Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.141943-04-6,1-Benzylpiperidine-3-carboxylic acid,as a common compound, the synthetic route is as follows.

(c) Synthesis of N-[4-(aminocarbonyl)phenyl]-1-benzylpiperidine-3-carboxamide To a solution of 1-benzyl-3-piperidinecarboxylic acid (1.37 g, 6.23 mmol) in N,N-dimethylformamide (28 ml) were added p-aminobenzamide (0.92 g, 6.54 mmol), triethylamine (1.3 ml, 9.33 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (1.79 g, 9.34 mmol) and 1-hydroxybenzotriazole monohydrate (0.93 mg, 6.88 mmol) at room temperature, and stirred overnight. Then, the reaction mixture was poured into a saturated aqueous sodium hydrogencarbonate solution and extracted with chloroform. The organic layer was washed with a saturated aqueous sodium chloride solution and then dried over magnesium sulfate. The solvent was distilled off under reduced pressure and the resulting residue was purified by a silica gel column chromatography (eluent: chloroform/methanol = 95/5) to obtain N-[4-(aminocarbonyl)phenyl]-1-benzylpiperidine-3-carboxamide (551 mg, 26%). Melting point: 211-212C., 141943-04-6

141943-04-6 1-Benzylpiperidine-3-carboxylic acid 16244010, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Sumitomo Pharmaceuticals Company, Limited; EP1500643; (2005); 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.885279-92-5,1-Boc-1,8-diaza-spiro[4.5]decane,as a common compound, the synthetic route is as follows.

A 40-mL vial was charged with N-(1H-pyrazol-3-yl)acetamide (125 mg, 1.00 mmol, 1.00 equiv), DCM (10 mL), and N,N-diisopropylethylamine (258 mg, 2.00 mmol, 2.00 equiv).4-Nitrophenyl chloroformate (222 mg, 1.10 mmol, 1.10 equiv) in DCM (2 mL) was addeddropwise at 0 C. The resulting solution was stirred for 2 h at room temperature. Then tertbutyl 1,8-diazaspiro[4.5]decane-1-carboxylate (240 mg, 1.00 mmol, 1.00 equiv) was added. The resulting solution was stirred overnight at room temperature and quenched by water (10 mL). The mixture was extracted with DCM (3 x 10 mL) and the organic layers were combined, washed with water (3 x 10 mL), dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue was chromatographed on a silica gel column to provide 295 mg (75% yield) of tert-butyl 8-(3 -acetamido- 1H-pyrazole- 1 -carbonyl)- 1,8- diazaspiro[4.5]decane-1-carboxylate as a light yellow oil. LCMS (ESI, m/z): 392 [M+H]., 885279-92-5

As the paragraph descriping shows that 885279-92-5 is playing an increasingly important role.

Reference：
Patent; ABIDE THERAPEUTICS, INC.; WEBER, Olivia D.; SHAGHAFI, Michael B.; GRICE, Cheryl A.; JONES, Todd K.; (274 pag.)WO2017/87854; (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.10315-06-7,Methyl 1-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

5L reaction flask to dry slowly purged with nitrogen, will 233.3g1-benzyl-4-piperidine carboxylic acid methyl ester (1mol) and 240ml of toluene into a reactor, with stirring, cooled until the internal temperature at about -5 . The resulting red aluminum – morpholine complex (approximately 2.6mol) was dropped to control the reaction temperature between -5 ~ 0 . 3h addition was complete, the reaction was continued insulation 2h. Was added slowly prepared 4N sodium hydroxide solution (containing 360gNaOH), control the internal temperature not higher than 20 , the addition was completed, stirring was stopped, the organic layer was washed with water (1500ml / times, 4 times), the organic layer was concentrated at 75 concentrated under reduced pressure until no solvent was evaporated to give 1-benzyl-4-piperidinemethanol 201.6g, as a pale yellow oily liquid. Yield: 98.2%. HPLC: 99.30%

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

Reference：
Patent; Shanghai Goldentree Resin Powder Co., Ltd.; Zhu, Ben; (8 pag.)CN105693596; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1067915-34-7, Ethyl 1-benzyl-5,5-difluoro-4-oxopiperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Ethyl 1- benzyl-5,5-difluoro-4-oxopiperidine-3-carboxylate (6.00 g, 20.2 mmol; prepared as described in WO 2005/040120, p. 30) was dissolved in 3N HCl (60 mL) and heated to reflux for 16 hours. The reaction was cooled, adjusted to pH 8 with solid NaHCO3, then extracted three times with ethyl acetate. The combined organics were washed with saturated NaCl, dried over Na2SO4 and concentrated in vacuo to a white solid (5.1 g). MS APCI (+) m/z 244.0 (M+l) detected., 1067915-34-7

1067915-34-7 Ethyl 1-benzyl-5,5-difluoro-4-oxopiperidine-3-carboxylate 49761228, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ARRAY BIOPHARMA INC.; ALLEN, Shelley; CELESTE, Laura L.; DAVIS, T. Gregg; DELISLE, Robert Kirk; GRESCHUK, Julie Marie; GROSS, Stefan, D.; HICKEN, Erik, James; JACKSON, Leila, J.; LYSSIKATOS, Joseph, P.; KALLAN, Nicholas C.; MARMSATER, Fredrik, P.; MUNSON, Mark, C.; PHENEGER, Jed; RAST, Bryson; ROBINSON, John, E.; SCHLACHTER, Stephen T.; TOPALOV, George T.; WRIGHT, A. Dale; ZHAO, Qian; WO2010/22076; (2010); A1;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1062580-52-2,(3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride,as a common compound, the synthetic route is as follows.

To the reaction flask was added 200g (3R,4R)-N-(phenylmethyl)-3-methylamino-4-methylpiperidine hydrochloride, 210g 2,4-dichloro-7H-pyrrolo[2,3-D]pyrimidine (compound II), 160g of potassium carbonate, 1000mL of water and a 500 mL of ethanol, stirring while reflux, TLC monitored the reaction. After completion of the reaction, cooled to below 30 deg. C, 2000mL of ethyl acetate was added, with stirring, suction filtered, the filter cake was washed with 200 mL of ethyl acetate, the aqueous layer was extracted with ethyl acetate 1000mL and then the combined organic phase was dried over anhydrous sodium sulfate, suction filtered, evaporated to dryness to obtain 295g crude oil, the crude was added 300mL ethyl acetate and 900mL hexane, dissolved clear, cooled to -10 deg. C overnight incubation, solid precipitation, filtration, drying, 280g white solid product compound IV.

1062580-52-2, As the paragraph descriping shows that 1062580-52-2 is playing an increasingly important role.

Reference：
Patent; Nantong Changyou Pharmaceutical Science and Technology Co., Ltd.; Li, Zebiao; Liu, Jie; Pan, Jing; Zhang, Lei; Yan, Jun; Lu, Lianling; (10 pag.)CN105732641; (2016); A;,
Piperidine – Wikipedia
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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

(A) (S)-terf-butyl 3-((7-chloropyrido[4,3-ib]pyrazi n-5-ylami no)methyl)piperidi ne- 1 -carboxylate.[0123] A solution of (S)-teri-butyl 3-(aminomethyl)piperidine-1 -carboxylate (100 mg, 0.5 mmol), 5,7-dichloropyrido[4,3-?>]pyrazine (100 mg, 0.5 mmol) and DIPEA (77 mg, 0.6 mmol) in THF (5 ml_) was stirred at room temperature for 4 hours. The volatiles were removed under reduced pressure, and the residue was treated with ethyl acetate, with brine, and concentrated to give the crude title compound.

140645-24-5, As the paragraph descriping shows that 140645-24-5 is playing an increasingly important role.

Reference：
Patent; HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; DENG, Wei; JI, Jianguo; WO2012/167423; (2012); 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.1180112-41-7,tert-Butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate,as a common compound, the synthetic route is as follows.,1180112-41-7

tert-Butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate (1.5 g, crude) and 2,6-dichloro-4- ethylpyridine-3,5-dicarbonitrile (synthesis described in example 3 step 2, 1 g, 4.5 mmol) were dissolved in tetrahydrofuran (20 mL) and triethylamine (1.14 g, 11.25 mmol) was added at 0 C. The resultant mixture was stirred at ambient temperature for 2 hours and then diluted with ethyl acetate (60 mL). The mixture was washed with water (40 mL) and brine (40 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure to afford the title compound (2.1 g, crude) as a yellow oil which was used in the next step without further purification. LCMS m/z = 437.8 [M+Na]+.

1180112-41-7 tert-Butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate 56962134, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ADAMS, Nicholas David; BENOWITZ, Andrew B.; RUEDA BENEDE, Maria Lourdes; EVANS, Karen Anderson; FOSBENNER, David T.; KING, Bryan Wayne; LI, Mei; MILLER, William Henry; REIF, Alexander Joseph; ROMERIL, Stuart Paul; SCHMIDT, Stanley J.; WIGGALL, Kenneth; (1283 pag.)WO2017/216726; (2017); A1;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.914988-10-6,tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,914988-10-6

To a solution of (±)-tert-butyl 3-cyano-4-oxo-piperidine-1-carboxylate (200 mg, 892 mumol, CAS 914988-10-6) in acetone (50 mL) was added potassium carbonate (370 mg, 2.68 mmol) and methyl iodide (380 mg, 2.68 mmol) in one portion. The reaction was stirred at 30 C for 12 hrs. On completion, 20 mL water was added to the solution. Then the solution was extracted with ethyl acetate (3 x 30 mL), washed with water (100 mL), dried over anhydrous sodium sulfate, and concentrated in vacuo to give the title compound. 1H NMR (400MHz, CDCl3) delta = 4.25 (s, 2H), 2.85 – 2.80 (m, 2H), 2.50 – 2.45 (m, 2H), 1.40 (s, 3H), 1.39 (s, 9H).

914988-10-6 tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate 42609283, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; RAZE THERAPEUTICS, INC.; MAINOLFI, Nello; MOYER, Mikel P.; (208 pag.)WO2017/156177; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

23499-01-6, 1-(4-Nitrophenyl)piperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 6 1-(4-Nitrophenyl)-4-piperidone was reacted in a similar manner to Example 2 with N-benzyl-N-methylamine and then with fumaric acid. 4-(N-benzyl-N-methylamino)-1-(4-nitrophenyl)piperidine fumarate was obtained. Melting point 183 C.

23499-01-6, As the paragraph descriping shows that 23499-01-6 is playing an increasingly important role.

Reference：
Patent; BASF Aktiengesellschaft; US5260318; (1993); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

10315-06-7, Methyl 1-benzylpiperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of the corresponding b-carboline-3-acid methyl ester(1 mmol), NaOH (4 mmol), C2H5OH (5 ml) and H2O (10 ml) was refluxed for 3 h, and the ethanol was removed on the rotary evaporator.The mixture was neutralized (pH = 5) with 5 N HCl and cooled. The precipitate was collected, washed well with H2O and dried in vacuum. The material was used without further purificationfor the following steps.

10315-06-7, 10315-06-7 Methyl 1-benzylpiperidine-4-carboxylate 11436222, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Wang, Jin; Wang, Zhi-Min; Li, Xue-Mei; Li, Fan; Wu, Jia-Jia; Kong, Ling-Yi; Wang, Xiao-Bing; Bioorganic and Medicinal Chemistry; vol. 24; 18; (2016); p. 4324 – 4338;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem