Month: March 2022

53617-36-0,53617-36-0, 1-Methyl-4-(piperidin-4-yl)piperazine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 72; 4-methoxy-N,2,6-trimethyl-N-[2-[2-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]-2-oxoethoxy]ethyl]benzenesulphonamide; A suspension is prepared of 350 mg (1.06 mM) of acid obtained according to preparation III in 3 ml of DCM and 243 mg (1.27 mM) of EDCI (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) and 173 mg (1.27 mM) of HOAT, are added. The mixture is agitated for 30 min at ambient temperature, and 232 mg (1.27 mM) of 1-methyl-4-(4-piperidinyl)piperazine are then added. The reaction mixture is agitated for 18 hours at ambient temperature and is then poured over 10 ml of water and extracted with DCM. The organic phase is washed with water, dried and concentrated under reduced pressure. The residue is purified by silica gel chromatography in eluting with the aid of a DCM/methanol mixture (90/10; v/v). 449 mg of the product sought after are thus obtained as a yellow oil (yield=86percent). 1H NMR (300 MHz, CD3CN) delta: 6.74 (s, 2H); 4.35 (d, 1H); 4.01 (q, 2H); 3.81 (s, 3H); 3.69 (d, 1H); 3.56 (t, 2H); 3.26 (t, 2H); 2.89 (t, 1H); 2.75 (s, 3H); 2.58 (s, 6H); 2.40 (m, 10H); 2.17 (s, 3H); 1.75 (m, 2H); 1.27 (m, 2H).

53617-36-0 1-Methyl-4-(piperidin-4-yl)piperazine 795707, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Laboratoires Fournier S.A.; US2006/178360; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138022-04-5, tert-Butyl methyl(piperidin-4-ylmethyl)carbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl N-methyl-N-(4-piperidylmethyl)carbamate (3.00 g, 13.1 mmol, CAS138200-04-5) in a mixed solvent of CHCl3 (25 mL) and ACN (25 mL) was added K2CO3 (3.63 g, 26.2 mmol) and but-3-ynyl methanesulfonate (2.53 g, 17.0 mmol, Intermediate SG). The mixture was stirred at 70 C. for 16 hours. On completion, the reaction mixture was filtered and concentrated in vacuo to give a residue. The residue was purified by column chromatography (SiO2, PE/EA=6/1) to give the title compound (2.30 g, 62% yield) as light yellow oil. 1H NMR (400 MHz, CDCl3) delta 3.09 (d, J=6.8 Hz, 2H), 2.97-2.97 (m, 2H), 2.84 (s, 3H), 2.59 (t, J=8.0 Hz, 2H), 2.45-2.32 (m, 2H), 2.04-1.93 (m, 3H), 1.65-1.55 (m, 3H), 1.45 (s, 9H), 1.30-1.20 (m, 2H)., 138022-04-5

138022-04-5 tert-Butyl methyl(piperidin-4-ylmethyl)carbamate 23004743, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Kymera Therapeutics, Inc.; Mainolfi, Nello; Ji, Nan; Kluge, Arthur F.; Weiss, Matthew M.; Zhang, Yi; (1443 pag.)US2019/192668; (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.19099-93-5,1-Cbz-Piperidin-4-one,as a common compound, the synthetic route is as follows.

A mixtureof benzyl-4-oxopiperidine-1-carboxylate (11. 7 g, 50 mmol),potassium cyanide (4.87 g, 75 mmol) and ammonium carbonate (24 g, 250 mmol) in ethanol (100 ml), was placed in a stainless steel bomb and heated at 110C overnight. The reaction mixture was poured into ice-water(300 ml)and the resulting mixture was filtered. The pH of the mixturein water (100 ml)was adjusted to 2 by addition of anaqueous hydrochloric acid solution (6.0 M). The mixture was filtered and the filter cake was recrystallized15 from methanol: diethyl ether= 1:1 to afford benzyl-2,4-dioxo-1, 3,8-triazaspiro[4.5]decane-8-carboxylate as a white solid (10.0 g, 66%). LCMS (ESI): m/z = 304.1 [M+H(1 H-NMR (300 MHz, DMSO-d6):6 = 1.43-1.56 (m, 2H), 1.63-1.85(m, 2H), 2.45-2.60 (m, 2H), 3.33 (s, 2H), 3.88 (dd, J = 9.7, 4.0 Hz, 2H), 5.09 (s, 2H), 7.20-7.53 (m, 5H), 8.54 (s, 1H), 10.66 (s,1H). 20

19099-93-5, As the paragraph descriping shows that 19099-93-5 is playing an increasingly important role.

Reference：
Patent; X-RX DISCOVERY, INC.; BABISS, Lee; CLARK, Matthew; KEEFE, Anthony, D.; MULVIHILL, Mark, J.; NI, Haihong; RENZETTI, Louis; RUEBSAM, Frank; WANG, Ce; XIE, Zhifeng; ZHANG, Ying; WO2015/154023; (2015); 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.62718-31-4,1-Benzylpiperidine-4-carbonitrile,as a common compound, the synthetic route is as follows.,62718-31-4

Step a: To a solution of N^V-diisopropylamine (14.0 mL, 97.5 mmol) in THF (100 mL) was added (at -78 C and under N2) -butyllithium (1.6 M in hexane; 59.0 mL, 94.25 mmol) dropwise. The resulting mixture was stirred for 30 min at RT. 1-benzyl piperidine-4- carbonitrile (6.5 g, 32.5 mmol) in THF (50 mL) was added at -78 C. After stirring for 30 min at this temperature, -propyl iodide (20.5 mL, 211.3 mmol) was added. The resulting mixture was stirred at -78 C for 1 h. The mixture was quenched by addition of saturated aqueous ammonium chloride solution and it was extracted with EtOAc. The combined organic phases were washed with brine, dried over Na2S04, filtered and concentrated to obtain 1 -benzyl -4-propylpiperidine-4- carbonitrile (6.0 g, 24.8 mmol). This compound was used without further purification. MS m/z 243 (M+H)+.

As the paragraph descriping shows that 62718-31-4 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; CHEN, Zhuoliang; DORE, Michael; FORTANET, Jorge Garcia; KARKI, Rajesh; KATO, Mitsunori; LAMARCHE, Matthew J.; PEREZ, Lawrence Blas; WILLIAMS, Sarah; SENDZIK, Martin; WO2015/107494; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

24686-78-0, 1-Benzoylpiperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1′-Benzoyl-3,4-dihydro-6-methoxy-spiro[(2H)-1-benzopyran-2,4′-piperidine]-4-one Pyrrolidine (8.35 ml, 7.11 g, 0.1 mol) was added to a suspension of 2′-hydroxy-5′-methoxyacetophenone (16.62 g, 0.1 mol) in methanol (100 ml). The mixture was stirred for 10 minutes, then 1-benzoyl-4-piperidone (20.32 g, 0.1 mol) was added and the mixture was heated under reflux for 7 hr. The mixture was cooled and the solvent was evaporated under reduced pressure. Water (400 ml) was added and the mixture was extracted with ethyl acetate (3*400 ml). The combined organic fractions were evaporated under reduced pressure and the residue was recrystallized from methanol to give the ketone as a pale yellow solid (29.54 g, 84percent). 1 H NMR (CDCl3): delta7.41 (5H, s), 7.30 (1H, d, J=3.1 Hz), 7.12 (1H, dd, J=9.0, 3.1 Hz), 6.94 (1H, d, J=9.0 Hz), 4.5 (1H, br s), 3.8 (3H, s), 3.7-3.2 (3H, m), 2.73 (2H, s), 2.3-1.5 (4H, m)., 24686-78-0

As the paragraph descriping shows that 24686-78-0 is playing an increasingly important role.

Reference：
Patent; Merck & Co., Inc.; US5206240; (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,180307-56-6

Step B: tert-Butyl 4-[(E)-2-(4-Fluoro-l-oxo-13-dihydro-2-benzofuran-5-yl)ethenyllpiperidine- 1-carboxylate To a flask added 5-bromo-4-fluoro-2-benzofuran-l (3H)-one (0.10 g, 0.43 mmol) palladium(II)acetate (0.097 g, 0.043 mmol), triethylamine (0.12 mL, 0.88 mmol) and tert-butyl 4-ethyenylpiperidine-l-carboxylate (0.27 g, 1.2 mmol); the resulting mixture was then dissolved in DMF (15 mL) and heated in an oil bath at 130 C for 2 h. The flask was cooled to room temperature, diluted with EtOAc and washed with saturated sodium bicarbonate and water, then dried (Na2SC>4), filtered and adsorbed into silica gel. MPLC (hexanes/EtOAc = 1/1) purification provided tert-butyl 4-[(E)-2-(4-fluoro- 1 -oxo- 1 ,3-dihydro-2-benzofuran-5-yl)ethenyl]piperidine- 1-carboxylate. LC/MS: [(M+2)]+ =233.

180307-56-6 tert-Butyl 4-vinylpiperidine-1-carboxylate 10910832, apiperidines compound, is more and more widely used in various fields.

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;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

301225-58-1, tert-Butyl 4-(propylamino)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A 4-(N-((4-Nitrobenzyl)oxycarbonyl)-N-(prop-1-yl)amino)-piperidine trifluoroacetate The title compound was prepared by the reaction of 4-(N-(prop-1-yl)amino)-1-tert-butoxycarbonylpiperidine (from Example 17, Step A) with (4-nitrobenzyl)chloroformate, followed by treatment of the product with 50% TFA in CH2Cl2 to remove the tert-butoxycarbonyl group, affording the title compound. ESI-MS: 322.2 (M+H).

301225-58-1, As the paragraph descriping shows that 301225-58-1 is playing an increasingly important role.

Reference：
Patent; Merck & Co., Inc.; US6399619; (2002); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.23499-01-6,1-(4-Nitrophenyl)piperidin-4-one,as a common compound, the synthetic route is as follows.

EXAMPLE 224 1-(4-Amino-phenyl)-piperidin-4-one hydrochloride A mixture of 1-(4-nitro-phenyl)-piperidin-4-one (Synthesis 1981, 606) (4.0 g, 18 mmol) and 500 mg of 10% Pd/C in 75 mL of methylene chloride was hydrogenated under H2 (5~10 psi) for 1 hour. The catalyst was then removed by filtering through a short pad of silica gel. The filtrate was treated with hydrogen chloride gas and the precipitate was collected to give 2 g of the title compound as a tan solid; 1H NMR (300 MHz, DMSO-d6) delta 2.44 (t, J=6.0 Hz, 4H), 3.65 (t, J=6.0 Hz, 4H), 7.14 (d, J=9.0 Hz, 2H), 7.25 (d, J=9.0 Hz, 2H); MS (ES) m/z: 190.9 (MH+); HRMS Calcd. for C11H15N2O (MH+): 190.1106. Found: 190.1096., 23499-01-6

23499-01-6 1-(4-Nitrophenyl)piperidin-4-one 3842562, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Hu, Baihua; Sum, Fuk-Wah; Malamas, Michael S; US2002/28835; (2002); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

89895-06-7,89895-06-7, 1-(Piperidin-4-yl)ethanone hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 65 5-chloro-2-(piperidin-4-yl)-1H-indole A mixture of 0.60 gm (3.4 mMol) 4-chlorophenylhydrazine hydrochloride and 0.54 mL (6.7 mMol) pyridine in 20 mL ethanol were stirred at 60C for 15 minutes. To this mixture was then added 4-acetylpiperidine hydrochloride and the reaction mixture was stirred for 2 hours at 70C. The reaction mixture was concentrated under reduced pressure and the residue was treated with polyphosphoric acid. This mixture was heated at 90-100C for 48 hours. The reaction mixture was quenched with a slurry of ice in 5N sodium hydroxide. The aqueous mixture was extracted well with ethyl acetate. The organic phases were combined, washed with saturated aqueous sodium chloride, dried over sodium sulfate and concentrated under reduced pressure. The residue was subjected to silica gel chromatography, eluding with a dichloromethane gradient containing 4-20% methanol. Fractions containing product were combined and concentrated under reduced pressure to provide 0.26 gm (36%) of the title compound as a tan solid. MS(FD): m/e=234 (M+) EA: Calculated for: C13H15N2Cl: Theory: C, 66.52; H, 6.44; N, 11.93. Found: C, 66.24; H, 6.34; N, 11.73.

89895-06-7 1-(Piperidin-4-yl)ethanone hydrochloride 44151897, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ELI LILLY AND COMPANY; EP812826; (1997); 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.220223-46-1,Methyl N-Boc-3-Oxopiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: A solution of Intermediate 55b (0.79 g, 2.9 mmol) and benzyl bromide (0.40 mL,3.4 mmol) in N,N-dimethylacetamide (5 mL) is treated with powdered potassium carbonate (0.5 g, 3.6 mmol) and the mixture is stirred at 65 C overnight. The mixture is cooled, filtered, and concentrated in vacuo. Purification of the crude material by flash chromatography (hexanes/ethyl acetate gradient) affords 1-tert-butyl 3-ethyl 3-benzyl-4-oxopiperidine-1,3-dicarboxylate 55c as a clear oil.

220223-46-1, The synthetic route of 220223-46-1 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Azimioara, Mihai; Alper, Phil; Cow, Christopher; Mutnick, Daniel; Nikulin, Victor; Lelais, Gerald; Mecom, John; McNeill, Matthew; Michellys, Pierre-Yves; Wang, Zhiliang; Reding, Esther; Paliotti, Michael; Li, Jing; Bao, Dingjiu; Zoll, Jocelyn; Kim, Young; Zimmerman, Matthew; Groessl, Todd; Tuntland, Tove; Joseph, Sean B.; McNamara, Peter; Seidel, H. Martin; Epple, Robert; Bioorganic and Medicinal Chemistry Letters; vol. 24; 23; (2014); p. 5478 – 5483;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem