Day: March 9, 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.690261-64-4,2-(Piperidin-4-yl)pyrimidine hydrochloride,as a common compound, the synthetic route is as follows.

A solution of EDC.HCI (ALFA-AESAR, 340 mg, 1.77 mmol), TEA (ALFA-AESAR, 0.25 mL, 1 .77 mmol), HOBt (ALDRICH, 240 mg, 1 .77 mmol), Intermediate 30 (295.3 mg, 1.48 mmol) and 4,4,4-trifluorobutyric acid (ALFA-AESAR, 252 mg, 1.77 mmol) in DMF (15 mL) was stirred at rt overnight. The mixture was then washed with NaHCC>3 saturated solution and EtOAc was added, the two phases were separated and the aqueous one was further extracted with EtOAc. The collected organic layer was dried(anh) Na2SC>4, filtered and evaporated. The crude so obtained was purified by flash chromatography (Si SNAP 50, CyHex EtOAc from 1/1 to 0/10, then DCM/MeOH 8/2) to give title compound (141 mg, 33%) as a white solid. 1H NMR (500 MHz, DMSO-de) delta ppm: 8.75 (d, J = 4.9 Hz, 2H), 7.35 (t, J = 4.9 Hz, 1 H), 4.44 (d, J = 13.2 Hz, 1 H), 3.94 (d, J = 13.7 Hz, 1 H), 3.22-3.13 (m, 1 H), 3.13-3.05 (m, 1 H), 2.82-2.72 (m, 1 H), 2.70-2.57 (m, 2H), 2.57-2.45 (m, 2H), 2.02-1.90 (m, 1 H), 1.79-1.67 (m, 1 H),1.65-1.51 (m, 1 H). [ES+ MS] m/z 288 (MH+)., 690261-64-4

690261-64-4 2-(Piperidin-4-yl)pyrimidine hydrochloride 56965759, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BIOVERSYS AG; PORRAS DE FRANCISCO, Esther; REMUINAN-BLANCO, Modesto Jesus; BOUROTTE, Marilyne; DEPREZ, Benoit; WILLAND, Nicolas; (89 pag.)WO2019/34701; (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.10315-06-7,Methyl 1-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

1.5 (1-Benzylpiperidin-4-yl)-N-methoxy-N-methylcarboxamide A solution of 4.17 g (42.8 mmol) of N,O-dimethylhydroxylamine hydrochloride in 195 mL of THF is cooled to -20 C., and 6.51 g (28 mmol) of methyl (1-benzylpiperidin-4-yl)carboxylate are added. Next, 85 mL of a 1M solution of isopropylmagnesium bromide in THF are added over 20 minutes while keeping the temperature in the region of 5 C. The mixture is stirred at -10 C. for 20 minutes. The reaction medium is hydrolyzed with 40 mL of 20% ammonium chloride solution and then extracted with ethyl acetate. The combined organic phases are washed with water and with brine, and then dried over anhydrous sodium sulfate and evaporated under reduced pressure. 6.9 g of an oily product are obtained.1H NMR (DMSO-d6, 250 MHz) delta ppm: 1.5-1.75 (m, 4H); 1.9-2.05 (m, 2H); 2.55-2.7 (m, 1H); 2.8-2.9 (m, 2H); 3.09 (s, 3H); 3.46 (s, 2H); 3.67 (s, 3H); 7.2-7.4 (m, 5H).

10315-06-7, As the paragraph descriping shows that 10315-06-7 is playing an increasingly important role.

Reference：
Patent; SANOFI-AVENTIS; US2009/124624; (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.154307-84-3,(2S,5S)-5-Hydroxypiperidine-2-carboxylic acid hydrochloride,as a common compound, the synthetic route is as follows.

Step 2 To a solution of (2S,5S)-5-hydroxypiperidine-2-carboxylic acid, HCl (0.603 g, 3.32 mmol) in 1,4-dioxane (4 mL) and water (16 mL) was added potassium carbonate (1.835 g, 13.28 mmol) followed by (9H-fluoren-9-yl)methyl carbonochloridate (0.859 g, 3.32 mmol) at 0 C. The mixture was stirred at RT for 18 hrs and then treated with water (10 ml). The resulting mixture was extracted with diethyl ether (2*15 ml). The aqueous phase was acidified with aq. HCl (1M) to pH 2-3, and extracted with DCM (3*20 ml). The combined organic layers were dried over MgSO4 and concentrated to give the crude product (2S,5S)-1-(((9H-fluoren-9-yl)methoxy)carbonyl)-5-hydroxypiperidine-2-carboxylic acid (800 mg, 65.6% yield) as a white solid. 1H NMR (500 MHz, methanol-d4) d 7.86-7.78 (m, 2H), 7.69-7.57 (m, 2H), 7.48-7.37 (m, 2H), 7.37-7.20 (m, 2H), 4.81-4.77 (m, 1H), 4.59-4.36 (m, 2H), 4.32-4.20 (m, 1H), 4.18-4.08 (m, 1H), 3.75-3.64 (m, 2H), 3.58-3.43 (m, 1H), 2.01-1.89 (m, 1H), 1.81-1.57 (m, 1H), 1.30-1.17 (m, 1H). ESI-MS(+) m/z=368.2 (M+Na), 154307-84-3

The synthetic route of 154307-84-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; Miller, Michael Matthew; Mapelli, Claudio; Allen, Martin Patrick; Bowsher, Michael S.; Boy, Kenneth M.; Gillis, Eric P.; Langley, David R.; Mull, Eric; Poirier, Maude A.; Sanghvi, Nishith; Sun, Li-Qiang; Tenney, Daniel J.; Yeung, Kap-Sun; Zhu, Juliang; Reid, Patrick C.; Scola, Paul Michael; (892 pag.)US9308236; (2016); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

5810-56-0,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.

EXAMPLE 3 A mixture of 0.088 mole of 4-acetamidopiperidine, 15 g of potassium carbonate, 0.088 mole of 2-chloro-6-methoxypyridine in 100 ml of dimethylsulfoxide is heated with stirring to 130 C. for 50 hours, then it is cooled, the mixture is poured into water and the suspension thus obtained is extracted with diethyl ether. The aqueous phase is extracted with methylene chloride, the organic phase is washed with water, it is dried on anhydrous sodium sulfate and evaporated to dryness. 4-acetamido-1-(6-methoxy-2-pyridyl)piperidine is thus obtained which, after crystallisation in 95% ethanol, melts at 125 to 127 C. Yield: 43% of the theoretical.

5810-56-0 4-Acetamidopiperidine 1445156, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Sanofi; US4409228; (1983); 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.936130-82-4,Methyl 4-(piperidin-4-yl)benzoate hydrochloride,as a common compound, the synthetic route is as follows.

936130-82-4, To a stirred solution of methyl 4- (quinidin-4-yl) benzoate (5.0 g, 22.8 mmol) andPotassium carbonate (25.0 g, 182.2 mmol) in tetrahydrofuran (50 ml) / water (50 ml) was added portionwiseDi-n-butyl dicarbonate(10.0 g, 45.8 mmol) and keep the temperature below 10 C. After adding,The reaction mixture was stirred at room temperature for an additional 0.5 hour and then diluted with water (50 ml)And extracted with ethyl acetate (50 ml x 2). The combined organic layers were washed with brine,Dried over anhydrous sodium sulfate and concentrated in vacuo. The residue was purified by silica gel column chromatography (eluent: petroleum ether / ethyl acetate = 6/1 to 1/1) to give4- (4- (methoxycarbonyl) phenyl) piperidine-1-carboxylic acidThe third butyl ester(1.9 g, yield: 26.4%) as a white solid.

936130-82-4 Methyl 4-(piperidin-4-yl)benzoate hydrochloride 42614593, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.; DING, ZHAO ZHONG; WU, HAO; SUN, FEI; WU, LI FANG; YANG, LING; (97 pag.)TWI558709; (2016); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem