Day: August 26, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.62718-28-9,1-Methylpiperidine-4-carboxamide,as a common compound, the synthetic route is as follows.

Intermediate 20: step a 1-Methylpiperidine-4-carbothioamide To a suspension of 1-methylpiperidine-4-carboxamide (3.97 g, 27.9 mmol, Amfinecom) in a mixture of toluene (70 mL) and THF (30 mL) was added Lawesson’s reagent (6.78 g, 16.8 mmol). The resulting light yellow suspension was heated at reflux for 22 h. The reaction mixture was diluted with DCM and MeOH and was concentrated onto silica gel for purification by column chromatography (Silica gel, 1-8% MeOH in 98:2 DCM:conc. aq. NH4OH, water layer removed in a separatory funnel), affording the title compound as a yellow solid.

62718-28-9 1-Methylpiperidine-4-carboxamide 339011, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; JACKSON, Paul Francis; Manthey, Carl; Rhodes, Kenneth; Scannevin, Robert; Leonard, Kristi Anne; Barbay, Joseph Kent; Todd, Matthew; Springer, Barry A.; US2012/302573; (2012); A1;,
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91419-48-6, tert-Butyl 4-carbamoylpiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-CARBAMOYL-PIPERIDINE-L-CARBOXYLIC acid TERT-BUTYL ester (2) (45.4 g, 0.199 mol), Lawesson’s reagent (40.2 g, 0.099 mol, 0.5 equiv), 1,2-dimethoxyethane (DME) (500 mL) and chloroform (200 mL) were combined and stirred at room temperature. The course of the reaction was followed by tlc analysis (30% ethyl ACETATE/HEXANE) and on completion the reaction mixture was evaporated to dryness (glassy solid). The solid was dissolved in ethyl acetate and washed with half saturated potassium carbonate solution, dried (MGSO4), filtered and concentrated to yield the title compound as a colourless solid. The crude product was crystallised from ethyl acetate and hexane to give the title compound (3) (35 g, 0.14 mol, 72%).

As the paragraph descriping shows that 91419-48-6 is playing an increasingly important role.

Reference£º
Patent; METRIS THERAPEUTICS LIMITED; WO2004/58750; (2004); A1;,
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143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

20 g of (S)?N-Boc-3-pyridinol was dissolved in 100 mL of toluene, and 21 mL of triethylamine and 9.2 mL of methanesulfonyl chloride were added thereto at 0¡ã C. The mixture was stirred for 1 hour under ice cooling, subsequently ethyl acetate and water were added thereto, and an organic layer was separated. The organic layer was washed with a saturated aqueous solution of sodium hydrogen carbonate, a saturated aqueous solution of ammonium chloride and water, and then was dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and thus 26.8 g of the title compound was obtained as a colorless solid.

As the paragraph descriping shows that 143900-44-1 is playing an increasingly important role.

Reference£º
Patent; TAIHO PHARMACEUTICAL CO., LTD.; Hosoi, Fumihito; Nakachi, Yoshinori; Kajiwara, Daisuke; (63 pag.)US9782412; (2017); B2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24666-56-6,3-Aminopiperidine-2,6-dione hydrochloride,as a common compound, the synthetic route is as follows.

Methyl-4-bromo-2-(bromomethyl) benzoate (100 g, 324.70 mmol), 3-Aminopiperidine-2,6-dione.hydrochloride (53.2 g, 324.70 mmol), triethylamine (113.29 mL, 811.75 mmol), and dry dimethylformamide (400 mL) were combined and stirred at room temperature under inert atmosphere for 18 hours. The reaction was cooled to 5C and diluted with water (400 mL), acetic acid (115 mL), diethylether (300 mL) with continued stirring at room temperature for 2 hours. The resultant solid was filtered, washed with ether (100 mL) and further dried under high vacuum to give 3-(5-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (46 g, 142.35 mmol, 43.8 % yield) as a light blue solid. MS(ESI) m/z 325.0 [M+1].

24666-56-6 3-Aminopiperidine-2,6-dione hydrochloride 134548, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; CELGENE CORPORATION; ALEXANDER, Matthew, D.; CORREA, Matthew, D.; HANSEN, Joshua; RAHEJA, Raj, Kumar; SAPIENZA, John; (128 pag.)WO2017/120422; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216854-23-8,(S)-tert-Butyl piperidin-3-ylcarbamate,as a common compound, the synthetic route is as follows.

A solution of tot-butyl (3S)-piperidin-3-ylcarbamate (499 mg, 0.00249 mol; CNH Technologies) and triethylamine (0.52 mL, 0.0037 mol) dissolved in methylene chloride (5.0 mL, 0.078 mol) was cooled to 0 C and to this was added 3-chloro-2-methylbenzenesulfonyl chloride (0.62 g, 0.0027 mol) (6:56). After stirring for 10 min. the reaction mixture was allowed to gradually warm to rt while stirring for 24h. The reaction was quenched with water (1:09), diluted with EtOAc and 0. IN HC1 and brine were added. The layers were separated and the organic layer was washed with saturated sodium bicarbonate, brine, dried (Na2S04), filtered, and concentrated in-vacuo to afford 1.03g of the desired product as awhite solid. The .HNMR confirmed that the desired product was isolated.

The synthetic route of 216854-23-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INCYTE CORPORATION; WO2006/20598; (2006); A2;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.256411-39-9,1-Boc-4-(Cyanomethyl)piperidine,as a common compound, the synthetic route is as follows.

Step A: 4-(N-HYDROXYCARBAMIMIDOYLMETHYL) PIPERIDINE-1-CARBOXYLIC acid tert-butyl ester. To a solution OF 4- (CYANOMETHYL) PIPERIDINE-1-CARBOXYLIC acid tert-butyl ester (2.2 g, 10 MMOL, prepared as described in Example 12) in absolute ethanol (20 mL) was added hydroxylamine hydrochloride (2.1 g, 30 MMOL), water (4 mL) and potassium carbonate (2.2 g, 16 MMOL). The reaction mixture was stirred 30 min. at ambient temperature and then heated overnight at reflux for 6 h. Water (10 mL) was added and the mixture was allowed to cool on an ice-bath. The solid inorganic material was removed by filtration and the solvent was evaporated. The residue was treated with DICHLOROMETHANE, dried and evaporated. The oily residue was sub- mitted to column chromatography (100 g, kiselgel 60) with ethyl acetate as eluent. The frac- tions eluting at Rf = 0.32 were collected to give 0.67 g OF 4- (N- HYDROXYCARBAMIMIDOYLMETHYL) PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER.’H NMR (400 MHz, CDCI3) 8 1.07-1. 20 (m, 2H), 1.45 (s, 9H), 1.67-1. 77 (m, 3H), 2.06 (d, 2H), 2.62-2. 77 (m, 2H), 4.1 (brs, 2H), 4.54 (s, 2H), 7.7 (brs, 1H). HPLC: Rt = 6.43 min.

The synthetic route of 256411-39-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVO NORDISK A/S; WO2004/54973; (2004); A2;,
Piperidine – Wikipedia
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169750-96-3, tert-Butyl (3-methylpiperidin-3-yl)carbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-[4-(2-tert-butyl-4-pyridyl)-2-thienyl]-3-chloro-benzoic acid (300 mg, 0.8086 mmol) in DMF (10 mL), was added DIPEA (418 mg, 3.2344 mmol), followed by the addition of HATU (615 mg, 1.6172 mmol). The reaction mixture was stirred for 30 min at RT. tert-Butyl N-(3-methyl-3-piperidyl)carbamate (433 mg, 2.022 mmol) was added and the reaction mixture stirred for 16 h at RT. The reaction was monitored by TLC and LCMS. On completion, the reaction mixture was diluted with water (50 mL) and extracted with EtOAc (2*100 mL). The combined organic layer was washed with water (2*50 mL) and brine (2*50 mL) and dried over anhydrous sodium sulfate to obtain 500 mg of crude product. The crude compound was purified by reverse phase combi-flash to afford tert-butyl N-[1-[4-[4-(2-tert-butyl-4-pyridyl)-2-thienyl]-3-chloro-benzoyl]-3-methyl-3-piperidyl]carbamate (300 mg) as a white solid.

As the paragraph descriping shows that 169750-96-3 is playing an increasingly important role.

Reference£º
Patent; Medivation Technologies LLC; Pujala, Brahmam; Jangir, Ramniwas; Guguloth, Rambabu; Shinde, Bharat Uttam; Rai, Roopa; Pham, Son Minh; Bernales, Sebastian; Lindquist, Jeffrey; Guha, Mausumee; Kallem, Satyanarayana; Bhatt, Bhawana; Bhagwat, Vikas Ramdas; (162 pag.)US2018/51013; (2018); 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.

To a stirred solution of 1 -methyl-3 -hydroxymethylpiperidine (2 g, 15.5 mmol) in DCM (30 mL) at 0C, triethylamine (4.9 g, 46 mmol) and tosyl chloride (4.41 g, 23.2 mmol) were added and allowed the mixture to stir at room temperature for 6 h. After completion, the reaction mixture was diluted with water (30 mL) and extracted with DCM (3 x 30 mL). The combined organic layer was dried over sodium sulfate and concentrated. The resulting crude was purified by flash chromatography (silica gel, 12 g cartridge) using 0-20% EtOAc in hexanes as eluent to obtain (l-methylpiperidin-3-yl)methyl 4- methylbenzenesulfonate (Yield: 2.50 g, 58%) as white solid. LCMS (ES) m/z = 284.36 [M+H]+; NMR (400 MHz, DMSO-d6) d ppm: 0.87-0.95 (m, 1H), 1.33-1.50 (m, 4H), 1.63 (m, 1H), 1.80-1.85 (m, 2H), 2.06 (s, 3H), 2.42 (s, 3H), 2.46-2.52 (m, 1H), 3.90 (m, 2H), 7.48 (d, J= 8.0 Hz, 2H). 7.78 (d, J= 8.0 Hz, 2H).

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

Reference£º
Patent; JUBILANT BIOSYS LIMITED; VENKATESHAPPA, Chandregowda; D A, Jeyaraj; PENDYALA, Muralidhar; SIVANANDHAN, Dhanalakshmi; RAJAGOPAL, Sridharan; (233 pag.)WO2019/175897; (2019); A1;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.22065-85-6,1-Benzylpiperidine-4-carbaldehyde,as a common compound, the synthetic route is as follows.

Example 11 Production of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methylpiperidine using a mixed solvent of 2-propanol and toluene and sodium methoxide and adopting method A Into a 50-mL four-necked flask were charged 2.0 g (10.4 mmol) of 5,6-dimethoxy-1-indanone, 2.5 g (12.3 mmol, 1.2 equivalents) of 1-benzyl-4-formylpiperidine and 24 mL of a mixed solvent (2-propanol: toluene = 16: 14). After the air in the system was replaced with nitrogen, 2.4 g (12.4 mmol, 1.2 equivalents) of a 28%-sodium methoxide/methanol solution was poured into the reaction solution with refluxing (83C). After completion of the pouring, stirring was continued with refluxing for 1 hour and 2 minutes to complete the reaction. Then, the reaction solution was cooled to 7C (cooling rate: 33C/hour). Crystals began to be precipitated at 42C. The crystals were collected by filtration, washed with water (30 ml) and 6 mL of methanol and then dried at 50C (drying time: 1 hour and 20 minutes) to obtain 2.87 g of the crystals of the title compound (yield: 73.1%). 1H-NMR data of these crystals agreed with those obtained in Example 1.

22065-85-6 1-Benzylpiperidine-4-carbaldehyde 89584, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Eisai R&D Management Co., Ltd.; EP1911745; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4897-50-1, 4-Piperidinopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(1) To 4-(4-carboxypiperidin-1-yl)-1-(3-ethoxybenzyl)-1H-pyrazolo[3,4-d] pyrimidine hydrochloride (50 mg; compound obtained in Reference Example A9-(3)) was added successively chloroform (1 mL), 4-piperidinopiperidine (26 mg), 1-hydroxybenzotriazole (24 mg), triethylamine (17 muL) and 1-ethyl-3-[3-(dimethylamino)-propyl]carbodiimide hydrochloride (35 mg) and the mixture was stirred at room temperature for 17 hours. The reaction mixture was diluted with chloroform (5 mL) and thereto was added an aqueous saturated sodium hydrogencarbonate solution (10 mL). After stirring, the organic layer was separated, dried over sodium sulfate and concentrated in vacuo. The resultant residue was purified by HPLC (Solvent; 10 mM ammonium carbonate/methanol = 80: 20 –> 5: 95) to give 1-(3-ethoxybenzyl)-4-[4-[(4-piperidino-piperidin-1-yl)carbonyl]piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine (44 mg, yield: 69 percent) as an amorphous solid. MS(APCI)m/z; 532 [M+H]+

As the paragraph descriping shows that 4897-50-1 is playing an increasingly important role.

Reference£º
Patent; TANABE SEIYAKU CO., LTD.; EP1772454; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem