Some tips on 1158759-03-5

The synthetic route of 1158759-03-5 has been constantly updated, and we look forward to future research findings.

1158759-03-5, tert-Butyl ((4-methylpiperidin-4-yl)methyl)carbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 4d (0.35 g, 1.13 mmol), tert-butyl ((4-methylpiperidin-4-yl)methyl)carbamate (0.39 g, 1.70 mmol) DIEA (0.36 g, 2.83 mmol) was added to DMSO (10 mL) and stirred at 100 C for 2 h. The reaction solution was added water (10 mL), EA extraction (10 mL ¡Á 2), the combined organic phases were washed with brine (50 mL), dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure, the residue was purified by column chromatography to give compound 4e (0.15 g, 27%), 1158759-03-5

The synthetic route of 1158759-03-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JACOBIO PHARMACEUTICALS CO., LTD; MA, CUNBO; GAO, PANLIANG; CHU, JIE; WU, XINPING; WEN, CHUNWEI; KANG, DI; BAI, JINLONG; PEI, XIAOYAN; (171 pag.)TW2019/25186; (2019); A;,
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Downstream synthetic route of 849928-30-9

849928-30-9 1-Boc-2-Phenyl-4-piperidinone 44558601, apiperidines compound, is more and more widely used in various fields.

849928-30-9, 1-Boc-2-Phenyl-4-piperidinone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A suspension of potassium tert-butoxide ( 1.25 g, 11.1 mmol) and methyltriphenylphosphonium bromide (3.86 g, 1.1 mmol) in tetrahydrofuran (100 mL) was stirred at 40 C for 30 minutes. The mixture was then cooled to room temperature and a solution of tert-butyl 4-oxo-2-phenylpiperidine-l-carboxylate (2.35 g, 8.5 mmol) in tetrahydrofuran (30 mL) was added slowly. The reaction mixture was stirred at 40 C for 24 hours. The mixture was cooled to room temperature and quenched by the addition of water and diluted with ethyl acetate (250 mL), The organic layer was separated then washed with water, 10% aqueous citric acid and brine, dried over anhydrous sodium sulfate, filtered and concentrated. Column chromatography on silica gel (hexane:ethyl acetate 95:5 to 9:1) provided tert-butyl 4-methylene-2-phenylpiperidine-l-carboxylate (2.24 g, 96%). NMR (400 MHz, CDCI3): 7.31 (m, 4H), 7.21 (m, 1H), 5.48 (br d, 1H), 4.84 (dd, 2H), 4.07 (br dd, 1H), 2.85 (br, t, 1H), 2.78 (dtr, 1H), 2.64 (dd, 1H), 2.28 (dtr, lH), 2.20 (br d, 1H), 1.42 (s, 9H). GC/MS (EI) for C7H23NO2: 273 (M+)., 849928-30-9

849928-30-9 1-Boc-2-Phenyl-4-piperidinone 44558601, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; EXELIXIS, INC.; RICE, Kenneth; WO2012/71509; (2012); A2;,
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Some tips on 239482-98-5

239482-98-5, As the paragraph descriping shows that 239482-98-5 is playing an increasingly important role.

239482-98-5, 2-(Aminoethyl)-1-N-Boc-piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2 EPO 2-r2-(5-Chloro-4-ethoxycarbonylmethyl-3,6-difluoro-pyridin-2-ylamino)-ethyl1- piperidine-1-carboxylic acid tert-butyl ester(3-Chloro-2,5,6-trifluoro-pyridin-4-yl)-acetic acid ethyl ester (667 mg, 2.63 mmol) and 2-(2-amino-ethy.)-piperidine-1-carboxylic acid tert-butyl ester (500 mg, 2.19 mmol) are dissolved in 10 ml DMSO in a microwave vial. Sodium carbonate (4648 mg, 4.38 mmol) is added and the vial is closed. The reaction mixture is heated in the microvLambda/ave for 8 min at 120 C. A second batch is reacted in the same way.The solvent of the combined batches is evaporated by reduced pressure. The crude product is purified by column chromatography (silica gel, eluent = 5% to 50% EtOAc in cyclohexane).LC/MS (II) (5-95%, 5 min): 3.86, 484 (M+H+Na).

239482-98-5, As the paragraph descriping shows that 239482-98-5 is playing an increasingly important role.

Reference£º
Patent; SANTHERA PHARMACEUTICALS (SCHWEIZ) GMBH; WO2006/45459; (2006); A1;,
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Brief introduction of 1023301-84-9

As the paragraph descriping shows that 1023301-84-9 is playing an increasingly important role.

1023301-84-9, tert-Butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Take 4-trifluoromethoxybenzyl alcohol (85 mg, 0.44 mmol, 1.1 eq.).N,N’-carbonyldiimidazole (77 mg, 0.48 mmol, 1.2 eq.)In a 25 mL single-mouth bottle, DMF was dissolved and stirred at room temperature for 2 h.Compound 2-7 (105 mg, 0.4 mmol) was dissolved in DMF.Add triethylamine (64 muL, 0.48 mmol, 1.2 eq.),The reaction solution was added and stirred at room temperature. TLC tracking monitoring.The oil pump was rotated to remove most of the solvent, and EA and saturated sodium bicarbonate solution were added, washed with saturated brine, dried, dried, and passed through a column (PE: EA = 2:1). A white powder of 130 mg was obtained in a yield of 73%., 1023301-84-9

As the paragraph descriping shows that 1023301-84-9 is playing an increasingly important role.

Reference£º
Patent; Guangzhou Hengnuokang Pharmaceutical Technology Co., Ltd.; Zhang Jiancun; Lin Cai; Zou Qingan; (45 pag.)CN108456208; (2018); A;,
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Brief introduction of 1239319-82-4

As the paragraph descriping shows that 1239319-82-4 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1239319-82-4,tert-Butyl 2-amino-7-azaspiro[3.5]nonane-7-carboxylate,as a common compound, the synthetic route is as follows.

1239319-82-4, A solution of the appropriate chloride (1 eq) (ex: 5-chloro-6-methyl-3-(3- trifluoromethoxy-phenyl)-7,8-dihydro-6H-9-oxa-1 ,2,3a,4,6-pentaaza-cyclopenta- (ajnaphthalene) and the appropriate amine (3 to 5 eq) (ex: 1-methyl-piperidin-4- ylamine) in nBuOH (15 mL/mmol) was heated up to 180- 185C under microwave irradiation for 5 h – 10 h (or 24 h at 160-180C in a silicon bath). The solvent was evaporated under vacuum and the residue was purified by flash chromatography (Isolute/Flash, Sill, 2.5% MeOH with 7N ammonia in DCM) or by semi-preparative HPLC (Gemini C18 (150 10 mm; 5 m), Solvent A: water with 0.1 % formic acid; Solvent B: acetonitrile with 0.1 % formic acid. Gradient: 40% of A to 0% of A).The NH-BOC-protected amines got deprotected in the reaction conditions and reacted giving a mixture of regioisomers. Amine: 2-amino-7-aza-spiro[3.5]nonane-7-carboxylic acid tert-butyl esterExample 487-[6- ethyl-3-(3-trifluoromethoxy-phenyl)-7,8-dihydro-6H-9-oxa-1 ,2,3a,4,6- pentaaza-cyclopenta[a]naphthalen-5-yl]-7-aza-spiro[3.5]non-2-ylamineHPLC-MS (method 1 ): Rt=3.37 min, [M+H]+m/z 490.2.1H NMR (700 MHz, MeOD) delta 8.49 (s, 1 H), 8.42 – 8.36 (m, 1 H), 7.66 (td, J = 8.1 , 2.2 Hz, 1 H), 7.42 (d, J = 8.2 Hz, 1 H), 4.45 – 4.39 (m, 2H), 3.47 (ddd, J = 30.1 , 20.6, 10.2 Hz, 4H), 2.96 (d, J = 4.9 Hz, 3H), 2.37 (s, 1 H), 2.34 – 2.27 (m, 2H), 1.90 (dd, J = 12.6, 7.5 Hz, 3H), 1.81 (ddd, J = 22.6, 10.9, 5.6 Hz, 4H), 1.65 (dd, J = 12.3, 8.3 Hz, 2H).Example 49(7-Aza-spiro[3.5]non-2-yl)-[6-methyl-3-(3-trifluoromethoxy-phenyl)-7,8- dihydro-6H-9-oxa-1 ,2,3a,4,6-pentaaza-cyclopenta[a]naphthalen-5-yl]-amineHPLC-MS (method 1 ): Rt=3.21 min, [M+H]+m/z 490.2.1H NMR (300 MHz, MeOD) delta 8.60 (s, 1 H), 8.37 (d, J = 8.0 Hz, 1 H), 7.66 (t, J = 8.1 Hz, 1 H), 7.44 (d, J = 8.3 Hz, 1 H), 4.56 – 4.44 (m, 2H), 4.38 (dd, J = 16.0, 8.0 Hz, 1 H), 3.28 (dd, J = 6.9, 2.5 Hz, 2H), 3.25 – 3.15 (m, 2H), 3.16 – 3.05 (m, 2H), 2.79 (s, 3H), 2.59 – 2.44 (m, 2H), 2.07 – 1.92 (m, 4H), 1.92 – 1.81 (m, 2H).

As the paragraph descriping shows that 1239319-82-4 is playing an increasingly important role.

Reference£º
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); GARCIA COLLAZO, Ana Maria; PASTOR FERNANDEZ, Joaquin; BLANCO APARICIO, Carmen; RODRIGUEZ HERGUETA, Antonio; MARTIN HERNANDO, Jose Ignacio; RAMOS LIMA, Francisco Javier; HERNANDEZ HIGUERAS, Ana Isabel; SALUSTE, Carl-Gustave Pierre; GONZALEZ CANTALAPIEDRA, Esther; MARTINEZ GONZALEZ, Sonia; SALGADO SERRANO, Antonio; NOYA MARINO, Beatriz; WO2011/80510; (2011); A1;,
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Brief introduction of 1454-53-1

1454-53-1, The synthetic route of 1454-53-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1454-53-1,Ethyl 1-benzyl-4-oxopiperidine-3-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

To a 0 C solution of ethyl l-benzyl-4-oxopiperidine-3-carboxylate hydrochloride 1 (6.0 g, 20.2 mmol), urea (2.54 g, 42.42 mmol) in MeOH (100 ml) was added NaOMe (6.14 g, 113.7 mmol) under nitrogen atmosphere. The resulting mixture was stirred at 60 C for 20 hours. The reaction mixture was cooled down to the room temperature and concentrated under reduced pressure, the residue was purified by column chromatography (silica gel, dichloromethane/methanol= 10: 1) to provide the desired compound 2 (2.2 g, 42%). LRMS (M + H+) m/z: calcd 258.29; found 258.30.

1454-53-1, The synthetic route of 1454-53-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ZHOU, Han-Jie; PARLATI, Francesco; WUSTROW, David; WO2014/15291; (2014); A1;,
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Some tips on 1209780-71-1

1209780-71-1, The synthetic route of 1209780-71-1 has been constantly updated, and we look forward to future research findings.

1209780-71-1, tert-Butyl 3,3-difluoro-4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

tert-Butyl 3,3-difluoro-4- hydroxypiperidine-1-carboxylate (0.0706 g, 0.298 mmol) was treated with 1 M KOtBu in THF (0.283 mL, 0.283 mmol) and stirred for 15 minutes. The solution was treated with 2- ([l,2,4]triazolo[4,3-a]pyridin-3-yl)-6,8-difluoroquinoline (0.042 g, 0.149 mmol) and DMF (0.80 mL) then the mixture was stirred at ambient temperature for 16 hours. The mixture was directly chromatographed on SiO2 eluting with a gradient of 2% NH4OH in isopropanol/ethyl acetate. The desired product was collected and concentrated to a colorless oil, (72 mg). MS APCI (+) m/z 500.0 (M+l) detected.

1209780-71-1, The synthetic route of 1209780-71-1 has been constantly updated, and we look forward to future research findings.

Reference£º
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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Simple exploration of 845909-49-1

The synthetic route of 845909-49-1 has been constantly updated, and we look forward to future research findings.

845909-49-1, Ethyl 4-fluoropiperidine-4-carboxylate hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

845909-49-1, Intermediate BKIII): 1-Cyclobutyl-4-fluoro-piperidine-4-carboxylic acid ethyl esterTo a 250 mL round bottle was added compound B1 (P ethyl 4-fluoropiperidine-4- carboxylate, hydrochloride (1.25 g, 5.91 mmol, 1.0 eq), CH2CI2 (40 mL), cyclobutanone B1 (II) (1.30 g, 7.68 mmol, 1.30 eq), and glacial HOAc (0.338 mL, 5.91 mmol, 1.0 eq). After stirring at rt for 5 to 10 min, sodium triacetoxyborohydride (2.00 g, 9.45 mmol, 1.60 eq) was added in one portion. A cloudy solution was obtained. The reaction mixture was stirred at rt for 2 h. To the reaction mixture, 100 mL aqueous NaOH (1 M) was added, and the resulting suspension was stirred at rt for 10 min. The reaction was extracted with EtOAc (150 mL). The organic layer was collected, washed with brine (200 mL), dried over Na2SO4, filtered, and concentrated to afford the desired product, BKIII), as a colorless oil. The crude product was cleaned and subjected to the next step without purification (see next step for the overall reaction yield). 1H NNR (400 MHz, CDCI3, ppm) delta 1.28 (t, J = 7.20 Hz, 3H), 1.64-1.73 (m, 2H), 1.82-1.99 (m, 4H), 2.01-2.21 (m, 6H), 2.72-2.80 (m, 3H), 4.22 (q, J = 7.2 Hz, 2H); 19F NMR (376 Hz, CDCI3, ppm) delta – 166.83.

The synthetic route of 845909-49-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; WO2008/125945; (2008); A2;,
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Simple exploration of 52763-21-0

52763-21-0, The synthetic route of 52763-21-0 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.52763-21-0,Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

Step 1. Preparation of ethyl 1-benzyl-3-hydroxypiperidine-4-carboxylate (i-16b).A solution of ethyl 1-benzyl-3-oxopiperidine-4-carboxylate, HC1 salt (20.0 g, 67.2 mmol) in MeOH (200 ml) in a 500 ml 3-neck flask equipped with thermocouple was cooled to 0C,followed by the additon of sodium borohydride (7.62 g, 201 mmol) portionwise over a period of 75 mm, avoiding excessive gas evolution. After addition, the mixture was stirred at room temperature for 2.5 hr. The mixture was cooled to 0C, quenched dropwise with 200 ml H20 and extracted into EtOAc. The combined organics were washed with water followed by brine, dried over Na2SO4, filtered and concentrated in vacuo to give ethyl 1-benzyl-3-hydroxypiperidine-4-carboxylate. LCMS (ESI) calc?d for C15H21N03 [M+H]: 264, found:264.

52763-21-0, The synthetic route of 52763-21-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; BARR, Kenneth Jay; MACLEAN, John; ZHANG, Hongjun; BERESIS, Richard Thomas; WO2014/28600; (2014); A2;,
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Brief introduction of 38385-95-4

The synthetic route of 38385-95-4 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.38385-95-4,2-(Piperidin-4-yl)-1H-benzo[d]imidazole,as a common compound, the synthetic route is as follows.

To a stirred mixture of 4-biphenyl carboxylic acid (10.0 g, 50.5 mmol) and 2-(piperidin- 4-yl)-lH-benzimidazole (10.1 g, 50.5 mmol) in DCM (400 mL) is added l-(3- dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (12.0 g, 62.7 mmol) and 4- dimethylaminopyridine (3.08 g, 25.2 mmol). After 3 h the reaction mixture is diluted with saturated aqueous NaHCU3 (200 mL) and water (100 mL). The mixture is stirred for a few minutes. The organic layer is separated, washed with water, dried over Na2SO4, filtered and concentrated under reduced pressure. Trituration with EtOAc and further washing with EtOAc gives 14.1 g of [4-(lH-benzimidazol-2-yl)piperidin-l- yl] (biphenyl-4-yl)methanone., 38385-95-4

The synthetic route of 38385-95-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COGAN, Derek; MOSS, Neil; SARKO, Christopher Ronald; BAMFORD, Samantha Jayne; LOKE, Pui Leng; NAPIER, Spencer Charles, R.; TYE, Heather; WHITTAKER, Mark; WO2010/80357; (2010); A1;,
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