Month: March 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.53617-36-0,1-Methyl-4-(piperidin-4-yl)piperazine,as a common compound, the synthetic route is as follows.,53617-36-0

(Example 32) N-(4-Fluorophenyl)-N’-(4-{[2-({[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}amino)pyridin-4-yl]oxy}phenyl)cyclopropane-1,1-dicarboxamide To a solution of [4-(4-{[1-(4-fluorophenylcarbamoyl)cyclopropanecarbonyl]amino}phenoxy)pyridin-2-yl]-N-(phenoxycarbonyl)carbamic acid phenyl ester (50 mg) in N,N-dimethylformamide (1.0 ml) was added 1-methyl-4-(piperidin-4-yl)piperazine (56.7 mg) at room temperature, followed by stirring overnight. The reaction mixture was partitioned between ethyl acetate and water. The organic layer was washed with a saturated aqueous solution of ammonium chloride and brine in this order, and dried over anhydrous sodium sulfate. The solvent was concentrated under reduced pressure. The resultant residue was purified by silica gel column chromatography (Fuji Silysia NH, eluent; ethyl acetate, then ethyl acetate:methanol = 95:5). Fractions containing the target compound were concentrated under reduced pressure. A solid was precipitated by addition of diethyl ether:heptane = 1:3 to the resultant residue. The solvent was removed under reduced pressure. The solid residue was dried under reduced pressure to provide the titled compound as white powder (37.7 mg, 79 percent). 1H-NNR Spectrum (CDCl3) delta (ppm): 1.40-1.94 (9H, m), 2.28 (3H, s), 2.30-2.70 (8H, m), 2.88 (2H, m), 4.02-4.14 (2H, m), 6.54 (1H, dd, J = 2.4, 5.6 Hz), 7.00-7.10 (4H, m), 7.23 (1H, brs), 7.45-7.60 (5H, m), 8.03 (1H, d, J = 5.6 Hz), 8.89 (1H, brs), 9.12 (1H, brs). ESI-MS (m/z): 616 [M+H]+.

As the paragraph descriping shows that 53617-36-0 is playing an increasingly important role.

Reference：
Patent; Eisai R&D Management Co., Ltd.; EP1889836; (2008); 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.952681-82-2,2-(1′-(tert-Butoxycarbonyl)spiro[chroman-2,4′-piperidine]-4-yl)acetic acid,as a common compound, the synthetic route is as follows.

952681-82-2, Preparation of 5.8:[0250] To a solution of the carboxylic acid 5.7 (433 mg, 1.2 mmol) in acetonitrile (15 mL) was added ./V,./V-diisopropylethylamine (0.86 mL, 4.9 mmol) and diethylamine (1.6) (0.36 mL, 3.5 mmol). The reaction mixture was cooled with ice-bath and TBTU (463 mg, 1.44 mmol) was added portionwise to the reaction mixture. The reaction mixture was stirred at room temperature overnight. The reaction mixture was concentrated, dissolved in ethyl acetate. The organic solution was washed with saturated aqueous sodium bicarbonate and dried over sodium sulfate. Evaporation of the solvent gave the crude product, which was chromato graphed using ethyl acetate/hexane (1:1) as eluent. Yield: 80%.1H NMR (400 MHz, CDCl3) delta 7.20 (m, IH), 7.10 (m, IH), 6.88 (m, 2H), 3.81 (m, 2H), 3.56-3.30 (m, 6H), 3.08 (m, IH), 2.92 (dd, IH), 2.40 (dd, IH), 2.12 (m, IH), 1.83-1.62 (m, 3H), 1.48 (s+m, HH), 1.20 (t, 3H).

952681-82-2 2-(1′-(tert-Butoxycarbonyl)spiro[chroman-2,4′-piperidine]-4-yl)acetic acid 56965736, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ADOLOR CORPORATION; WO2007/118151; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

50607-30-2, Piperidine-2,4-dione is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50607-30-2, Step 1) 4-hydroxypiperidin-2-one [0258] To a solution of piperidine-2,4-dione (1 g, 8.8 mmol) in MeOH (25 mL) was added NaBH4 (1 g, 26.55 mmol) at 0°C. The reaction was stirred at rt overnight, then concentrated in vacuo. The residue was purified by a silica gel column chromatography (DCM/MeOH (v/v) = 5/1) to give the title compound as ayellow solid (960 mg, 87percent). LC-MS (ESI, pos. ion) m/z: 138[M + Na]+.

As the paragraph descriping shows that 50607-30-2 is playing an increasingly important role.

Reference：
Patent; XI, Ning; WANG, Tingjin; YI, Lei; WO2013/138210; (2013); 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.3612-20-2,1-Benzylpiperidin-4-one,as a common compound, the synthetic route is as follows.

8-benzyl-1,3,8-triazaspiro[4.5]decane-2,4-dione1-Benzylpiperidin-4-one (49A) (20.0 g, 105.68 mmol)Soluble in ethanol (140mL), add potassium cyanide with stirring(14.3 g, 219.6 mmol) and water (140 mL),The mixture was stirred at 85 C for 36 hours.The reaction solution was cooled to room temperature, filtered, and the filter cake was washed with hot water (100 mL×3).The filter cake is dried to a white solid8-benzyl-1,3,8-triazaspiro[4.5]decane-2,4-dione (49B)(24.3 g, yield: 88.68%)., 3612-20-2

As the paragraph descriping shows that 3612-20-2 is playing an increasingly important role.

Reference：
Patent; Sichuan Hai Sike Pharmaceutical Co., Ltd.; Fan Jiang; Zhu Fengfei; Chen Qingping; Wang Chengtao; (251 pag.)CN109206417; (2019); 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.24686-78-0,1-Benzoylpiperidin-4-one,as a common compound, the synthetic route is as follows.

(a) 1-Benzoyl-4-(1-pyrrolidinyl)-1,2,3,6-tetrahydro- pyridine. In a 1000-ml round-bottomed flask equipped with a Dean-Stark apparatus, a condenser, a calcium chloride guard tube, a magnetic stirrer and oil-bath heating, 94.7 g (0.466 mole) of 1-benzoyl-4-piperidinone, 200 ml of toluene and 52.5 g (0.74 mole) of pyrrolidine are introduced. The mixture is heated under reflux until the water has been completely removed (approximately 3 hours). The mixture is allowed to cool and is evaporated. An orange oil remains.

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

Reference：
Patent; Synthelabo; US4661498; (1987); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

72551-53-2, Ethyl 1-benzylpiperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,72551-53-2

A 4N-aqueous sodium hydroxide solution (15 ml) was added to a solution of ethyl 1-benzyl-3-piperidinecarboxylate (7.00 g, 28.3 mmol) in a mixture of tetrahydrofuran (30 ml) and 1,4-dioxane (30 ml), and the resulting mixture was stirred at room temperature for 4 hours. After a 4N-aqueous sodium hydroxide solution (15 ml) was added again, the resulting mixture was stirred overnight at room temperature. After completion of the reaction, the reaction solution was neutralized by the addition of 2N-hydrochloric acid (15 ml) under ice-cooling and the resulting mixture was subjected to azeotropic concentration with toluene. The residue was suspended in ethanol, followed by filtration, and the filtrate was concentrated to obtain 1-benzyl-3-piperidinecarboxylic acid (6.3 g, 100%).

72551-53-2 Ethyl 1-benzylpiperidine-3-carboxylate 2736370, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Sumitomo Pharmaceuticals Company, Limited; EP1403255; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

936130-82-4,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.936130-82-4,Methyl 4-(piperidin-4-yl)benzoate hydrochloride,as a common compound, the synthetic route is as follows.

A solution of methyl 4-(piperidin-4-yl)benzoate, HCl (1.279 g, 5 mmol), N-ethyl-N-propan-2-ylpropan-2-amine (3.49 mL, 20.00 mmol) and 1-bromo-2-methoxyethane (0.470 mL, 5.00 mmol) in dichloromethane (10 mL) was heated at 40 C. or 18 h. A few drops of DMF were added to aid solubility. The reaction mixture was cooled, diluted with DCM (30 ml) and washed with water (2×30 ml) and saturated sodium chloride solution (30 ml). This was dried over MgSO4, filtered and evaporated to dryness. The crude product was purified by silica column chromatography, eluting with a gradient of 0 to 5% MeOH in DCM. Pure fractions were evaporated to dryness to afford methyl 4-(1-(2-methoxyethyl)piperidin-4-yl)benzoate (0.723 g, 52.1%) as a colourless oil. 1H NMR (399.9 MHz, CDCl3) delta 1.75 (1H, t), 1.81-1.90 (3H, m), 2.09-2.15 (2H, m), 2.55 (1H, q), 2.60-2.63 (2H, m), 3.08-3.11 (2H, m), 3.37 (3H, s), 3.53-3.56 (2H, m), 3.89-3.90 (3H, m), 7.27-7.31 (2H, m), 7.95-7.98 (2H, m). MS: m/z 278 (MH+).

As the paragraph descriping shows that 936130-82-4 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; US2008/153812; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

85908-96-9, N-Boc-2-Piperidone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

85908-96-9, [0151] N-Boc-lactam 2a-1 (300 mg, 1.50 mmol) was dissolved in THF (3 mL), a THF solution of phenylmagnesium bromide (1 mol/L solution, 1.5 mL, 1.50 mmol) was added at 0 C., and the mixture was stirred at 0 C. for 1 hr. Water (1.0 mL) was added, anhydrous sodium sulfate was added, water in the reaction system was removed, and the mixture was filtered through cotton. The obtained filtrate was concentrated by a rotary evaporator. The obtained crude product was purified by silica gel column chromatography (solvent :hexane and ethyl acetate) to give N-Boc-aminoketone 3a-1 (313 mg, 1.13 mmol) as a colorless liquid (yield 75%). MS: m/z 278 ([M+1], C16H23NO3

As the paragraph descriping shows that 85908-96-9 is playing an increasingly important role.

Reference：
Patent; SEED RESEARCH INSTITUTE CO., LTD.; ISHIKAWA, Teruhiko; IWAMI, Morita; (10 pag.)US2017/327513; (2017); 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

(S)-tert-butyl 3-((2-chloro-5-nitropyrimidin-4-ylamino)methyl) piperidine-1-carboxylate (12)[0074] To 1.267 g (6.53 mmol, 1.0 equiv.) of 2,4-dichloro-5-nitropyrimidine (Toronto Research Chemicals) in 8 mL of anhydrous THF at -78 0C was added dropwise a solution of 6.53 mmol (1 equiv.) of an amine and 1.25 mL of JV,iV-diisopropylethylamine in 6.5 mL anhydrous THF.[0075] The reaction mixture was stirred for 30 min at -78 0C and then allowed to warm to 25 0C and stirred for an additional 1 h. The solvent was removed in vacuo and the residue purified by flash chromatography on silica gel. EPO [0076] (S)-tert-butyl 3-((2-chloro-5-nitropyrimidin-4-ylamino)methyl) piperidine- 1- carboxylate (12):[0077] was synthesized using the procedure described above, using (S)-l-Boc-3- (aminomethyl) piperidine (1.4 g, 6.53 mmol, CNH Technologies) as the amine. Purification was performed on silica gel, using a 6 / 1 mixture of hexanes / ethyl acetate as the mobile phase. The desired product was obtained as a yellow solid (1.90 g) in 78 % yield. 1H NMR (300 MHz, CDCl3), ppm: 9.05 (s, IH), 8.56 (br s, IH), 3.85 (dd, 2H), 3.59 (m, 2H), 3.03 (br t, IH), 2.87 (dd, IH), 1.86 (m, 2H), 1.69 (m, IH), 1.46 (s, 9H), 1.40 (m, 2H, overlapping with 1.46 ppm).

140645-24-5, The synthetic route of 140645-24-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; N.V. ORGANON; PHARMACOPEIA INC.; WO2008/51826; (2008); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5810-56-0,4-Acetamidopiperidine,as a common compound, the synthetic route is as follows.

5810-56-0, EXAMPLE 22; 4-Acetamido-N-ethoxycarbonylpiperdine; A solution of 4-acetamidopiperidine (20.7 g), sodium bicarbonate (10.6 g) and water (300 ml) was cooled to 0C, and 17.7 g of ethyl chloroformate was added dropwise, with stirring. Upon completion of the addition, the reaction mixture was allowed to warm to ambient temperature and was diluted with water and ethyl acetate. The layers were separated, and the organic layer was washed with saturated sodium chloride solution, dried over anhydrous magnesium sulfate and filtered. The filtrate was evaporated to give 32.2 g (100%) of product.

As the paragraph descriping shows that 5810-56-0 is playing an increasingly important role.

Reference：
Patent; Aventis Pharmaceuticals Inc.; EP892802; (2003); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem