Tag: M.W:200-300

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.

A. Mix 10.0 kg of purified water, 2.6 kg of acetonitrile, 1.7 kg (3R, 4R) -1-benzyl-N, 4-dimethylpiperidine-3-amine dihydrochloride and 2.3 kg of potassium carbonate, and stir To dissolve B. Add 1.8 kg of 4-chloro-7-p-toluenesulfonyl-pyrrolo [2,3-d] pyrimidin-4-amine to the product obtained in the previous step several times, and raise the temperature to 75-85 C for 10 hours for reaction. HPLC detection; C. Reduce the temperature to 20-30 C and stir for 2 hours, suction filter, wash the filter cake with 3kg of purified water and set aside;, 1062580-52-2

1062580-52-2 (3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride 45790119, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Jiangsu Haiyuekang Pharmaceutical Technology Co., Ltd.; Pei Xinyu; Chen Zeming; Xie Rongguang; (12 pag.)CN110668995; (2020); 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.301225-58-1,tert-Butyl 4-(propylamino)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A 4-(N-(N-Benzylcarbamoyl)-N-(prop-1-yl)amino)-piperidine trifluoroacetate The title compound was prepared by the reaction of 4-(N-(prop-1-yl)amino)-1-tert-butoxycarbonylpiperidine (from Example 17, Step A) with benzyl isocyanate, followed by treatment of the product with 50% TFA in CH2Cl2 to remove the tert-butoxycarbonyl group, affording the title compound. ESI-MS: 276.1 (M+H)., 301225-58-1

The synthetic route of 301225-58-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Merck & Co., Inc.; US6399619; (2002); 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.61995-20-8,Benzyl 3-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,61995-20-8

A mixture of benzyl 3-oxopiperidine-l-carboxylate (25 g, 0.107 mmol, 1.0 ep), ethyl cyanoacetate (14.54 g, 0.129 mmol, 1.2 eq), NH4OAc (2.09 g, 0.026 mmol, 0.25 eq) and acetic acid (5 mL) in toluene (250 mL) was refluxed at 130 C for 16 h. After the completion of reaction (TLC: Rf. 0.5 (30% ethyl acetate in hexane)), the reaction mixture was cooled to room temperature, quenched with a saturated aqueous solution of NaHC03 (500 mL) and extracted with EtOAc (2 x 300 mL). The combined organic layer was dried over Na2S04, filtered and concentrated under reduced pressure to afford crude product. The crude was purified by column chromatography (200-400 mesh silica-gel, eluent hexanes/EtOAc 90: 10 to 80:10,) to afford benzyl (?T)-3-(l-cyano-2-ethoxy-2- oxoethylidene)piperidine-l-carboxylate (24 g, yield: 68%) as a thick liquid. LCMS: 89%; *H NMR (400 MHz, DMSO-<) delta (ppm): 7.46 - 7.33 (m, 4H), 7.10 (d, / = 12.7 Hz, 1H), 5.19 - 5.15 (d, / = 13.4 Hz, 3H), 4.19 (dq, / = 14.2, 7.1 Hz, 2H), 3.59 - 3.50 (m, 2H), 2.10 (dt, / = 16.7, 6.3 Hz, 1H), 2.03 - 1.90 (m, 1H), 1.82 (d, / = 8.5 Hz, 2H), 1.22 (dq, / = 10.8, 6.1, 4.3 Hz, 4H). MS (ESI) m/z 329 [C18H20N2O4 + H] + As the paragraph descriping shows that 61995-20-8 is playing an increasingly important role. Reference：
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH; NACRO, Kassoum; (223 pag.)WO2018/21977; (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.24686-78-0,1-Benzoylpiperidin-4-one,as a common compound, the synthetic route is as follows.

Method 1 Preparation of 3,4-Dihydro-spiro[(2H)-1-benzopyran-2,4′-piperidine]-4-one hydrochloride A solution of 2-acetylphenol (5 g, 0.037 mmol), 1-benzoyl-4-piperidone (7.5 g, 0.037 mmol), pyrrolidine (2.6 g, 0.037 mol) and CH3 OH (50 ml) was heated at reflux for 8 hours. After cooling to room temperature overnight, the solid was filtered to yield 8.2 g of 1′-benzoyl-3,4-dihydro-spiro[(2H)-1-benzopyran-2,4′-piperidin]-4-one. The mother liquor was concentrated to dryness and the residue triturated with ether to yield an additional 1.7 g (83percent total yield).

24686-78-0, The synthetic route of 24686-78-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Merck & Co., Inc.; US5206240; (1993); 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.19099-93-5,1-Cbz-Piperidin-4-one,as a common compound, the synthetic route is as follows.

To a -20 0C solution of N,N,N’,N’-tetraniethylethylenediamine (0.335 g, 2.89 mmol) in THF (1 mL) was added n-butyllithium (2.5M, 1.15 mL, 2.89 mmol) over 10 min. After 30 min, the mixture was cooled to -78 0C and tert-butyl (6-chloropyridin-2-yl)carbamate (0.300 g, 1.31 mmol) in THF (0.8 mL) was added over 15 min. After Ih, the reaction was warmed to -50 0C, stirred for 2h and then N-benxyloxycarbonyl-4-piperidinone (0.459 g, 1.97 mmol) in THF (1 mL) was added over 10 min. The reaction was allowed to warm to room temperature and then stirred for 24 h. A solution of saturated aqueous NaHCO3 was added and the mixture extracted with EtOAc (3x). The combined organic layers were washed with H2O, brine, dried over MgStheta4, filtered, and concentrated under reduced pressure. The crude product was purified by silica gel chromatography, eluting with a gradient of 25 to 50% ethyl acetate: hexane to give the title compound (0.160 g). MS: mlz = 338.0 (M + 1).

19099-93-5, 19099-93-5 1-Cbz-Piperidin-4-one 643496, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK & CO., INC.; WO2006/99268; (2006); 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.24666-55-5,Benzyl (2,6-dioxopiperidin-3-yl)carbamate,as a common compound, the synthetic route is as follows.

3-N-benzyloxycarbonylamino-2,6-piperidinone hydrochloride 40 g (0.153 mol) was added to a 1 L reaction flask.40% hydrobromic acid solution 300ml, acetic acid 400ml,Stir well and mix well, heat to 60 C, keep warm for 1 h,Cool to room temperature, distill off the solvent and water under reduced pressure.Add 1 L of ethyl acetate to the residue and stir for 0.5 h.The product was white filtered to give a white solid (30.4 g, yield: 95.2%)., 24666-55-5

The synthetic route of 24666-55-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shijiazhuang Duen Pharmaceutical Technology Co., Ltd.; Fang Yu; Du Yumin; (8 pag.)CN109776493; (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.141774-61-0,tert-Butyl (piperidin-2-ylmethyl)carbamate,as a common compound, the synthetic route is as follows.

To a solution of Compound L (14.71 g, 46.7 mmol) in THF(250 mE) at -60 C. was added 0.5 M KHMDS solution inTHF (103 mE) dropwise. After stirring at -60 C. for 30 mithe reaction mixture was added to a solution of 4-nitrophenylchloroformate at -60 C. (9.41 g, 46.7 mmol) in THF (200This reaction mixture was then stirred for 30 mm at -60C., followed by addition of piperidine-2-yl-methylcarbamicacid tert-butyl ester, also referred to herein as (R,S)-piperi-dine-2-yl-methylcarbamic acid tert-butyl ester, (5.0 g, 23.3mmol) in portions. The reaction was allowed to warm toambient temperature and then stirred for 18 h. The reactionwas then concentrated under vacuum, and the residue dilutedwith EtOAc (500 mE). The mixture was then washed withwater (2×250 mE) and brine (250 mE). The organic layer wasseparated, dried over Na2504, and filtered. Removal of sol-vents under vacuum afforded crude Compound N. CrudeCompound N was purified by flash chromatography using100% EtOAc. Removal of solvent under vacuum affordedCompound N in 50% yield (6.5 g, 11.7 mmol) as a whitesolid. EC-MS [M+H] 556.1 (C30H41N307+H, calc: 555.3)., 141774-61-0

The synthetic route of 141774-61-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Signature Therapeutics, Inc.; Jenkins, Thomas E.; Husfeld, Craig O.; US9139612; (2015); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1067915-34-7,Ethyl 1-benzyl-5,5-difluoro-4-oxopiperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

1067915-34-7, 10245] A mixture of compound 6 (6.5 g, 21.9 mmol) in hydrochloric acid (6 N, 180 mE) was stirred at 1100 C. for 16 hours. The mixture was adjusted pH to 8 with 1 N aqueous NaOH solution. The mixture was extracted with EtOAc (180 mE), the organic layer was dried over Na2SO4 and concentrated in vacuo to give the crude product compound 7 as whitesolid. ECMS: 244 [M+1].

As the paragraph descriping shows that 1067915-34-7 is playing an increasingly important role.

Reference：
Patent; Novira Therapeutics, Inc.; Hartman, George D.; US2015/274652; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

189333-49-1, 3-Benzyl-3,9-diazaspiro[5.5]undecane is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of compound 2The mixture of the compound 1 (2.44 g) (US6291469, page 62, column 123), BoC2O (2 g) in MeOH (30 mL) was stirred overnight. After evaporation, the residue was purified by column to give the compound 2 (3 g, 87%).

189333-49-1, As the paragraph descriping shows that 189333-49-1 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2007/30061; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

236406-22-7, 1-Boc-4-(Aminomethyl)-4-methylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 0 oC solution of tert-butyl 4-(aminomethyl)-4-methylpiperidine-1- carboxylate (7.0 g, 30.66 mmol), NaHCO3 (3.86 g, 45.99 mmol) in ethanol (131 mL) and water (92 mL) was added benzyl chloroformate (4.4 mL, 30.66 mmol). The reaction mixture was stirred at room temperature for 2 hours and most of ethanol was removed under reduced pressure. The resulting mixture was extracted with Et2O (3 x 100 mL). Combined organic layers were washed with brine, dried over anhydrous MgSO4, filtrated and the volatiles were removed under reduced pressure. The resulting residue was purified on a silica gel pad (20 to 30% gradient of EtOAc/hexanes) to give tert-butyl 4-((benzyloxycarbonylamino)methyl)-4- methylpiperidine-1-carboxylate (9.78 g, 88% yield) as a yellowish oil.1H NMR (500 MHz, CDCl3) delta ppm 7.41- 7.29 (m, 5H), 5.17- 5.05 (m, 2H), 4.79 (br. s, 1H), 3.70- 3.58 (m, 2H), 3.22- 2.99 (m, 4H), 1.45 (s, 9H), 1.42- 1.35 (m, 2H), 1.31- 1.23 (m, 2H), 0.94 (s, 3H). MS (ES+) m/z 363 (M+1)., 236406-22-7

The synthetic route of 236406-22-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; RELAY THERAPEUTICS, INC.; D.E. SHAW RESEARCH, LLC; ALBRECHT, Brian K.; GIORDANETTO, Fabrizio; GREISMAN, Jack, Benjamin; MARAGAKIS, Paul; TAYLOR, Alexander M.; WALTERS, W. Patrick; (117 pag.)WO2018/57884; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem