Heterocyclic Building Blocks-piperidine

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;,
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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;,
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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;,
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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.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;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.221874-51-7,(R)-tert-Butyl (2-oxopiperidin-3-yl)carbamate,as a common compound, the synthetic route is as follows.

2-oxo-piperidin-3-yl carbamate (R)-tert-butyl (642 mg, 3.00 mmol) N, sodium hydride at room temperature to N- dimethylformamide (3 mL) solution of (132mg, 3.3 mmol) It was added. The reaction mixture was stirred for 30 minutes, iodomethane (206muL, 3.3 mmol) was added and stirring was continued for 1 hour. The reaction mixture was poured into water (50 mL), using the continuous extraction apparatus overnight, and extracted with EtOAc (100mL). The organic extract was evaporated to dryness under vacuum, the residue of the crude SiO2 chromatography (23g, CH2Cl2 / MeOH / NH4OH, 100: 0: 0 ~ 94: 5.7: 0.3) was purified by on, to give 1-methyl-2-oxo-piperidin-3-yl carbamic acid (R) -tert- butyl 310mg (45%) as a viscous oil colorless., 221874-51-7

221874-51-7 (R)-tert-Butyl (2-oxopiperidin-3-yl)carbamate 45092193, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; F.HOFFMANN-LA ROCHE AG; HENDRICKS, ROBERT THAN; HERMANN, JOHANNES CORNELIUS; KONDRU, RAMA K; LOU, YAN; LYNCH, STEPHEN M; OWENS, TIMOTHY D; SOTH, MICHAEL; (50 pag.)JP5667692; (2015); B2;,
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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.

A solution of 4-benzyloxycarbonylamino-piperidine-l-carboxylic acid tert-butyl ester (17.73 g, 53 mmol) in trifluoroacetic acid (30 ml) was stirred at room temperature for 30 min. The solvent was removed under reduced pressure and the residue was partitioned between IN aq, sodium hydroxide (30 ml) and a DCM-MeOH mixture (9-1, 100 ml). The aq. layer was extracted four more times with the same mixture. The combined extracts were dried over sodium sulfate, filtered and concentrated to dryness. The residue was chromatographed (DCM-MeOH 9-1 1% aq. ammonium hydroxide then DCM-MeOH 4-1) to afford the title piperidine (11.03 g, 47.07 mmol). .H NMR (CDC13) 8: 7.40-7.29 (m, 5H); 6.19 (br. s, 1H); 5.10 (s, 2H); 5.04 (s, 1H); 3.47 (m, 1H); 3.25 (br. d, J= 12.8 Hz, 2H); 2.81 (t, J= 12 Hz, 2H); 2.04 (m, 2H); 1.58 (m,2H)., 220394-97-8

220394-97-8 1-Boc-4-(Cbz-amino)piperidine 1514305, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ACTELION PERCUREX AG; WO2006/99884; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

140645-24-5, (S)-3-(Aminomethyl)-1-N-Boc-piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (S)-tert-hv&y 3-(aminomethyl)piperidine-l-carboxylate (500 mg,2.33 mmol) in CH2CI2 at -10 C was added triethylamine (650 uL, 4.66 mmol) followed by the dropwise addition of 2-methoxyethyl chloroformate (325 uL, 2.79 mmol). The reaction was warmed to room temperature and quenched with water. The aqueous layer was extracted with CH2CI2, and the combined extracts were dried over MgSCU, filtered, and evaporated. Purification via silica gel chromatography using 0 to 10%) EtOAc in CH2CI2 afforded 2-methoxyethyl ((iS)-l-(tert-butoxycarbonyl)piperidin-3-yl)methylcarbamate (496 mg, 67%). LC/MS: m/z 317.3 (M+H)+ at 2.56 min (10%-99% CH3CN (0.035% TFA)/H20 (0.05% TFA)). [001522] 2-Methoxyethyl ((i?)-piperidin-3-yl)methylcarbamate

140645-24-5, 140645-24-5 (S)-3-(Aminomethyl)-1-N-Boc-piperidine 1502022, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2006/28904; (2006); 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.24686-78-0,1-Benzoylpiperidin-4-one,as a common compound, the synthetic route is as follows.

EXAMPLE 1 Preparation of N-acetyl-4-piperidineacetaldehyde A 55 percent dispersion of sodium hydride in mineral oil containing 3.24 g. of a 55percent dispersion of sodium hydride in mineral oil was washed with three 50 ml portions of dry pentane and then the sodium hydride was suspended in 100 ml of anhydrous 1,2-dimethoxyethane (to be referred to hereinafter as DME). 16.58 g. of triethylphosphonoacetate in 50 ml of anhydrous DME were added to the sodium hydride suspension under a nitrogen atmosphere slowly with stirring and cooling to about 0° C. After the addition had been completed, the ice bath was removed and the mixture stirred for an additional hour at ambient temperature. The ice bath was then replaced and a solution of 10 g. of N-benzoyl-4-piperidone in 25 ml of anhydrous DME was added in dropwise fashion with stirring. After this addition had been completed, the ice bath was again removed and stirring continued for about three hours. Excess solvents were removed in vacuo from the reaction mixture. About 100 ml of an ice-water mixture were added. The resulting aqueous mixture was extracted with three 100 ml portions of ether, and the ether extracts separated, combined and dried. Removal of the ether therefrom in vacuo yielded a residue comprising N-benzoyl-4-(carbethoxymethylene) piperidine formed in the above reaction. Recrystallization of the residue from hexane yielded about 11.7 g. of colorless prisms of N-benzoyl-4-(carbethoxymethylene) piperidine melting at about 102°-103° C. N-benzoyl-4-(carbethoxymethylene) piperidine thus prepared had the following physical characteristics. Boiling point = 178°-180° C. at 0.03 mm Hg. nmr (CDCL3): delta1.28 (5, 3), 2.38 (broad m, 2), 3.05 (broad m, 2), 3.67 (broad m, 4), 4.18 (q, 2), 5.78 (broad s, 1), 7.41 (s,5). ir (KBr): 1715, 1660, 1620 cm-1. Anal: Calcd. for C16 H19 NO3: C, 70.31; H, 7.01; N, 5.13. Found: C, 70.42; H, 7.10; N, 5.07.

24686-78-0, Big data shows that 24686-78-0 is playing an increasingly important role.

Reference：
Patent; Princeton University; US3989691; (1976); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.885279-92-5,1-Boc-1,8-diaza-spiro[4.5]decane,as a common compound, the synthetic route is as follows.

A flask was charged with triphosgene (1.73 g, 5.82 mmol, 0.70 equiv), DCM (60 mL), and HFIP (2.80 g, 16.7 mmol, 2.00 equiv) under nitrogen. DIPEA (4.28 g, 33.2 mmol, 4.00 equiv) was added at 0 C, and then the reaction mixture was allowed to stir for 2 h at rt. tert-Butyl 1,8-diazaspiro[4.5]decane-1-carboxylate (2.00 g, 8.32 mmol, 1.00 equiv) was added and the mixture was stirred overnight. The mixture was then quenched with water (50 mL), extracted with DCM (2 x 80 mL) and the organic layers were combined, washed with brine (2 x 50 mL), dried over anhydrous sodium sulfate, filtered and concentrated. The residue was chromatographed on a silica gel column with EtOAc/petroleum ether (1/5) to provide 2.56 g (71% yield) of 1 -(tert-butyl) 8-(1,1,1,3,3,3 -hexafluoropropan-2-yl) 1,8- diazaspiro[4.5]decane-1,8-dicarboxylate as a yellow solid. LCMS (ESI, m/z): 435 [M+H]., 885279-92-5

885279-92-5 1-Boc-1,8-diaza-spiro[4.5]decane 34178602, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ABIDE THERAPEUTICS, INC.; GRICE, Cheryl A.; BUZARD, Daniel J.; SHAGHAFI, Michael B.; (150 pag.)WO2018/93949; (2018); 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.280774-03-0,(1-Isopropylpiperidin-4-yl)methanol,as a common compound, the synthetic route is as follows.

D. 1-Isopropylpiperidine-4-carboxaldehyde A solution of 1-isopropylpiperidine-4-methanol (0.40 g, 2.5 mmol) and N-methylmorpholine (0.46 g, 3.8 mmol) in methylene chloride (20 mL) was treated with tetrapropylammonium perruthenate (0.089 g, 0.25 mmol). After 3 h, the mixture was concentrated and the residue purified by column chromatography (SiO2: 10% to 20% methanol:methylene chloride) affording 0.20 g (50%) of the title compound. 1NMR; FIA-MS, m/e 156 (m+)., 280774-03-0

The synthetic route of 280774-03-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Eli Lilly and Company; US6635657; (2003); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem