Heterocyclic Building Blocks-piperidine

85275-45-2, tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The solution of N-Boc-3-hydroxypiperidine (2.1 g, 10 mmol, 1.0 eq) and DIPEA (2.1 mL, 15 mmol, 1.5 eq) in 20 mL DCM was stirred. To the solution was slowly added dropwise methanesulfonyl chloride (1.0 mL, 13 mmol, 1.3 eq) after cooling to 0 C., and mixture was allowed to raise to room temperature. Then the reaction mixture was washed successively with a 1 M HCl solution, saturated aqueous sodium bicarbonate solution, saturated aqueous sodium chloride solution and water. The obtained DCM layer was dried over anhydrous magnesium sulfate, filtered and evaporated to dryness to give the product as a yellow solid (2.65 g, 95.1% yield). MS m/z (ESI): 280.1 [M+H]., 85275-45-2

As the paragraph descriping shows that 85275-45-2 is playing an increasingly important role.

Reference£º
Patent; Si Chuan University; Yang, Shengyong; Wei, Yuquan; (168 pag.)US2017/305920; (2017); A1;,
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387827-19-2, tert-Butyl 4-(3-aminophenyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4 M HCl in dioxane (25 mL) was added to tert-butyl 4-[3-(amino)phenyl]-1-piperidinecarboxylate (2.60 g, 9.00 mmol) in dichloromethane (250 mL). The reaction mixture was stirred at room temperature overnight, concentrated in vacuo, and the residue was dissolved in water (50 mL). The mixture was nuetralized using KOH pellets and extracted with methylene chloride (3¡Á50 mL). The combined organic extracts were dried (MgSO4), concentrated and chromatographed to give the desired product (1.03 g). 1H NMR (400 MHz, CDCl3) delta 7.01 (t, 1H, J=7.6 Hz), 6.62-6.54 (m, 3H), 3.16 (br d, 2H, J=10.3 Hz), 2.75 (dt, 2H, J=2.7, 12.3 Hz), 2.56 (tt, 1H, J=3.6, 12.3 Hz), 1.81 (br d, 2H, J=12.3 Hz), 1.65 (dq, 2H, J=4.0, 12.3 Hz); ESMS m/e: 177.2 (M+H)+.

387827-19-2, 387827-19-2 tert-Butyl 4-(3-aminophenyl)piperidine-1-carboxylate 22049268, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Synaptic Pharmaceutical Corporation; US6727264; (2004); B1;,
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896464-16-7, tert-Butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,896464-16-7

Step 1: To a solution of compound 24a (1 equivalent) in dichloromethane, compound 11a (1.5 eq.) was added sequentially.HOAT (1.5 eq.), HATU (2 eq.), DIPEA (6 eq.), stirred at room temperature for 12 hours.The solvent is then sparged off and directly isolated by column chromatography to afford intermediate 24b.

As the paragraph descriping shows that 896464-16-7 is playing an increasingly important role.

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Chinese Academy Of Sciences Shanghai Life Sciences Institute; Zhang Ao; Gao Daming; Ni Jiabin; Hu Hongli; Ding Chunyong; (55 pag.)CN107814792; (2018); A;,
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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.832715-51-2,Isopropyl 4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

832715-51-2, 4,6-Dichloro-5-methylpyrimidine (1) (2.4235 Kg, 1.000 equivalents) and 4-hydroxypiperidine-1-carboxylic acid isopropyl ester (2) (2.8182 Kg, 1.012 equivalents) were dissolved in tetrahydrofuran (THF, 25.0028 Kg), and the resulting solution was cooled to -15 to -10 C. To the cold solution, potassium-tert-butoxide in tetrahydrofuran (1 M, 12.6051 Kg, 0.9399 equivalents) was added at a rate sufficiently slow to maintain the reaction mixture below 0 C. with reactor jacket cooling. The reaction mixture was then stirred at about -5 C. for about 2 hours before an additional portion of potassium-tert-butoxide in tetrahydrofuran (1 M, 0.5692 Kg, 0.0424 equivalents) was added to achieve >97% conversion of the pyrimidine after an additional hour of stirring at about -5 C. Most of the solvent was then removed by distillation at 30-65 C., 80 torr. Addition of water (19.9681 Kg) to the evaporation residue precipitated the product. Distillative removal of THF was then completed at 30-65 C., 80 torr, and the resulting stirred slurry was cooled to 0 C. for an hour. The solids were then collected by suction filtration, washed with water (8.011 Kg, 4 C.), and vacuum dried to constant weight at 50 C., 40 torr to provide product (3) (4.491 Kg, 96.3% yield).

As the paragraph descriping shows that 832715-51-2 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;,
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106-52-5, 1-Methylpiperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-((2′-chloro-4′-nitro-[1,1′-biphenyl]-4-yl)oxy)-1-methylpiperidine (28e): Diisopropylazo dicarboxylate (2.40 mmol) was added to a solution of phenol (1.20 mmol), PPh3 (2.40 mmol) and 4-hydroxy N-methyl piperidine (2.40 mmol) in THF (8 mL) at room temperature. The reaction mixture was stirred for 18 hours before the removal of solvent under reduced pressure. The remaining residue was purified by silica gel column chromatography (eluting with methylene chloride:methanol = 99:1 to 20:1) to yield a yellow amorphous solid (81%). 1H NMR (500 MHz, chloroform-d) delta 8.35 (d, J = 2.3 Hz, 1H), 8.15 (dt, J = 8.4, 2.2 Hz, 1H), 7.51 (d, J = 8.5 Hz, 1H), 7.43- 7.34 (m, 2H), 7.05- 6.94 (m, 2H), 4.41 (dt, J = 7.2, 3.7 Hz, 1H), 2.83- 2.65 (m, 2H), 2.34 (s, 3H), 2.07 (ddd, J = 13.9, 7.1, 3.5 Hz, 2H), 1.92 (ddd, J = 13.2, 7.9, 3.7 Hz, 2H). 13C NMR (126 MHz, CDCl3) delta 158.01, 146.90, 146.62, 133.42, 131.78, 130.57, 129.47, 125.32, 121.80, 115.58, 71.98, 52.60, 46.17, 30.74. HRMS (ESI+) m/z [M+H+] calcd for C18H19ClN2O3347.1163, found 347.1136.

106-52-5, 106-52-5 1-Methylpiperidin-4-ol 66048, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; THE UNIVERSITY OF KANSAS; BLAGG, Brian, S.J.; ZHAO, Huiping; WO2015/70091; (2015); A1;,
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832715-51-2, Isopropyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

832715-51-2, Step 3: 1 -Methylethyl 4-({7-[5-(methylthio)-2-pyridinyl]-6,7-dihydro-5H-pyrrolo[2,3- c/]pyrimidin-4-yl}oxy)-1 -piperidinecarboxylate (201) To a stirred solution of 200 (652 mg, 2.35 mmol) and 1 -methylethyl 4-hydroxy-1- piperidinecarboxylate 9 (526 mg, 2.81 mmol) in THF (24 mL) was added NaH (60% dispersion in mineral oil, 282 mg, 7.05 mmol) in one portion at RT. The reaction mixture was heated to reflux for 18 h, cooled to RT, and quenched with water (20 mL). The mixture was extracted with EtOAc (3 x 50 mL), dried over MgSO4, filtered, and concentrated under reduced pressure. The crude oil was purified using SiO2 flash chromatography (40% EtOAc in hexanes) to give 373 mg (37%) of the title product 201 as a colorless oil. 1H NMR (400 MHz, CDCI3): delta 8.73 – 8.66 (m, 1 H), 8.42 – 8.39 (m, 1 H), 8.30 (d, J = 2.4 Hz, 1 H), 8.77 – 8.70 (m, 1 H), 5.39 – 5.32 (m, 1 H), 4.92 (septuplet, J = 6.1 Hz, 1 H), 4.46 – 4.36 (m, 2 H), 3.85 – 3.76 (m, 2 H), 3.36 – 3.30 (m, 2 H), 3.12 – 3.05 (m, 2 H), 2.48 (s, 3 H), 2.03 – 1.95 (m, 2 H), 1.79 – 1.70 (m, 2 H), 1.25 (d, J = 6.4 Hz, 6 H); LCMS (ESI): m/z 430 (M + H)+.

The synthetic route of 832715-51-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2008/8895; (2008); A1;,
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3230-23-7, 4-Ethylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: B: Standard reaction procedure terminal alkyne: SeO2 (1.0 mmol) was added to a solutionof terminal alkyne (1.0 mmol) in dioxan (1 ml) followed by the addition of 10mol% of H2SO4 and amine (1.0 mmol). The reaction mixturewas then heated at 80oC for 10-12 h and the product formation wasmonitored by TLC. After completion, reaction mixture was partioned with waterethyl acetate, extracted with ethyl acetate (3 x 50ml). The combined organiclayers were washed with brine solution, concentrated on rotary evaporator andpurified by column chromatography using ethyl acetate and hexane to affordcorresponding pure products.

3230-23-7, 3230-23-7 4-Ethylpiperidine 76704, apiperidines compound, is more and more widely used in various fields.

Reference£º
Article; Meena, Samdarshi; Singh, Rohit; Vishwakarma, Ram A.; Aga, Mushtaq A.; Jain, Shreyans K.; Tetrahedron Letters; vol. 57; 33; (2016); p. 3715 – 3717;,
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4897-50-1, 4-Piperidinopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 2-tert-butoxycarbonylamino-4-oxo-4- [4- (2-oxo-1, 4- dihydro-2H-quinazolin-3-yl)-piperidin-1-yl]-butyric acid (1.14 g, 2.55 mmol) and 4- [PIPERIDINYL-PIPERIDINE] (525 mg, 2.81 mmol) in methylene chloride (20 [ML)] was added [3- (DIETHOXYPHOSPHORYLOXY)-1,] 2,3-benzotriain-4 [(3H)-ONE] (DEPBT, 840 mg, 2.81 mmol) in one portion followed by dropwise addition of triethylamine (0.427 [ML,] 3.06 mmol). The resulted mixture was stirred at room temperature overnight (15 h). The mixture was diluted with methylene chloride and washed with sodium hydroxide (0.5 N) solution and water. The layers were separated and the organic layer was dried with sodium sulfate and concentrated [IN VACUO] to give a light yellow foam. The crude product was purified by flash column chromatography (10percent [(1M] ammonia in methanol) in methylene chloride) to give a colorless foam (1.08 g, [71percent).] [APOS;H-NMR] (400 MHz, [CDC13)] [8] 8.86-8. 55 [(1H,] br), 7.05 [(1H,] br), 6.93 [(1H,] br), 6.82 [(1H,] br), 6.72 [(1H,] d, J = 7.6 Hz), 6.10-5. 68 [(1H,] br), 5.20 [(1H,] m), 54.70-4. 40 (2H, br), 4.20 (2H, br), 4. [01-3. 82] (2H, br. ), 3.10-2. 88 (3H, br), 2.99 (3H, br), 2.53 (6H, br), 1.90-1. 10 (23H, m). Mass spec.: 597 [(MH) +.]

4897-50-1, 4897-50-1 4-Piperidinopiperidine 78607, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2003/104236; (2003); A1;,
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648921-37-3, 3,3-Dimethyl-4-piperidone Hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

648921-37-3, Preparation of 1-66: A solution of 1-65 (4.20 g, 33.07 mmol) in CH2C12 (80 mL) was charged with benzyl chloroformate (6.70 g, 39.68 mmol) followed by triethyl amine (5.00 g, 49 mmol) over 20 min at 0C. The reaction mixture was stirred at RT for 16 h. The organic layer was washed with saturated NaHCC solution (50 mL), water (100 mL) and brine (50 mL). The organic layer was concentrated under reduced pressure to afford 1-66 as a liquid. MS (MM) m/z 262.1 [M + H]+.

648921-37-3 3,3-Dimethyl-4-piperidone Hydrochloride 57358418, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; IOMET PHARMA LTD.; MERCK SHARP & DOHME CORP.; COWLEY, Phillip, M.; MCGOWAN, Meredeth Ann; BROWN, Thomas, J.; HAN, Yongxin; LIU, Kun; PU, Qinglin; WISE, Alan; ZHANG, Hongjun; ZHOU, Hua; (70 pag.)WO2017/189386; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.287953-54-2,Benzyl 4-(chlorosulfonyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

(1) To a solution of Compound 1 (1574 mg) in dichloromethane (10 mL) was added an aqueous solution of dimethylamine (50% aqueous solution, 2 mL) under ice-cooling, and then the mixture was stirred at room temperature for 2 hours. To the reaction mixture were added an aqueous solution of hydrochloric acid (0.5 mol/L) and chloroform, stirred, then the organic layer was separated, washed with saturated saline, dried, and then concentrated under reduced pressure to give Compound 2 (1.609 g) as a colorless viscous material. MS (APCI): m/z 327 [M+H] +

287953-54-2, The synthetic route of 287953-54-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mitsubishi Tanabe Pharma Corporation; YAMAMOTO, Yasuo; SATO, Atsushi; MOROKUMA, Kenji; SHITAMA, Hiroaki; ADACHI, Takashi; MIYASHIRO, Masahiko; (260 pag.)EP3150578; (2017); A1;,
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