Day: September 4, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129888-60-4,tert-Butyl 3-((methylsulfonyl)oxy)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Stage (ii): tert-Butyl 3-iodopiperidine-1-carboxylate tert-Butyl 3-(methylsulfonyloxy)piperidine-1-carboxylate (0.54 g, 1.94 mmol) and sodium iodide (0.87 g, 5.8 mmol) were dissolved in acetone (10 ml) and the solution was refluxed under an inert gas for 6 h and then stirred at room temperature for 15 h. After thin layer chromatography control, the reaction mixture was heated in three portions in a microwave oven (CEM Discover): 10 min 100 C. 150 watt, 15 min 150 C. 200 watt, 20 min 100 C. 150 watt. After thin layer chromatography control, the three portions were combined, sodium thiosulfate solution (20 ml, 5 mmol/l) was added, the phases were separated and the aqueous phase was extracted with ethyl acetate (2*20 ml). The combined organic phases were washed with saturated sodium chloride solution (10 ml), dried over sodium sulfate and concentrated in vacuo. The crude product was purified by column chromatography (silica gel) with hexane/diethyl ether (3:1). Yield: 0.14 g (23%)

129888-60-4, 129888-60-4 tert-Butyl 3-((methylsulfonyl)oxy)piperidine-1-carboxylate 568122, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; GRUENENTHAL GmbH; US2010/152158; (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.22990-34-7,2-(4-Piperidyl)-2-propanol,as a common compound, the synthetic route is as follows.,22990-34-7

(a) A/-(2,2,2-Trifluoroethyl)-2-[4-(1-hydroxy-1-methyl-ethyl)-piperidinyl]-4-methy nitro-benzoic acid amideA mixture of 4-(1-hydroxy-1-methyl-ethyl)-piperidine (24 mg, 0.17 mmol), NaH-suspension (50% in mineral oil, 8 mg, -0.17 mmol) and THF (1 ml_) is stirred for 10 min. Then, Lambda/-(2,2,2- trifluoro-ethyl)-2-fluoro-4-methylamino-5-nitro-benzoic acid amide is added and it is stirred for 1.5 h. The mixture is diluted with EtOAc, washed with water, concentrated, dried and directly used in the next step.HPLC Rt = 1.34 min (method A). MS m/z: 419 [M+H]+.

22990-34-7 2-(4-Piperidyl)-2-propanol 5200321, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; PRIEPKE, Henning; DOODS, Henri; HEIM-RIETHER, Alexander; KUELZER, Raimund; PFAU, Roland; RUDOLF, Klaus; STENKAMP, Dirk; WO2012/76673; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

34622-39-4, (S)-2-Piperidinone-6-carboxylic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(b) (S)-6-Hydroxymethyl-piperidin-2-one To a solution of (S)-6-oxopiperidine-2-carboxylic acid (17 g, 120 mmol) in methanol (200 mL) was added thionyl chloride (87 mL, 1.2 mol) and the reaction mixture was stirred at RT overnight, concentrated, combined with the product of a similar preparation, washed with saturated aqueous NaHCO3, and extracted with EtOAc (4*200 mL). The organic layers were combined, dried over sodium sulfate and evaporated to provide crude (S)-methyl 6-oxopiperidine-2-carboxylate (36.5 g).

34622-39-4, 34622-39-4 (S)-2-Piperidinone-6-carboxylic acid 11126383, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; McKinnell, Robert Murray; Long, Daniel D.; US2013/287731; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

14691-88-4, 4-Amino-2,2,6,6-tetramethylpiperidine 1-Oxyl is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of this acid (110 mg, 0.296 mmol, crude) in dry DCM (3.5 mL) at 0 C. were added successively a solution of 4-amino-TEMPO (78.4 mg, 0.444 mmol) in dry DCM (0.5 mL), DMAP (40.2 mg, 0.326 mmol), HOBt.H2O (44.0 mg, 0.326 mmol) and EDCI (69.5 mg, 0.355 mmol). The resulting orange solution was stirred at room temperature under argon for 13 h, and then washed with sat. NH4Cl. The aqueous phase was separated and extracted once with DCM, and the combined organic layers were dried (Na2SO4), filtered and concentrated in vacuo. Flash chromatography (SiO2, EtOAc to 97:3, EtOAc/MeOH) afforded 91.2 mg (59%) of the title compound as an orange oil which solidified very slowly upon high vacuum. mp 168.0-168.8 C. (softening point: -75 C.); [alpha]D23 -14.1 (c 0.5, DCM); EIMS m/z 525 ([M+H]+, 10), 371 (27), 218 (28), 201 (74), 124 (100), 91 (35), 84 (26); HRMS (EI) n/z calcd for C30H43N3O3P 524.3042, found 524.3040., 14691-88-4

As the paragraph descriping shows that 14691-88-4 is playing an increasingly important role.

Reference£º
Patent; University of Pittsburgh – Of the Commonwealth System of Higher Education; Epperly, Michael W.; Gao, Xiang; Greenberger, Joel S.; Li, Song; Wipf, Peter; (63 pag.)US2019/210969; (2019); 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.2971-79-1,Methyl piperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: A mix of methyl piperidine-4-carboxylate or ethyl 2-(piperidin-4-yl)acetate (10 mmol) in acetonitrile (20 ml), 1a-j (11 mmol),anhydrous K2CO3 (12 mmol) was refluxed under nitrogen for 8 hat 85 C. The mixture was then cooled and filtered and the solvent removed in vacuum. The residue was dissolved in ethyl acetate(50 ml) and washed with water (15 ml). Drying and removal of the solvent followed by chromatography (ethyl acetate/petroleumether = 1:4) afforded desired product 2a-j.

2971-79-1, 2971-79-1 Methyl piperidine-4-carboxylate 424914, apiperidines compound, is more and more widely used in various.

Reference£º
Article; Wang, Jin; Wang, Zhi-Min; Li, Xue-Mei; Li, Fan; Wu, Jia-Jia; Kong, Ling-Yi; Wang, Xiao-Bing; Bioorganic and Medicinal Chemistry; vol. 24; 18; (2016); p. 4324 – 4338;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.157327-41-8,1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine,as a common compound, the synthetic route is as follows.

A mixture of 1-tert-butoxycarbonylpiperidine-4-one and N,N-dimethylformamide dimethylacetal was stirred for 6 hours heated to reflux to give 1-tert-butoxycarbonyl-3-[(dimethylamino)methylene]piperidine-4-one. A mixture of the obtained 1-tert-butoxycarbonyl-3-[(dimethylamino)methylene] piperidine-4-one, 2-hydrazinoethanol and MeOH was stirred for two hours heated to reflux to give a mixture of 2-(5-tert-butoxycarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-2-yl)ethanol and 2-(5-tert-butoxycarbonyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-1-yl)ethanol. A mixture of the obtained mixture, 4M HCl-EtOAc solution and EtOH was stirred for two hours at room temperature to give a mixture of 2-(4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-2-yl)ethanol dihydrochloride and 2-(4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c] pyridine-1-yl)ethanol dihydrochloride. ES-MS(+) : 168, 157327-41-8

157327-41-8 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine 53395404, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Astellas Pharma Inc.; EP1806347; (2007); 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.10315-07-8,1-Benzylpiperidine-4-carboxylic acid,as a common compound, the synthetic route is as follows.

General procedure: A 20 mL Radleys Carousel screw-capped glass tube was charged with carboxylic acid (2 mmol, 1.0 equiv), DMF (1.2 mL), T3P in DMF 50%(1.28 mL, 1.4 g, 1.1 equiv) and HCl (4 M in dioxane, 0.25 mL, 1.0mmol, 0.5 equiv) at r.t. The mixture was heated to 130 C (ca. 120 C internal) and stirred until the conversion according to LC-MS or TLCwas ?95%. The solution was quenched at 10 C with aq half-saturated Na2CO3 (5 mL; caution: gas evolution) and extracted with i-PrOAc (10mL and 2 ¡Á 5 mL or until no product was present in the aqueousphase). Combined organic phases were dried over MgSO4 and concentratedunder reduced pressure. The crude product was purified bychromatography on silica gel as described below. 1-Benzyl-N,N-dimethylpiperidine-4-carboxamide (17)The reaction was performed according to the general procedure with1-benzylpiperidine-4-carboxylic acid as starting material. Afterwork-up, the crude material was absorbed on Celite, concentrated todryness and purified by chromatography on silica gel (5 g Isolute SPEcolumn, Flash Si II; heptane-EtOAc, 4:1 to 1:9) to give 17.Yield: 450 mg (91%) yellow solid; mp 83.5-84.5 C.IR: 2926 (m), 1730 (w), 1635 (s), 1493 (m), 1341 (m), 1266 (m), 1139(m), 997 (m), 789 (w) cm-1. 1H NMR (500 MHz, CDCl3): delta = 7.31-7.35 (m, 4 H), 7.23-7.28 (m, 1 H),3.53 (s, 2 H), 3.05 (s, 3 H), 2.95 (m, 5 H), 2.49 (tt, J = 3.7, 11.4 Hz, 1 H),2.02 (t, J = 11.4 Hz, 2 H), 1.85-1.93 (m, 2 H), 1.68 (d, J = 12.9 Hz, 2 H).13C NMR (125 MHz, CDCl3): delta = 175.09, 138.45, 129.09, 128.19,126.96, 63.27, 53.21, 38.93, 37.06, 35.61, 28.53.MS: m/z = 247.16 [M + 1]+.HRMS (ESI): m/z [M + H]+ calcd for C15H22N2O: 247.1805; found:247.1809., 10315-07-8

10315-07-8 1-Benzylpiperidine-4-carboxylic acid 4714983, apiperidines compound, is more and more widely used in various.

Reference£º
Article; Bannwart, Linda; Abele, Stefan; Tortoioli, Simone; Synthesis; vol. 48; 13; (2016); p. 2069 – 2078;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

31140-42-8, 3-Boc-Amino-2,6-dioxopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl (2-78, 2,6-dioxopiperidin-3-yl)carbamate (1.0 g, 4.38 mmol) in THF (15 mL) was added NaH (263 mg, 6.57 mmol) at 0 C. After stirring for 20 minutes at room temperature, iodomethane (327 muL, 5.26 mmol) was added to the reaction mixture. After stirring for 2 hours, the mixture was diluted with EtOAc and quenched with water. The organic layer was collected and the aqueous layer was washed with EtOAc. The combined organic layers were dried over Na2SO4, filtered and concentrated. The crude compound 2-79 was carried forward in the next step without additional purification., 31140-42-8

The synthetic route of 31140-42-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DANA FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael; JANG, Jaebong; DE CLERCQ, Dries; ECK, Michael; (201 pag.)WO2017/185036; (2017); 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.167757-45-1,Benzyl 4-(aminocarbonyl)tetrahydro-1(2H)-pyridinecarboxylate,as a common compound, the synthetic route is as follows.,167757-45-1

General procedure: To a solution of the aldoxime or the amide (1.0 mmol) and Et3N (1.5mmol) in EtOAc (1 mL, 1 M) at r.t. was added XtalFluor-E8 (1.1 mmol)portionwise over ca. 2 min. The resulting solution was stirred at r.t.for 1 h. The reaction mixture was quenched with sat. aq Na2CO3 and extracted with CH2Cl2 (2 ¡Á 10 mL). The combined organic layers were washed with H2O and brine, dried (MgSO4), and concentrated under vacuum to afford the crude nitrile, which was purified by flash chromatography, if required.

167757-45-1 Benzyl 4-(aminocarbonyl)tetrahydro-1(2H)-pyridinecarboxylate 2776131, apiperidines compound, is more and more widely used in various.

Reference£º
Article; Keita, Massaba; Vandamme, Mathilde; Paquin, Jean-Francois; Synthesis; vol. 47; 23; (2015); p. 3758 – 3766;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

87120-72-7, tert-Butyl 4-aminopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

87120-72-7, Method G:Example G-1 : [1 -(4-Acryloylamino-benzenesulfonyl)-piperidin-4-yl]-carbamic acid benzyl ester4-Benzyloxycarbonylamino-piperidine-1 -carboxylic acid tert-butyl ester[00456] Diisopropylethylamine (0.9ml, 5.5mmol) was added in one portion to a stirred solution of 4-amino-piperidine-1 -carboxylic acid tert-butyl ester (1 .0g, 5.0mmol) in THF (10ml) at room temperature. To this mixture was added benzyl chloroformate (0.78ml, 5.5mmol) drop wise and the mixture was stirred at room temperature under a nitrogen atmosphere for 18 hours. After this time the mixture was diluted with ethyl acetate (50ml) and washed with water (100ml), saturated NaHCO3 (100ml) and HCl (100ml, 2M). The organic layer was separated, dried (MgSO ), filtered and concentrated under vacuum. The resulting residue was purified by flash column chromatography (elution: 50% heptane, 50% ethyl acetate) to give the title compound (1 .2g, 73% yield) as a colourless oil. Tr = 2.08 min m/z (ES+) (M+ Na+) 357.

The synthetic route of 87120-72-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHDI, INC.; DOMINGUEZ, Celia; WITYAK, John; PRIME, Michael; COURTNEY, Stephen; YARNOLD, Christoper; BROOKFIELD, Frederick; MARSTON, Richard; MACDONALD, Douglas; WO2011/60321; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem