New learning discoveries about 32018-96-5

32018-96-5 1-Benzyl-4-methylpiperidin-3-one 12084828, apiperidines compound, is more and more widely used in various fields.

32018-96-5, 1-Benzyl-4-methylpiperidin-3-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The TiCl4(0.2g, 1mmol), NEt3(0.15g, 1 . 5mmol) suspended 200 ml in toluene, then add 1-benzyl-4-methyl-3-ketone piperidine (20.3g, 100mmol), temperature control 35 C methylamine solution is added to the reaction solution (9.32g, 120mmol) reaction 4 hours, adding NaBH (OAC) 3 (0.32g, 1 . 5mmol), glacial acetic acid 2 ml, temperature control 35 C reaction, thin layer monitoring after the reaction is complete. Adding saturated salt water washing, anhydrous sodium sulfate for drying the organic phase, the organic phase concentrated, with residues 35% hydrochloric acid ethanol re-crystallization, to obtain (3R, 4R)-cis-1-benzyl-4-methyl-3-methylamino-piperidine dihydrochloride 17.2g, yield 85.0%, optical purity 99.0% (HPLC method)., 32018-96-5

32018-96-5 1-Benzyl-4-methylpiperidin-3-one 12084828, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Shandong Elohim Pharmaceutical Group Co., Ltd.; Liu, Xiaofeng; Sun, Yuanlong; Yang, Linlin; (12 pag.)CN105884781; (2016); A;,
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Some tips on 203662-51-5

As the paragraph descriping shows that 203662-51-5 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.203662-51-5,4-Allyl-1-Boc-4-hydroxypiperidine,as a common compound, the synthetic route is as follows.

4.i) 4-Hydroxy-4-oxiranylmethyl-piperidine-1-carboxylic acid tert-butyl esterA solution of 4-allyl-4-hydroxy-piperidine-1-carboxylic acid tert-butyl ester (3.1 g, 12.8 mmol, prepared according to J. Comb. Chem. 2002, 4, 125) in DCM and 0.3 M phosphate buffer (pH 8, 150 mL) was treated with mCPBA (3.5 g, 1.1 eq, 70%) and the mixture vigorously stirred at rt overnight. Further 3.5 g of mCPBA were added. After a total of 24 h, the phases were separated, the org. phase dried over MgSO4 and concentrated. CC (hex/EA 2:1 to 1:1 to EA) gave the desired intermediate as colourless oil (0.88 g, 26%).1H NMR (CDCl3) delta: 3.90-3.70 (m, 2H), 3.30-3.10 (m, 3H), 2.83 (dd, J=4.1, 4.9 Hz, 1H), 2.51 (dd, J=2.7, 4.9 Hz, 1H), 1.89 (dd, J=3.8, 14.5 Hz, 1H), 1.80-1.40 (m, 4H), 1.47 (s, 9H)., 203662-51-5

As the paragraph descriping shows that 203662-51-5 is playing an increasingly important role.

Reference£º
Patent; Actelion Pharmaceuticals Ltd; US2011/39823; (2011); A1;,
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Simple exploration of 153749-89-4

As the paragraph descriping shows that 153749-89-4 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.153749-89-4,tert-Butyl 2-cyanopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 9.1; 2-(2H-Tetrazol-5-yl)-piperidine-1-carboxylic acid tert-butyl ester; 2-Cyano-piperidine-1-carboxylic acid tert-butyl ester (2.1 g, 10 mmol) was mixed with sodium azide (0.715 g, 11 mmol) and ammonium chloride (0.588 g, 11 mmol) in N,N-dimethylformamide (7.5 mL). The reaction mixture was heated at 100 C. for overnight. The reaction mixture was cooled to room temperature and diluted with water. The product was extracted using ethyl acetate. The organic phase was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The crude yellow oil gave a white solid after trituration with ethyl acetate, as the title product (1.23 g, 48.6%).1H NMR (300 MHz, CDCl3): delta 5.63 (br, 1H), 4.02 (m, 1H), 2.76 (td, 1H), 2.43 (m, 1H), 1.96 (m, 2H), 1.8 (m, 2H), 1.55 (m, 2H), 1.49 (s, 9H)., 153749-89-4

As the paragraph descriping shows that 153749-89-4 is playing an increasingly important role.

Reference£º
Patent; AstraZeneca AB; NPS PHARMACEUTICALS, INC.; US2007/259916; (2007); A1;,
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New learning discoveries about 188869-05-8

188869-05-8, The synthetic route of 188869-05-8 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.188869-05-8,tert-Butyl 3-bromo-4-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-Butyl 3-bromor4-oxopiperidine-l-carboxylate (1.0 g, 3.6 mmol) and benzothioamide (490 mg, 3.6 mmol) were heated neat at 1400C for 10 minutes. After cooling down, the resulting brown solid was sonicated in AcOEt for 10 minutes. Filtration and drying yielded 2-phenyl-4, 5, 6, 7- tetrahydrothiazolo [5, 4-c] pyridine hydrobromide as a brown solid (829 mg, 78percent): 1H NMR (400 MHz, DMSO-d6) delta 3.06-3.12 (m, 2H), 3.49-3.57 (m, 2H), 4.46-4.53 (m, 2H), 7.50-7.56 (m, 3H), 7.90-7.94 (m, 2H), 9.35 (br, 2H); m/z (APCI pos) 217.1 (10percent) [M+H] .

188869-05-8, The synthetic route of 188869-05-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2008/11130; (2008); A2;,
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Downstream synthetic route of 336191-17-4

336191-17-4, 336191-17-4 tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate 34178604, apiperidines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.336191-17-4,tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate,as a common compound, the synthetic route is as follows.

tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate (7.21 g, 30.0 mmol) is dissolved in TEA (7.69 mL) in DCM (200 mL) at 0 C. and treated dropwise with cyclobutanone (2.92 mL, 38.9 mmol). The mixture is stirred for 30 min and sodium triacetoxyborohydride (9.53 g, 4.56 mmol) is added in portions. The reaction mixture is stirred at rt overnight, basified with 1N NaOH solution and extracted with DCM (2¡Á100 mL). The combined extracts are washed with water, brine, dried over anhydrous Na2SO4 and concentrated in vacuo to afford the title compound. LC-MS (Method 1): 295.4.

336191-17-4, 336191-17-4 tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate 34178604, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Xu, Yuelian; Caldwell, Timothy M.; Xie, Linghong; Chenard, Bertrand L.; US2008/247964; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Some tips on 79421-45-7

79421-45-7 1-(4-Nitrophenyl)piperidin-4-ol 613768, apiperidines compound, is more and more widely used in various fields.

79421-45-7, 1-(4-Nitrophenyl)piperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

79421-45-7, The 4-hydroxy-N-(4-nitrophenyl)piperidine (11.1 g, 50 mmol) obtained in Example 1(1) was dissolved in methanol (100 ml) and tetrahydrofuran (50 ml), and 10% palladium-carbon (8.0 g) was added thereto, followed by stirring at room temperature in an atmosphere of hydrogen gas for 7 hours. After the insoluble material was filtered with Celite, the filtrate was concentrated under reduced pressure, diethyl ether was added to the obtained residue, and the precipitate was collected by filtration, thereby obtaining 4-hydroxy-N-(4-aminophenyl)piperidine (9.25 g, 94%) as a reddish-purple solid.1H-NMR (CDCl3): delta (ppm) 1.65-1.77 (m, 2H), 1.94-2.11 (m, 2H), 2.71-2.85 (m, 2H), 3.23-3.92 (m, 5H), 6.64 (d, J=8.9 Hz, 2H), 6.83 (d, J=8.9 Hz, 2H)

79421-45-7 1-(4-Nitrophenyl)piperidin-4-ol 613768, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; TAIHO PHARMACEUTICAL CO., LTD.; US2011/319413; (2011); A1;,
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Analyzing the synthesis route of 1155-56-2

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

1155-56-2, 1-Benzyl-N-phenylpiperidin-4-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium borohydride (0.90 g, 23.9 mmol) was suspended in 20 mL of 1,2-dichloroethaneunder a nitrogen atmosphere and cooled in an ice water bath. Acetic acid (4.30 g,71.6 mmol) was added dropwise with an addition funnel. It was rinsed with 10 mL of 1,2-dichloroethane. The mixture was removed from the ice water bath and stirred atroom temperature for 16 h. A solution of 1-benzyl-4-piperidone (3.00 g, 15.9 mmol),aniline (2.62 g, 17.4 mmol), acetic acid (0.96 g, 15.9 mmol), and 12 mL of 1,2-dichloroethane was added dropwise with an addition funnel. It was rinsed with 10 mLof 1, 2 dichloroethane. The mixture was stirred for 24 h at room temperature. Thereaction mixture was poured over 100 mL of a 2 M aqueous sodium hydroxide solutionand extracted with chloroform (3 ? 100 mL). The combined organic extractswere dried with sodium sulfate, filtered, and the volatiles were evaporated providing4.40 grams of the reductive amination product. The residue was taken up in 120 mL1,2-dichloroethane and propionyl chloride (7.36 g, 79.5 mmol) was added with asyringe. The mixture was heated to reflux under a nitrogen atmosphere for 20 h. Thereaction mixture was allowed to cool to room temperature and the volatiles wereevaporated. The residue was taken up with 100 mL of saturated aqueous sodiumbicarbonate and 100 mL of chloroform. The organic layer was separated. The aqueouslayer was washed with chloroform (2 ? 100 mL). The combined organic extractswere dried with sodium sulfate, filtered, and the volatiles were evaporated providing5.70 g of a tan oil. The residue was dissolved in 15 mL of isopropanol and the solutionwas gently warmed. Oxalic acid (2.21 g, 17.5 mmol) in 5 mL of water was addedwith an addition funnel. It was rinsed with 2 mL of water followed by 3 mL of isopropanol.The mixture was allowed to cool to room temperature and was placed in are frigerator for 24 h. The white precipitate obtained was filtered, washed with icebath cooled isopropanol, and dried to provide 5.52 g of the oxalate salt 1 in 70%yield. An analytical sample was prepared by recrystallization from methanol. mp213-215C; 1H NMR (CD3OD) d 7.49-7.41 (m, 8 H), 7.19 (d, 2 H, J D 6.41 Hz),4.80-4.73 (m, 1 H), 4.22 (s, 2 H), 3.44 (br d, 2 H, J D 12.36 Hz), 3.10 (br t, 2 H, J D10.72 Hz), 2.04 (br d, 2 H, J D 13.23 Hz), 1.95 (q, 2 H, J D 7.33 Hz), 1.69-1.60 (m,2 H), 0.96 (t, 3 H, J D 7.33 Hz); 13C NMR (CD3OD) d 175.75, 165.21, 137.99,130.92, 129.97, 129.82, 129.60, 129.19, 128.97, 128.89, 59.97, 51.42, 49.98, 27.99,27.31, 8.51.Anal. Calcd for C23H28N2O5: C, 66.97; H, 6.84; N, 6.79. Found: C, 66.87; H, 6.99; N,6.76., 1155-56-2

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

Reference£º
Article; Walz, Andrew J.; Hsu, Fu-Lian; Organic Preparations and Procedures International; vol. 49; 5; (2017); p. 467 – 470;,
Piperidine – Wikipedia
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Brief introduction of 625471-18-3

625471-18-3 (S)-tert-Butyl 3-aminopiperidine-1-carboxylate 1501975, apiperidines compound, is more and more widely used in various fields.

625471-18-3, (S)-tert-Butyl 3-aminopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

625471-18-3, 1,1-Dimethylethyl (3S)-3-AMINOPIPERIDINE-L-CARBOXYLATE (2. 1G, 10. 5MMOL), cyclopentanone (4.65mL, 52. 5MMOL), and 10percent palladium on carbon (0.2g) in methanol (80ML) were hydrogenated at 60psi overnight in a Parr hydrogenator. The catalyst was filtered off and the filtrate evaporated in vacuo. The resultant oil was purified by flash chromatography on silica, eluting with ethyl ACETATE/CYCLOHEXANE (15: 85 to 30: 70), to give the title compound as an oil.

625471-18-3 (S)-tert-Butyl 3-aminopiperidine-1-carboxylate 1501975, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2005/305; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Some tips on 98977-34-5

As the paragraph descriping shows that 98977-34-5 is playing an increasingly important role.

98977-34-5,98977-34-5, 1-tert-Butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

NaH 60percent in oil (0.62g, 15.48mmol) was added portionwise to a solution of 1,3-(4-oxo-piperidine)-dicarboxylic acid, 1-(1,1-dimethylethyl) 3-ethyl ester (2g, 7.37mmol) suspended in THF (20ml) cooled at 0¡ãC. The mixture was stirred for 30 minutes at 0¡ãC and then allowed to warm to ambient temperature and stirred for a further 1 hour. 3- fluorobenzylbromide (1.36ml, 11.06mmol) was added and the resulting solution was stirred at room temperature overnight. Water and then EtOAc were added. The organic layer was extracted, washed with brine, dried over MgS04, filtrered and concentrated. The residue (2.78g) was purified by Normal phase on irregular SiOH (15-40muiotaeta, 300g); mobile phase (85percent heptane, 15percent EtOAc). The pure fractions were collected and the solvent was evaporated, yielding lg (35.7percent) of intermediate 88.

As the paragraph descriping shows that 98977-34-5 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; GUILLEMONT, Jerome, Emile, Georges; MOTTE, Magali, Madeleine, Simone; LANCOIS, David, Francis, Alain; THOMAS, Sebastien, Robert, Gaston; BALEMANS, Wendy, Mia, Albert; WO2013/160431; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Brief introduction of 216854-23-8

As the paragraph descriping shows that 216854-23-8 is playing an increasingly important role.

216854-23-8, (S)-tert-Butyl piperidin-3-ylcarbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of tert-butyl N-[(3S)-piperidin-3-yl]carbamate (100 mg, 0.499 mmol) and triethylamine (0.104 ml, 0.749 mmol) in DCM (2.5 ml) was cooled to 0C, benzyl chloroformate (0.101 ml, 0.599 mmol) was added, and the mixture was stirred for one hour. Water was added to the reaction mixture, then extraction with ethyl acetate was carried out. The organic layer was washed with a saturated aqueous sodium chloride solution and then dried over anhydrous sodium sulfate. The drying agent was removed by filtration, then concentration under reduced pressure was carried out. The resulting residue was purified by silica gel column chromatography (ethyl acetate/hexane) to give benzyl (3S)-3-[(2-methylpropan-2-yl)oxycarbonylamino]piperidine-1-carboxylate (159 mg, 95%) as a colorless solid. LCMS: m/z 335 [M+H]+, 216854-23-8

As the paragraph descriping shows that 216854-23-8 is playing an increasingly important role.

Reference£º
Patent; Chugai Seiyaku Kabushiki Kaisha; MURATA, Takeshi; KAWADA, Hatsuo; NIIZUMA, Satoshi; HARA, Sousuke; HADA, Kihito; SHIMADA, Hideaki; TANAKA, Hiroshi; MIO, Toshiyuki; EP2842946; (2015); A1;,
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Piperidine | C5H11N – PubChem