Day: November 6, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.268550-48-7,tert-Butyl 1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate,as a common compound, the synthetic route is as follows.

5-Bromo-3,4-dichloro-2-(2,5-dimethyl-1H-pyrrol-1-yl)pyridine (225 mg, 0.70 mmol) and 8- boc-2,8-diaza-spiro-[4.5]decan-1-one (197 mg, 0.77 mmol) were loaded in a microwave vial. The capped vial was evacuated using high vacuum and purged with nitrogen (each three times). Triethylamine (0.27 mL, 2.11 mmol) and NMP (2.3 mL) were added and the mixture was degassed by using the high vacuum and purged with nitrogen three times. The reaction mixture was heated in the microwave at 220 C for 1 h before it was cooled and dropped in vigorously stirred water (8 mL). The resulting precipitate was filtered off and the residue was purified by chromatography on silica gel (dichloromethane/ethanol) to give the title compound as a light brown solid (153 mg, 50%). 1H-NMR (500 MHz, CDCl3) ppm = 8.47 (s, 1H), 6.53 (bs, 1 H), 5.90 (s, 2H), 3.52 – 3.32 (m, 6H), 2.25 – 2.10 (m, 4H), 2.01 (s, 6H), 1.58 (d, J=13.0, 2H). HRMS m/z (ESI+) [M+H]+ C19H22BrClN4O, calc 437.0738, found 437.0733, Rt = 3.05 min (HPLC method B).

268550-48-7, The synthetic route of 268550-48-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GMBH; CANCER RESEARCH TECHNOLOGY LIMITED; SCHIEMANN, kai; STIEBER, Frank; BLAGG, Julian; MALLINGER, Aurelie; WAALBOER, Dennis; RINK, Christian; CRUMPLER, Simon Ross; WO2014/63778; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

160296-40-2, tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

60% Sodium hydride (717mg, [18MMOL)] was suspended in anhydrous dimethylformamide [(50ML)] under nitrogen at [5C.] To this was added portion-wise 6-bromo naphthalene-2-thiol (3.89g, 16mmol). The mixture was stirred at [5C] for 30 minutes. 1- (t- [BUTOXYCARBONYL)-4- (4-FLUOROBENZOYL) PIPERIDINE] (Reference Example 12; [5.] 00g 16mmol) was then added to the solution and the reaction heated at [60C] for 16 hours. The solution was poured into water [(75ML)] and washed with EtOAc [(2X75ML).] The organic phases were combined then washed with water then brine. The solution was dried over MgS04, after filtration and evaporation a solid was isolated. This was recrystallised from EtOAc/isohexane resulting in a cream solid (2.96g, 35%). NMR (DMSO-d6) 1.37 (s, [11H),] 1.72 (m, 2H), 2.86 (m, 2H), 3.52 (m, 1H), 3.92 (m, 2H), 7.31 (d, 2H), 7.55 (d, 1H), 7.69 (d, 1H), 7.93 (m, 4H), 8.17 (s, 1H), 8.26 (s, 1H) ; m/z 470., 160296-40-2

The synthetic route of 160296-40-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/33427; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

91419-52-2, 1-Boc-4-Cyanopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

91419-52-2, 4-Cyanopiperidine-1-formic acid tert-butyl ester (3.00 g, 14.27 mmol) was dissolved in tetrahydrofuran (30.00 mL), slowly added dropwise with lithium hexamethyldisilazide (1M, 28.54 mL) at -78 C and under nitrogen protection, stirred for 1 hour, slowly added dropwise with ethyl chloroformate (3.10 g, 28.54 mmol), and then stirred under nitrogen protection at -78 C for 1 hour. TLC showed that the reaction was complete. The reaction solution was quenched with a saturated solution of sodium bicarbonate (15 mL), and extracted with ethyl acetate (20 mL x 2), and the combined organic phases were washed with a saturated solution of ammonium chloride (50 mL), dried over anhydrous sodium sulfate (10 g), filtered and concentrated to give 1E. 1H NMR (400MHz, DMSO-d6) delta= 4.23 (q, J = 7.1 Hz, 2H), 4.00 – 3.92 (m, 2H), 2.95 (br, 2H), 2.07 (br d, J = 13.3 Hz, 2H), 1.89 – 1.76 (m, 2H), 1.40 (s, 9H), 1.24 (t, J = 7.1 Hz, 3H).

91419-52-2 1-Boc-4-Cyanopiperidine 1514443, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Medshine Discovery Inc.; LIU, Xile; DING, Charles Z.; CHEN, Shuhui; WU, Lingyun; HU, Lihong; WAN, Haiwen; (118 pag.)EP3567030; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4138-26-5, Piperidine-3-carboxamide is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4138-26-5

Piperidine-3-carboxylic acid amide 1a (25 g, 0.195 mol) was added portionwise to a stirred solution of lithium aluminum hydride (14.8 g, 0.39 mol, 2.0 equiv) in dry THF (0.6 L). When the initial effervescence had subsided, the reaction was heated at reflux under N2 at rt for 24 h. The reaction was quenched by dropwise addition of saturated sodium sulfate solution with stirring until no further effervescence was observed. The suspension was filtered through a celite plug, washed with THF (400 mL), and the filtrate concentrated under reduced pressure. The crude residue was distilled to yield pure product 1b as a colorless oil (12.4 g, 55percent).

4138-26-5 Piperidine-3-carboxamide 92980, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Du Bois, Daisy Joe; Mao, Long; Rogers, Daniel Harry; Williams, John Patrick; US2004/14775; (2004); 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.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

Step 8: N-(cis-3-{[(4,4-Difluoropiperidin-1-yl)sulfonyl]methyl}cyclobutyl)-N-methyl-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine To a mixture of 4,4-difluoropiperidine (77 mg, 0.64 mmol) and triethylamine (97 mg, 0.96 mmol) in tetrahydrofuran (20 mL) at 0¡ã C. was added dropwise a solution of cis-[3-(methyl{7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)cyclobutyl]methanesulfonyl chloride (150 mg, 0.320 mmol) in tetrahydrofuran (10 mL). The mixture was allowed to warm to room temperature overnight. The solvent was evaporated and the residue was taken up in ethyl acetate (80 mL). The solution was washed with brine (30 mL), dried over sodium sulfate and concentrated to afford the crude title compound (134 mg) as a white solid. LC/MS (exact mass) calculated for C24H29F2N5O4S2; 553.651. found (M+H+); 554.3., 21987-29-1

As the paragraph descriping shows that 21987-29-1 is playing an increasingly important role.

Reference£º
Patent; Pfizer Inc.; Brown, Matthew Frank; Fenwick, Ashley Edward; Flanagan, Mark Edward; Gonzales, Andrea; Johnson, Timothy Allan; Kaila, Neelu; Mitton-Fry, Mark J.; Strohbach, Joseph Walter; TenBrink, Ruth E.; Trzupek, John David; Unwalla, Rayomand Jal; Vazquez, Michael L.; US2014/243312; (2014); 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.177-11-7,1,4-Dioxa-8-azaspiro[4.5]decane,as a common compound, the synthetic route is as follows.

a) 8-(6-Methylpyrimidin-4-yl)-1,4-dioxa-8-azaspiro[4.5]decane; A solution of 1,4-dioxa-8-azaspiro[4.5]decane (3.04 g, 2.72 mL, 21.2 mmol), 4-chloro-6-methylpyrimidine (3.00 g, 23.4 mmol) and N,N-diisopropylethylamine (4.12 g, 5.56 mL, 31.8 mmol) in dioxane (50 mL) was heated to 140 C. in the microwave for 40 minutes. The reaction mixture was concentrated, then directly purified by flash chromatography (silica gel, 70 g, 0% to 15% MeOH/NH4OH (9:1) in dichloromethane). The title compound was obtained as orange oil (4.64 g, 93%).MS ISP (m/e): 236.2 (100) [(M+H)+].1H NMR (CDCl3, 300 MHz): delta (ppm)=8.52-8.51 (m, 1H), 6.42 (m, 1H), 4.01 (s, 4H), 3.83-3.79 (m, 4H), 2.45 (s, 3H), 1.79-1.75 (m, 4H)., 177-11-7

As the paragraph descriping shows that 177-11-7 is playing an increasingly important role.

Reference£º
Patent; Baumann, Karlheinz; Flohr, Alexander; Goetschi, Erwin; Green, Luke; Jolidon, Synese; Knust, Henner; Limberg, Anja; Luebbers, Thomas; Thomas, Andrew; US2011/201605; (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.159635-22-0,tert-Butyl 3-hydroxy-4-methylenepiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Method DStep 1: (S)-3-hydroxy-4-methylene-piperidine-1-carboxylic Acid tert-butyl ester; 3-Hydroxy-4-methylene-piperidine-1-carboxylic acid tert-butyl ester (4.50 g; 21.10 mmol) was dissolved in TBME (63 ml) and vinyl butyrate (22.5 ml). The solution was heated to 50 C. and the reaction started by the addition of Lipase TL IM (1.08 g (carrier-fixed); Novozymes, Denmark). The solution was stirred at 50 C. for 20 h until the enantiomeric excess of the retained alcohol was >99%. The enzyme was filtered off, the filter cake washed with TBME and the filtrate concentrated in vacuo. The residual oil was chromatographed on silicagel (100 g; 0.040-0.063 mm; CH2Cl2?CH2Cl2/acetone 9:1) to separate the formed optically enriched (R)-butyrate from the retained (S)-alcohol (1.83 g white crystals; 41%). Analytics: >99 GC; >99% ee (GC on BGB-176; 30 m¡Á0.25 mm; H2; 1.2 bar; 80 C. to 210 C. with 3 C./min; inj. 200 C.; Det. 210 C.; retention times: (R)-alcohol 29.60 min, (S)-alcohol 29.81 min). [alpha]D=-17.70 (c=1.00, CHCl3)., 159635-22-0

159635-22-0 tert-Butyl 3-hydroxy-4-methylenepiperidine-1-carboxylate 10584700, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Adam, Jean-Michel; Aebi, Johannes; Binggeli, Alfred; Green, Luke; Hartmann, Guido; Maerki, Hans P.; Mattei, Patrizio; Ricklin, Fabienne; Roche, Olivier; US2010/22518; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

496807-97-7, 3,3-Difluoropiperidine hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,496807-97-7

General procedure: To a solution of 1 -benzyl-1 H-pyrazole-4-carboxylic acid [5-(3-formyl-phenyl)-1 – (toluene-4-sulfonyl)-1 H-pyrrolo[2,3-b]pyridin-3-yl]-amide (100mg, 0.17mmol) in MeOH (1 ml_) was added 4A molecular sieves followed by dimethylamine, 2.0M solution in THF (4ml_, 8mmol) and the reaction stirred for 3 hours at RT. Sodium triacetoxyborohydride (72.1 mg, 0.34mmol) was added and the reaction stirred 18 hours at RT. The inorganic material was separated via filtration and the filtrate was diluted with DCM. The solution was washed with aqueous saturated sodium bicarbonate solution, dried (MgSO4) and concentrated in vacuo. The residue was purified using automated column chromatography eluting with DCM to 10% MeOH/DCM. Fractions containing pure compound were combined and concentrated in vacuo to give the desired compound as a colourless glass, 61 mg, 58.0%.

The synthetic route of 496807-97-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERNALIS (R&D) LIMITED; STOKES, Stephen; GRAHAM, Christoper John; RAY, Stuart Christopher; STEFANIAK, Emma Jayne; WO2013/114113; (2013); 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.923036-30-0,N-((3R,4R)-1-Benzyl-4-methylpiperidin-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine,as a common compound, the synthetic route is as follows.

Example 9; Preparation of [(3R, 4R)-1-benEyl-4-methyl-piperidin-3-yl]-methyl-(7H-pyrrolo[2,3-cl]pyrimidin-4-y.)-amine:; To a clean, nitrogen-purged reactor were charged 50% sodium hydroxide solution (210 ml) and (1-benzyl-4-methyl-piperidin-3-yl)-methyl-[7-(toluene-4-sulfonyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-amine (30.0 g, 0.061 mol). The mixture was heated to 95-105C for a minimum of 5 hours then cooled to 70- 900C and water (300 ml) was added. The slurry was cooled to room temperature over a minimum of 1.5 hours and held at room temperature for 1 hour. The solids were isolated by filtration and washed with water (120.0 ml) to obtain 25.2 g of the title compound, water wet.1H NMR (400 MHz, CD3OD): delta 8.05 (s, 1H), 7.36-7.28 (m, 5H)1 7.24-7.20 (m, 1H), 7.06 (d, J=3.7 Hz, 1H), 6.62 (d, J=3.7 Hz, 1H), 5.08 (bs, 1H), 3.58-3.52 (m, 5H), 2.85 (dd, J=11.2, 7.0 Hz, 1H), 2.68 (dd, J=11.2, 3.7 Hz, 1H), 2.65-2.59 (m, 1 H), 2.45-2.39 (m, 1H), 2.29-2.20 (m, 1H), 1.90-1.81 (m, 1 H), 1.70- 1.63 (m, 1 H), 0.98 (d, J=7.0 Hz, 3H). 13C NMR (400 MHz, Of6-DMSO1 mixture of isomers): delta 166.8, 164.4, 158.6, 155.1 , 138.4, 137.9, 137.8, 136.6, 135.5, 135.3, 112.7, 110.0, 72.4, 64.3 (b), 62.4, (b), 60.3 (b), 44.5, 41.8, 40.9, 30.5, 24.8.

923036-30-0, The synthetic route of 923036-30-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2007/12953; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4606-65-9, 3-(Hydroxymethyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Scheme 6, step B. To a solution ofpiperidin-3-ylmethanol (2.10 g, 0.018 mol) inCHzCh (20 mL) is added triethylamine (5.53 g, 0.0547 mol) followed by tbutyldimethylchlorosilane( 4.127 g, 0.0275 mol) and the reaction mixture is stirred atroom temperature. After 24 hours, the reaction mixture is washed with water, saturated solution ofNaHC03, and brine. The combined organic layers are combined and dried25over sodium sulfate, filtered, and concentrated under reduced pressure. The resultingresidue is purified by flash chromatography (silica gel) over a gradient using 0-10%MeOH in dichloromethane to afford the title compound (2.50 g, 60 %). Mass spectrum(m/z): 231.2 (M+1)., 4606-65-9

The synthetic route of 4606-65-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ELI LILLY AND COMPANY; BLANCO-PILLADO, Maria-Jesus; VETMAN, Tatiana Natali; FISHER, Matthew Joseph; KUKLISH, Steven Lee; WO2014/4230; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem