Day: August 27, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.143900-43-0,(R)-tert-Butyl 3-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture oftert-butyl (R)-3-hydroxypiperidine-l-carboxylate (5.15 g, 25 mmol) and Et3N (7.6 g, 77 mmol) in DCM (50 mL) was stirred at 0 C, MsCl (5.8 g, 52 mmol) was added to solution in dropwise, keep stirred for 3 h. The solvent was washed by saturated aqueous NaHC03 (50 mL 2) then brine (50 mL), dried over Na2S04, purified by flash chromatography on silica gel (DCM: 100%) to afford product as yellow solid, 3.06 g. ESI-MS m/z 280 (MH)+.

The synthetic route of 143900-43-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VENATORX PHARMACEUTICALS, INC.; BURNS, Christopher, J.; CHU, Guo-Hua; HAMRICK, Jodie; BOYD, Steven, A.; CONDON, Stephen, M.; (0 pag.)WO2019/232053; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1029413-55-5, tert-Butyl 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 4.178-[ [5-Fluoro-2- [ ri-(4-piperidyl)pyrazol-4-yll amino I -4-pyridyll amino I -2-methyl-3.,4- dihydroisoq uinolin- 1-one A mixture of 8-[(2-chloro-5-fluoropyridin-4-yl)amino]-2-methyl-3,4- dihydroisoquinolin- 1-one (100 mg, 0.33 mmol), tert-butyi 4-(4-aminopyrazol-l- yl)piperidine-l-carboxylate (114 mg, 0.43 mmol), sodium te/t-butoxide (51.5 mg, 0.54 mmol) and 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (41.4 mg, 0.07 mmol) in anhydrous dioxane (3 mL) was degassed with nitrogen and then bis(dibenzylideneacetone)palladium (32.7 mg, 0.057 mmol) was added. The mixture was heated at 15O0C for 30 minutes in a microwave reactor. MeOH (0.40 mL) was added and the mixture loaded onto an SCX column. The product was eluted first with MeOH and then with a 7M solution of NH3 in MeOH. Fractions containing product were combined and evaporated. The residue was stirred in a solution of HCl in dioxane (2 mL) overnight and then purified directly by preparative HPLC. Fractions containing product were combined and evaporated to afford example 4.17 (1.8 mg, 1% yield); 1H NMR spectrum (300 MHz, DMSO): delta 1.70 – 1.79 (2H, m), 1.89 (2H, d), 2.26 – 2.28 (2H, m), 2.54 (IH, d), 2.60 – 2.64 (IH, m), 2.71 – 2.74 (2H, m), 2.96 (IH, d), 3.00 (IH, s), 3.05 (3H, s), 3.55 (2H, t), 4.06 – 4.14; Mass spectrum: m/z (ESI+) (M+H)+ = 436.63.

1029413-55-5 tert-Butyl 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylate 27281520, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/153589; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

142752-12-3, 1-(4-Aminophenyl)piperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 23 7-[4-(4-Hydroxypiperidin-1-yl)phenylamino]-1-isopropyl-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2(1H)-one Prepared from 200 mg (0.79 mmol) of 1-isopropyl-7-methanesulfinyl-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2(1H)-one, 302 mg (1.57 mmol) of 1-(4-aminophenyl)-4-hydroxypiperidine and 182 muL (2.36 mmol) of trifluoroacetic acid in 3.2 mL of acetonitrile. After the workup, the crude residue is triturated in ethyl acetate/dichloromethane and filtered. The filtrate is concentrated further to produce a second crop of crystals. The two are combined and dried to give 45 mg (13%) of the title compound: mp >120 C. (dec). Analysis calculated for C20H26N6O2.0.3 C4H8O2.0.5 H2O: C, 60.93; H, 7.09; N, 20.11. Found: C, 60.95; H, 6.82; N, 20.35.

The synthetic route of 142752-12-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Dobrusin, Ellen Myra; Hamby, James Marino; Kramer, James Bernard; Schroeder, Mel Conrad; Showalter, Howard Daniel Hollis; Toogood, Peter; Trumpp-Kallmeyer, Susanne A.; US2004/44012; (2004); 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.7583-53-1,1-Methyl-3-piperidinemethanol,as a common compound, the synthetic route is as follows.

2-Nitro-4-trifluoromethyl-phenol (2.07 g,10 mmol) (1-methyl-piperidin-3-yl)-methanol (1.36 g,10.5 mmol) and triphenylphosphine (2.75 g, 10.5mmol), were diluted with 30 mL of THF and placedunder nitrogen. The reaction was cooled to 0¡ãC,then DIAD (2.12 g, 10.5 mmol) was added dropwise in2 mL of THF. The reaction mixture was allowed tostir for 12 hours while warming to room temperature.The reaction mixture was diluted with ethyl acetate(100 mL) and HCl (50 mL of 2N). Aqueous layer waswashed with ethyl acetate (2 x 50 mL), then basifiedwith solid sodium hydroxide to pH=12. The productwas extracted with ethyl acetate (3 x 50 mL), Theorganic layer was washed with brine, dried overMgS04, filtered, and dried under reduced pressure.The product was purified by Biotage 40M cartridgeeluting with CH2Cl2/MeOH/NH4OH (90/8/2) to yield ayellow solid.

As the paragraph descriping shows that 7583-53-1 is playing an increasingly important role.

Reference£º
Patent; ICOS CORPORATION; WO2006/12308; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

123855-51-6, tert-Butyl 4-(hydroxymethyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Boc-piperidinemethanol (27) or Boc-piperidineethanol (28) (23 mmol) dissolved in pyridine (50 mL) and cooled down under nitrogen. Then a tosyl chloride (27,87 mmol) was added portionwise. The was carried out for 3 h on bath-ice, then warm to room temperature and stirred for additional 10 h. The reaction mixture was extracted with CH2Cl2 (150 mL) and the organic phase was washed with 1 M KHSO4 (4 ¡Á 50 mL), water, brine and dried over Na2SO4. The tosyl derivatives (29, 30) were separated by column chromatography using SiO2 and CH2Cl2 followed by CH2Cl2/MeOH = 9/0.1. Next tosyl derivatives (2.44 mmol) were reacted with 4-chlorophenylpiperazine (2 mmol) by heating them in the presence of TEA (21.5 mmol) the boiling mixture of THF/toluene (5 mL/10 mL) for 20 h. After solvent evaporation the crude product was purified on silica gel column chromatography (CH2Cl2/MeOH 9/0.5, v/v) to yield Boc-protected piperidine 31 and 32. For the next stage the products were converted into their TFA salts and were isolated as white foams.

123855-51-6 tert-Butyl 4-(hydroxymethyl)piperidine-1-carboxylate 2764081, apiperidines compound, is more and more widely used in various.

Reference£º
Article; Zajdel, Pawe?; Marciniec, Krzysztof; Ma?lankiewicz, Andrzej; Sata?a, Grzegorz; Duszy?ska, Beata; Bojarski, Andrzej J.; Partyka, Anna; Jastrzbska-Wisek, Magdalena; Wrobel, Dagmara; Weso?owska, Anna; Paw?owski, MacIej; Bioorganic and Medicinal Chemistry; vol. 20; 4; (2012); p. 1545 – 1556;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

7149-42-0, (1-Methylpiperidin-4-yl)methanamine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

18.84 mg (0.050 mmol) of the intermediate compound (XII.7) and 22.77 mg (0.225 mmol) triethylamine are placed in 1 ml of ethanol, 9.62 mg (0.075 mmol) (1-methyl-piperidin-4-yl)-methylamine in 1 ml of ethanol are added. The reaction mixture is stirred for 16 hours at 70 C. Then the mixture is evaporated down, the residue is purified by chromatography (LCMS). Corresponding fractions are lyophilised. Yield: 15.70 mg (56% of theoretical)

As the paragraph descriping shows that 7149-42-0 is playing an increasingly important role.

Reference£º
Patent; Breitfelder, Steffen; Maier, Udo; Hoenke, Christoph; Joergensen, Anne T.; Pautsch, Alexander; Brandl, Trixi; Grauert, Matthias; Hoffmann, Matthias; Scheuerer, Stefan; Erb, Klaus; Pieper, Michael; Pragst, Ingo; US2007/238730; (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.52763-21-0,Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

A solution of NaOMe in MeOH (23.6 g, 25% in MeOH, 0.109 mol) is added to a stirred solution of formamidine (4.02 g, 38.6 mmol) in MeOH (50 ml) at rt. The mixture is stirred for 15 min. Ethyl-3-oxo-N-benzylpiperidine-4-carboxylate hydrochloride (9.58 g, 32.2 mmol) is added and the mixture is stirred at rt overnight. Acetic acid (2.33 g, 38.5 mmol) is added and the solvent is removed in vacuo. Water (100 ml) is added to the residue and the solution is extracted with DCM (2 x 100 ml). The combined extracts are washed with brine (40 ml) and dried (Na2SO4), and the solvent is evaporated to provide the title compound as a yellow solid, which is used in the next step without further purification.

52763-21-0 Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride 2723880, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; NEUROGEN CORPORATION; WO2007/146122; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

106243-23-6, 4-(1H-imdazol-4-yl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1.2. 2-[4-(1H-Imidazol-4-yl)piperid-1-yl]-5,6-dihydro-4H-imidazo-[4,5,1-ij]quinoline 1 g (0.0052 mol) of 2-chloro-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline, 1.57 g (0.0104 mol) of 4-(1H-imidazol-4-yl)piperidine and 5 ml of isoamyl alcohol are heated at 120 C. for 1 day. The alcohol is then evaporated to dryness, the residue is taken up in a water/ether (50/50) mixture and the product sucked dry. The product is purified by chromatography on a column of silica gel, the eluent being a dichloromethane/methanol/aqueous ammonia (95/5/0.5) mixture, is then triturated in ether and dried under vacuum at 60 C. 1 g of product is obtained. Melting point=250-255 C.

As the paragraph descriping shows that 106243-23-6 is playing an increasingly important role.

Reference£º
Patent; Synthelabo; US5589476; (1996); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

3466-80-6, 2-Phenylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Chloro-4-hydroxybenzoic Acid {2-Methoxy-4-[2-(2-phenylpiperidin-1-yl)ethoxy]benzylidene}hydrazide This compound was prepared analogously to the compound described in the previous example starting from resin bound 3-chloro-4-hydroxybenzoic acid hydrazide (resin-[building block 1]) (2 g, ~2 mmoles), 4-(2-bromoethoxy)-2-methoxybenzaldehyde ([building block 2]) (0.73 g, 1.5 equivs.), and 2-phenylpiperidine ([building block 3]) (3.0 g, 10 equivs.). After cleavage with 50% trifluoroacetic acid, the residue (1.0 g) was purified by column chromatography on silica gel (28 g) eluding with a mixture of methanol and dichloromethane (1:13). This afforded 0.24 g of the title compound. 1H-NMR (400 MHz, DMSO-d6): deltaH=1.4 (2H, m), 1.65 (4H, m), 2.25 (2H, m), 2.75 (1H, m), 3.16 (1H, d), 3.25 (2H, d), 3.83 (3H, s), 4.0 (2H, m), 6.50 (1H, d), 6.54 (1H, s), 7.07 (1H, d), 7.23 (1H, t), 7.35 (4H, m), 7.73 (1H, d), 7.77 (1H, dd), 7.96 (1H, d), 8.65 (1H, s), 10.9 (1H, s), 11.6 (1H, s).

3466-80-6 2-Phenylpiperidine 103020, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Novo Nordisk A/S; US6613942; (2003); 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.236406-39-6,8-Boc-2,8-Diazaspiro[4.5]decane,as a common compound, the synthetic route is as follows.

At room temperature,To a solution of tert-butyl 2,8-azaspiro[4,5]decane-8-carboxylate (192 mg, 0.88 mmol) in EtOAc (15 mL)And potassium carbonate (276 mg, 2 mmol),Stir at room temperature for 2 hours.Distilled water (30 mL) was added to the reaction mixture, and ethyl acetate (20 mL¡Á3).The layers were combined, dried over anhydrous magnesium sulfate, and concentrated, then purified by silica gel column (DCM: MeOH_NH3H2O=200:10:0.2)A pale yellow oil (260 mg).

The synthetic route of 236406-39-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Zhejiang Sitaili Pharmaceutical Co., Ltd.; Chinese Academy Of Medical Sciences Pharmaceutical Bio-technology Institute; Liu Mingliang; Guo Huiyuan; Lv Kai; Wang Apeng; Chai Yun; Huang Guocheng; Tao Zeyu; Li Xiaoning; Chen Shihong; (23 pag.)CN108484601; (2018); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem