Day: November 9, 2020

166815-96-9, tert-Butyl 4-((tosyloxy)methyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-hydroxy-4-(4-bromo-2-fiuoroanilino)-6-methoxyquinazoline (100 g) and potassium carbonate (113.8 g) were suspended in iV-methylpyrrolidinone (1070 ml) and stirred for 10 minutes prior to the addition of l-(fert-butoxycarbonyl)-4-(4- methylphenylsulfonyloxymethyl)piperidine (152.2 g). The reaction mixture was then heated to 950C for 4 hours before being cooled back to 7O0C. Water (1922 ml) was then added over a period of 15 minutes. The reaction mixture was held at 730C for 1 hour before being cooled to 4O0C and the product isolated by filtration. The product was washed with water (549 ml), slurry washed with ethyl acetate (549 ml) at 5O0C for 1 hour and then washed with ethyl acetate (275 ml) and dried at 500C. Yield: 137 g, 86%; NMR Spectrum (DMSOd6) 1.15-1.3 (m, 2H), 1.46 (s, 9H), 1.8 (d, 2H), 2.0-2.1 (m, IH), 2.65-2.9 (m, 2H) 3.95 (s, 3H), 4.02 (br s, 2H), 4.05 (d, 2H), 7.2 (s, IH), 7.48 (d, IH), 7.55 (t, IH), 7.65 (d, IH), 7.8 (d, IH), 8.35 (s, IH), 9.55 (br s, IH); Mass Spectrum [ESI] (M+H)+ = 561-563.; 7-hydroxy-4-(4-bromo-2-fluoroanilino)-6-methoxyquinazoline (5.0 g) and potassium carbonate (5.7 g) were suspended in N-methylpyrrolidinone (53.5ml) and stirred for 10 minutes. l-(tert-butoxycarbonyl)-4-(4-methylphenylsulfonyloxymethyl)pirhoeridine (7.6 g) was then added. The reaction mixture was then heated to 950C and stirred at that temperature for 3.5 hours before being cooled back to 7O0C. Isopropanol (25 ml) was added and then water (75 ml) was added over a period of 15 minutes. The reaction mixture was then stirred at 730C for 1 hour before cooling to 4O0C and isolation of the product by filtration. The product was washed with water (27.4 ml) and dried at 5O0C. Yield: 6.72 g, 87.2%; NMR Spectrum (DMSOd6) 1.15-1.3 (m, 2H), 1.46 (s, 9H), 1.8 (d, 2H), 2.0-2.1 (m, IH), 2.65-2.9 (m, 2H) 3.95 (s, 3H), 4.02 (br s, 2H), 4.05 (d, 2H), 7.2 (s, IH), 7.48 (d, IH), 7.55 (t, IH), 7.65 (d, IH), 7.8 (d, IH), 8.35 (s, IH), 9.55 (br s, IH); Mass Spectrum [ESI] (M+H)+ = 561-563.

166815-96-9, The synthetic route of 166815-96-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/36713; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

167757-45-1, Benzyl 4-(aminocarbonyl)tetrahydro-1(2H)-pyridinecarboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of compound VI-A-43 (13.8 g), P2S5 (15.4 g) and anhydrous NaHCO3 (17.9 g) in ethylene glycol dimethyl ether (207 muL) was stirred at 60 C. overnight. After cooling to room temperature, the solution was filtered and concentrated to about of original volume, then poured into ice/water. The precipitated light yellow solid was collected by filtration and dried to give 13.5 g of intermediate X-B-43., 167757-45-1

The synthetic route of 167757-45-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

84163-13-3, 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

84163-13-3, 10g of reactant 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride and 10.4g of reactant 1-[4-(3-chloropropoxyl)-3-inethoxyphenyl]ethyl ketone were placed in a 250ml reaction flask, and a solution prepared with 17.9g potassium carbonate and 120ml water was added thereto. The reaction mixture was heated to 80-90 C and stirred for 1.5 hours, then naturally cooled to room temperature under stirring and filtered. The filter cake was washed twice with water, and then washed twice with methanol, and dried in vacuum at 50 C to obtain 15.1g crude iloperidone. The yield was 91.0%. The crude product was decolored by active carbon, then recrystallized with toluene to obtain iloperidone. The purity was 99.5% (determined by HPLC), and the melting point was 118~120C.

84163-13-3 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride 11334359, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhejiang Huahai Pharmaceutical Co., Ltd.; EP2479176; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

154775-43-6, 3-(1-(tert-Butoxycarbonyl)piperidin-4-yl)propanoic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154775-43-6

Step A Iodomethane (556 muL, 8.93 mmol) was added dropwise to a cooled (0 C.) mixture of commercially available 3-[1-(tert-butoxycarbonyl)piperidin-4-yl]propanoic acid (2.09 g, 8.12 mmol) and K2CO3 (2.81 g, 20.3 mmol) in 20 mL of DMF. The reaction mixture was permitted to warm to rt and stir overnight. The reaction mixture was diluted with ether and washed four times with water, then once with brine. The ethereal layer was dried over anhydrous MgSO4, filtered, and concentrated. Purification by MPLC (silica, 40% ethyl acetate/hexanes) provided tert-butyl 4-(3-methoxy-3-oxopropyl)piperidine-1-carboxylate:

The synthetic route of 154775-43-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Goble, Stephen D.; Mills, Sander G.; Yang, Lihu; Pasternak, Alexander; US2007/238723; (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.71233-25-5,1-tert-Butyl 4-ethyl 3-oxopiperidine-1,4-dicarboxylate,as a common compound, the synthetic route is as follows.,71233-25-5

G. 5-Amino-3,6-dihydro-2H-pyridine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester (35a2) To a solution of 34a2 (24 g, 88.5 mmol) was added ammonium in EtOH (88 mL, 180 mmol, 2M). The reaction mixture was heated to 60 C for 3 h. The solvent was evaporated under reduced pressure to afford a yellow solid (23 g, 91.5percent). MS (ES+): m/z=271 (M+1)

The synthetic route of 71233-25-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hurley, Timothy Brian; Lee, Kwangho; Peukert, Stefan; Wattanasin, Sompong; US2009/325948; (2009); 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.24211-55-0,(S)-Piperidin-3-ol,as a common compound, the synthetic route is as follows.

2,3′-difluoro-4′-((1-(2-fluoro-2-methylpropyl)piperidin-4-yl)methoxy)biphenyl-4-carboxylic acid (0.04 g, 0.10 mmol) and (S)-piperidin-3-ol (0.02 g, 0.19 mmol) were dissolved in DMF 2 mL. DIPEA (0.08 mL, 0.48 mmol), EDCI (0.04 g, 0.19 mmol) and HOBt (0.03 g, 0.19 mmol) were added thereto slowly, following with stirring at 60 C. for 3 hours. After the completion of the reaction, excess amount of water was added to the reaction mixture. The resulting precipitate was filtered, and dissolved in CH2Cl2. The solution was concentrated under reduced pressure. The obtained concentrate was purified by column chromatography (40 g ISCO silica gel cartridge, 0-20% MeOHCH2Cl2) to yield the title compound as light-yellow solid (0.02 g, 42%). 1H NMR (400 MHz, CDCl3) delta 7.40 (t, 1H, J=5.8 Hz), 7.29-7.21 (m, 4H), 6.99 (t, 1H, J=6.4 Hz), 3.88 (d, 2H, J=4.6 Hz), 3.78-3.27 (m, 4H), 2.97 (d, 2H, J=8.2 Hz), 2.45 (s, 1H), 2.40 (s, 1H), 2.16 (t, 2H, J=8.5 Hz), 1.91-1.65 (m, 7H), 1.45-1.23 (m, 8H); MS (ESI) mz 505 (M++H)

24211-55-0, The synthetic route of 24211-55-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; Lee, ChangSik; Jang, TaegSu; Choi, DaeKyu; Ko, MooSung; Kim, DoHoon; Kim, SoYoung; Min, JaeKi; Kim, WooSik; Lim, YoungTae; US2015/166480; (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.91419-48-6,tert-Butyl 4-carbamoylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

91419-48-6, 2) Second Step: Synthesis of the t-butyl ester of 4-cyanopiperidine-1-carboxylic acid 2.05 g (9 mmol) of the t-butyl ester of 4-carbamoylpiperidine-1-carboxylic acid as obtained in the first step above were introduced into a Schlenck tube in the presence of 1.7 ml of DIEA (1-1 eq.). The medium was flushed under argon, and 18 ml of anhydrous THF were then added. The reaction medium was then cooled to a temperature of 0 C. and 1.38 ml of trifluoroacetic anhydride (1.1 eq.) were added dropwise. The medium then became totally clear. If the reaction is not complete after 1 hour, a further 0.5 equivalent of DIEA and then of trifluoroacetic anhydride are added. The reaction was monitored by TLC, staining with ninhydrin. At the end of the reaction, the organic phase was washed successively with aqueous solutions of 5% NaHCO3, 0.1N KHSO4 and saturated NaCl solution. The expected product was not visible under UV light. In the event of appearance of a UV-visible compound, a purification by flash chromatography in a gradient of eluent ranging from cyclohexane up to a 9/1 cyclohexane/ethyl acetate mixture may be performed. 1.1 g of a very pale yellow liquid that solidified after a few hours were obtained.1H NMR: (CDCl3): 3.63 (m, 2H), 3.36 (m, 2H), 2.8 (m, 1H), 1.84 (m, 4H), 1.45 (s, 9H).MS m/z: 211 (M++1)

91419-48-6 tert-Butyl 4-carbamoylpiperidine-1-carboxylate 2735646, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Institut Pasteur De Lille; Centre National De La Recherche Scientifique; Universite De Lille 2, Universite Du Droit Et De La Sante; Institut National De La Sante Et De La Recherche Medicale (Inserm); US2011/136823; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

50585-89-2, Methyl piperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50585-89-2, Potassium 3-methoxycarbonyl-piperidine-1-carbodithioate (13 Kmpc) was prepared by the dropwise addition of 14 CS2 (1.2mL, 20mmol) into a solution of methyl nipecotate (2.8mL, 20mmol) in 15 methanol (30mL) in the presence of 16 KOH (1.2g, 20mmol), stirring the reaction mixture for 1h. The yellow solid which separated was filtered off, washed with ethanol and thereafter with ether and dried (Scheme 2 ). Yield: 80%; m.p. 202C. Anal. Found: C, 37.15; H, 4.88; N, 5.70; S, 24.58%. Calc. for C8H12NO2S2K (257.40): C, 37.32; H, 4.70; N, 5.44; S, 24.91%. IR (KBr, cm-1): nu(C-H) 2944, 2857; nu(C=O) 1658; nu(CN) 1565; nu(C=S) 1012. 1H NMR (CDCl3: delta, ppm): 1.68-2.43 (m, H-3, H-4, H-5), 2.64 (t, 2H, H-6axial), 2.91 (d, 2H, H6-equatorial), 2.82 (t, 2H, H-2axial), 3.13 (d, 2H, H-2equatorial), 4.09 (s, 3H, -OCH3). 13C NMR (CDCl3: delta, ppm): 23.88-49.99 (piperidine ring), 51.01 (-OCH3), 173.50 (C=O), 212.46 (C=S).

The synthetic route of 50585-89-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Nath, Paras; Bharty; Kushawaha; Maiti; Polyhedron; vol. 151; (2018); p. 503 – 509;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1022150-11-3, (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 2.5g (5.1mmol) of formula 10 was added to the methanol solution in 25ml of hydrochloric acid, stirred at room temperature 2hour. Concentrated under reduced pressure, the residue was added 30ml of water, extracted with ethyl acetate, the organic phase was washed with 5% aqueousSodium hydroxide solution was washed until neutral. The organic phase was concentrated under reduced pressure to give a pale yellow oil 1.82g, yield 92%

1022150-11-3, The synthetic route of 1022150-11-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Okuura Dayton (Shanghai) Pharmaceutical Co., Ltd.; Yu, Libing; Guo, Maojun; Yang, Qingang; Ren, Huasen; (19 pag.)CN105622613; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

37675-18-6, (S)-Ethyl piperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 5 To a mixture of (S)-ethyl nipecotate (1.15 g) and tetrahydrofuran (16 ml) was added lithium aluminum hydride (278 mg) at 0C. The mixture was stirred for 3 hours with elevating the temperature to room temperature. Water (0.28 ml), 25% potassium hydroxide solution (0.28 ml) and water (0.84 ml) were added thereto in this order, and the mixture was stirred for 15 hours. The insolubles were filtered off using celite and the mother liquor was concentrated, to give (S)-3-(hydroxymethyl)piperidine (797 mg). [alpha]D = -11.3 (c = 0.730, MeOH). 1H-NMR (300 Hz, CDCl3) delta: 1.07-1.20 (1H, m), 1.40-1.54 (1H, m), 1.61-1.82 (3H, m), 2.39 (1H, dd, J=12.0 and 9.9 Hz), 2.54-2.62 (3H, m), 2.95-3.01 (1H, m), 3.13-3.18 (1H, m), 3.40-3.54 (2H, m).

37675-18-6, The synthetic route of 37675-18-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP1553074; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem