Month: August 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.189442-78-2,1-Boc-N-methoxy-N-methylpiperidine-3-carboxamide,as a common compound, the synthetic route is as follows.

Step 2: To a solution of compound B (4.7 g, 17.2 mMol) in 70 ml of THF at 0 C. (under N2) was added a 3.0 M (11.5 ml, 34.5 mMol) solution of Methyl Magnesium Bromide in THF. After the addition was complete, the cooling bath was removed and the resulting mixture was allowed to rise to room temperature where it was allowed to stir overnight. The resulting mixture was quenched with a saturated aqueous KHSO4 solution and diluted with EtOAc. The organic phase was washed with brine, dried over MgSO4, filtered and evaporated to dryness. The crude residue was passed through a plug of silica gel and eluted with 5-20% EtOAc/Hexane. Yield: 2.37 g, approximately 60%. H NMR (500 MHz, CDCl3) 4.10 (d, J=12.0 Hz, H), 3.92 (s, H), 2.94 (dd, J=10.3, 13.3 Hz, H), 2.82-2.77 (m, H), 2.52-2.48 (m, H), 2.18 (s, 3H), 1.98 (dd, J=3.6, 12.9 Hz, H), 1.73-1.69 (m, H), 1.56-1.44 (m, 11H).

189442-78-2 1-Boc-N-methoxy-N-methylpiperidine-3-carboxamide 22248320, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Ledeboer, Mark; Pierce, Albert; Bemis, Guy; Farmer, Luc; Wang, Tiansheng; Messersmith, David; Duffy, John; Salituro, Francesco; Wang, Jian; US2006/183761; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

287952-67-4, 4-(4-Trifluoromethoxyphenoxy)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add 20 mL of dichloromethane to 2-chloro-3-nitro-5-trifluoromethylbenzoic acid (12 mmol), stir at room temperatureOxalyl chloride (30.5 mmol) and 0.05 mL of DMF were slowly added dropwise and reacted for two hours.After the reaction was completed, the reaction solution was spoked, dissolved in 15 mL of dichloromethane, and slowly added dropwise with ammonium thiocyanate (36 mmol).Add PEG-400 (0.2g), stir at room temperature for 1.5 hours; filter,The filtrate was added dropwise to a solution of 4-(2-fluoro-4-methylphenoxy)piperidine in dichloromethane, and stirred at room temperature for 40 min.After the reaction is completed, the reaction solution is spun dry, column chromatography,Obtained yellow solid 1i, yield 54%.

The synthetic route of 287952-67-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sichuan University; Yu Luoting; Wei Yuquan; Gao Chao; (52 pag.)CN108456204; (2018); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

34622-39-4, (S)-2-Piperidinone-6-carboxylic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S)-6-oxopiperidine-2-carboxylic acid (1.00 g, 6.99 mmol), 2,4-dichlorobenzylamine (1.48 g, 8.38 mmol) and 3-{[(ethylimino)methylene]amino}-N,N-dimethylpropan-1-aminiumchloride (EDCI) (1.61 g, 8.38 mmol), in CH2Cl2 was stirred at r.t. for 24 h. Solvents were evaporated and the mixture was solved in EtOH (40 mL), then Et2O was added (60 mL). The desired product crystalized over night. It was filtered to give a white solid in 62percent yield (1.30 g, 4.32 mmol). mp (EtOH/Et2O) 142-144 ¡ãC; TLC Rf (CH2Cl2/MeOH: 96/4) 0.3; 1H NMR (DMSO[d6], 400 MHz): delta ppm 1.56-1.81(m, 3H, CH2CH2CH2CH), 1.86-1.96 (m, 1H, CH2CH2CH2CH), 2.15 (t, J=6.8 Hz, 2H, CH2CH2CH2CH), 3.95 (dd, J= 5.9, 3.0 Hz, 1H,CH2CH2CH2CH), 4.28 (dd, J = 15.8, 5.6 Hz, 1H, NHCH2), 4.37 (dd, J = 15.8, 5.6 Hz, 1H, NHCH2), 7.38 (d, J = 8.3 Hz, 1H, ArH), 7.42 (dd, J = 8.3, 2.1 Hz, 1H, ArH), 7.57 (br d, J = 2.5 Hz, 1H, NHCH), 7.60 (d,J= 2.1 Hz, 1H, ArH), 8.52 (br t, J = 5.8 Hz, 1H, NHCH2); 13C NMR(DMSO[d6],100 MHz): delta ppm 18.9 (CH2), 26.4 (CH2), 31.7 (CH2), 40.2 (CH2), 55.4 (CH), 127.7 (CH), 128.9 (CH), 130.6 (CH), 132.6 (C), 133.3 (C), 135.9 (C), 170.9 (CH), 172.7 (C). Anal. Calcd for C13H14Cl2N2O2: C, 51.85; H, 4.69; N, 9.30. Found: C, 51.82; H, 4.70; N, 9.29percent.

As the paragraph descriping shows that 34622-39-4 is playing an increasingly important role.

Reference£º
Article; Homerin, Germain; Lipka, Emmanuelle; Rigo, Benoit; Millet, Regis; Dezitter, Xavier; Furman, Christophe; Ghinet, Alina; Tetrahedron; vol. 73; 35; (2017); p. 5327 – 5336;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

149353-75-3, 4-(1-(tert-Butoxycarbonyl)piperidin-4-yl)benzoic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 229 59.1 tert-butyl 4-[4-(cyclopropylmethylcarbamoyl)-phenyl]-piperidine-1-carboxylate 500 mg tert-butyl 4-(4-carboxyphenyl)-piperidine-1-carboxylate are placed in 28 ml dimethylformamide, then 1.14 ml diisopropylethylamine and 747 mg HATU are added. The reaction mixture is stirred for 15 min at ambient temperature, then 194 mg cyclopropylmethylamin hydrochloride are added. The reaction mixture is stirred overnight at ambient temperature. Then the product is purified by preparative HPLC (method A). 480 mg product are obtained as an oil. Analytical HPLC-MS (method B): RT=1.64 min.

As the paragraph descriping shows that 149353-75-3 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2011/21501; (2011); 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.79099-07-3,1-Boc-4-Piperidone,as a common compound, the synthetic route is as follows.

In a 100 mL single-necked flask,will4-oxopiperidine-1-Formic acid tert-butyl ester(1.81 g, 9.08 mmol)Was dissolved in CH2Cl2 (42 mL)The ice bath was cooled with stirring,DAST (4.0 mL, 29.4 mmol) was slowly added dropwise to the reaction system,The reaction was stirred at this temperature for 4 h.The reaction was quenched by adding saturated aqueous NaHCO3 (30 mL) to the reaction system,Then extracted with CH2Cl2 (50 mL x 3)The organic phases were combined and washed with saturated NaCl solution (20 mL)Anhydrous Na2SO4 dry,filter,Concentrated under reduced pressure,The crude product was isolated by silica gel column chromatography (eluent: PE / EtOAc (v / v) = 5/1)To give the object as a colorless liquid (1.21 g, 60%).

79099-07-3 1-Boc-4-Piperidone 735900, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Guangdong HEC Pharmaceutical Co., Ltd.; Zhong, Xue; Liu, Bing; Xue, Yaping; Li, Xuke; Wang, Feng; He, Wei; Chen, Xiaoyan; Zhang, Yingjun; Zheng, Changchun; (56 pag.)CN106187838; (2016); 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.141699-59-4,tert-Butyl 4-((methylsulfonyl)oxy)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

NaH (1.2 eq., 0.68 mmol) was added portionwise to a stirred solution of 4-iodopyrazole (0.57 mmol) in DMF (2 L) at 4C. The resulting mixture was stirred for 1 hour at 4C and compound 23-4 (1.1 eq., 0.63 mmol) was then added. The resulting mixture was heated to 100C for 12 h. The reaction was quenched with H2O and extracted with EtOAc several times. The combined organic layers were dried, filtered, and concentrated to afford an orange oil. The residue was purified by silica gel chromatography (eluting with 5% EtOAc in pentane) to give compound 23-1 a as a white solid (140 g, 66%).

As the paragraph descriping shows that 141699-59-4 is playing an increasingly important role.

Reference£º
Patent; PFIZER INC.; WO2006/21881; (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.1155-56-2,1-Benzyl-N-phenylpiperidin-4-amine,as a common compound, the synthetic route is as follows.

Step 2 A chloroform solution (1 ml) of propionyl chloride (0.16 ml, 1.8 mmol) was added dropwise to a chloroform solution (4 ml) of (1-benzyl-4-piperidinyl)-phenyl-amine (0.4 g, 1.5 mmol) and triethylamine (0.4 ml, 2.9 mmol), and the mixture was stirred at room temperature for 40 minutes. The solvent was distilled off, and 10% hydrochloric acid (20 ml) and diethyl ether (20 ml) were added to the residue. A 8 N NaOH aqueous solution was added to make the aqueous layer basic, the mixture was extracted with dichloromethane (2*20 ml), the organic layer was washed with water (20 ml) and an aqueous saturated sodium chloride solution (20 ml), and dried over anhydrous sodium sulfate, and the solvent was distilled off. The residue was purified by silica gel column chromatography (solvent: hexane-ethyl acetate) to obtain oily N-(1-benzyl-4-piperidinyl)-N-phenylpropionamide (283 mg).

As the paragraph descriping shows that 1155-56-2 is playing an increasingly important role.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP1559428; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

37675-20-0, (R)-(Piperidin-3-yl)methanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: [(R)-1-(4-Bromo-8,9-dihydro-7H-6-oxa-2,9a-diazabenzo[cd]azulen-1-yl)piperidin-3-yl]methanol A mixture of 4-bromo-1-methanesulfonyl-8,9-dihydro-7H-6-oxa-2,9a-diazabenzo[cd]azulene (0.305 g, 0.92 mmol), (R)-1-piperidin-3-ylmethanol (0.212 g, 1.84 mmol) and N,N-diisopropylethylamine (0.319 mL, 1.84 mmol) in propan-2-ol (2.0 mL) was heated in a sealed vial at 150 C. under microwave irradiation for 17 hours. The reaction mixture was partitioned between ethyl acetate and aqueous sodium bicarbonate solution. The aqueous phase was further extracted with ethyl acetate and the combined organic extracts were washed with brine, dried over sodium sulfate, filtered and evaporated in vacuo. The residue was purified via flash chromatography on silica gel (solvent gradient: 25-100% ethyl acetate in toluene, then 50-100% methyl acetate in ethyl acetate) to yield 71 mg (21%) of the title compound as a white solid. LCMS (ESI): [M+H]+=366/368.

37675-20-0 (R)-(Piperidin-3-yl)methanol 853001, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Genentech, Inc.; Braun, Marie-Gabrielle; Garland, Keira; Hanan, Emily; Purkey, Hans; Staben, Steven T.; Heald, Robert Andrew; Knight, Jamie; Macleod, Calum; Lu, Aijun; Wu, Guosheng; Yeap, Siew Kuen; (183 pag.)US2018/65983; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

561314-57-6, 2,8-Diazaspiro[4.5]decan-3-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,8-Diazaspiro[4.5]decan-3-one (0.12 g, 0.75 mmol) and prop-2-yn-1-yl 3-oxo-9- azabicyclo[3.3.1]nonane-9-carboxylate (0.17 g, 0.75 mmol) were dissolved in DOE (7.5 mL) at rt and titanium isopropoxide (0.66 mL, 2.25 mmol) was added. The reactionmixture was heated to reflux under N2 for 16 h then cooled to rt. STAB (0.80 g, 3.75 mmol) was added, the reaction mixture again heated to reflux for 16 h then cooled to rt. The reaction mixture was quenched with the addition of sat. NaHCO3 sol. (10 mL), diluted with DCM (10 mL) then filtered through a pad of celite. The layers were separated and the aqueous layer was extracted with DCM (4 x 20 mL). The organiclayers were combined and washed with brine, then dried (Mg504). The solvents were removed in vacuo, and the residue was purified by column chromatography (normal phase, [Biotage SNAP cartridge KP-sil 25 g, 40-63 tim, 60 A, 27 mL per mm, gradient 1% to 10% MeOH in DCM]) to give an inseparable mixture of diastereomers This mixture was purified by preparative reversed phase HPLC (Phenomenex Gemini-NX 5im 018 11OA Axia column, 100 x 30 mm, eluting with 15 to 35% MeCN/Solvent B over 14.4 mm at 30 mL/min [where solvent B is 0.2% of (28% NH3/H20) in H20] and collecting fractions by monitoring at 205 nm) to give prop-2-yn-1-yl 3-(3-oxo-2,8- diazaspi ro[4. 5]dec-8-yl)-9-azabicyclo[3. 3.1 ]nonane-9-carboxylate Example 5-2 Isomer 1 (0.02 g, 7%) as a colourless solid and prop-2-yn-1-yl 3-(3-oxo-2,8-diazaspi ro[4. 5]dec-8-yl)-9-azabicyclo[3.3. 1 ]nonane-9-carboxylate Example 5-2 Isomer2(0.03 g, 11%) as a colourless solid.

561314-57-6 2,8-Diazaspiro[4.5]decan-3-one 10559599, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; HEPTARES THERAPEUTICS LIMITED; CONGREVE, Miles Stuart; BROWN, Giles Albert; TEHAN, Benjamin Gerald; PICKWORTH, Mark; CANSFIELD, Julie Elaine; (105 pag.)WO2015/140559; (2015); 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.189442-78-2,1-Boc-N-methoxy-N-methylpiperidine-3-carboxamide,as a common compound, the synthetic route is as follows.

Step 2: To a solution of compound B (4.7 g, 17.2 mMol) in 70 ml of THF at 0 C. (under N2) was added a 3.0 M (11.5 ml, 34.5 mMol) solution of Methyl Magnesium Bromide in THF. After the addition was complete, the cooling bath was removed and the resulting mixture was allowed to rise to room temperature where it was allowed to stir overnight. The resulting mixture was quenched with a saturated aqueous KHSO4 solution and diluted with EtOAc. The organic phase was washed with brine, dried over MgSO4, filtered and evaporated to dryness. The crude residue was passed through a plug of silica gel and eluted with 5-20% EtOAc/Hexane. Yield: 2.37 g, approximately 60%. H NMR (500 MHz, CDCl3) 4.10 (d, J=12.0 Hz, H), 3.92 (s, H), 2.94 (dd, J=10.3, 13.3 Hz, H), 2.82-2.77 (m, H), 2.52-2.48 (m, H), 2.18 (s, 3H), 1.98 (dd, J=3.6, 12.9 Hz, H), 1.73-1.69 (m, H), 1.56-1.44 (m, 11H).

189442-78-2 1-Boc-N-methoxy-N-methylpiperidine-3-carboxamide 22248320, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Ledeboer, Mark; Pierce, Albert; Bemis, Guy; Farmer, Luc; Wang, Tiansheng; Messersmith, David; Duffy, John; Salituro, Francesco; Wang, Jian; US2006/183761; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem