was dissolved in ethanol (80 mL), water (20 mL) and sodium cyanide (4.0 g, 80 mmol) were added, and stirring was conducted at 80 C. for 24 hours. Ethanol was distilled off, water and ethyl acetate were added, and then the resultant mixture was subject to Celite filtration, followed by extraction with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate and concentrated under a reduced pressure, and the obtained residue was purified by using silica gel column chromatography (hexane:ethyl acetate=3:1?2:1) to give tert-butyl 4-(cyanomethyl)piperidine-1-carboxylate (6.87 g, 77%, 3 steps) as a white solid. 1H-NMR (CDCl3) delta: 1.21-1.31 (2H, m), 1.46 (9H, s), 1.78-1.86 (3H, m), 2.31 (2H, d, J=6.4 Hz), 2.64-2.78 (2H, m), 4.07-4.21 (2H, m)., 161975-39-9

The synthetic route of 161975-39-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; KOWA CO., LTD.; Morimoto, Toshiharu; Koshizawa, Tomoaki; Watanabe, Gen; Ohgiya, Tadaaki; Yamasaki, Nao; Inoue, Noriyuki; US2013/102621; (2013); A1;,
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19099-93-5, 1-Cbz-Piperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

490 g of ammonium carbonate and 70 g of potassium cyanide were added to the reaction flask,700 mL of water and 700 mL of ethanol were added. Finally, 100 g of 1-benzyloxycarbonyl-4-piperidone was added, heated to 60 C, and reacted till the inorganic salt dissolves completely. After a period of time there will be a lot of crystals appear, reacted for 24 hours, and cooled to room temperature. The reaction solution was filtered off and the cake was washed with 1000 mL of water. The filter cake was then added to a 2000 mL mixture of ethanol and water (V ethanol: V = 4: 1), heated to 50C after slow cooling, followed by recrystallization to give 130 g of compound 5.

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

Reference：
Patent; Henan Normal University; Mao Longfei; Jia Shuhong; Li Wei; Wu Doucan; Dong Wenpei; Shen Jiaxuan; Jiang Tao; Xu Guiqing; Jiang Yuqin; (9 pag.)CN105017252; (2017); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem