Heterocyclic Building Blocks-piperidine

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;,
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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;,
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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;,
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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;,
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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;,
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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
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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;,
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769944-78-7,769944-78-7, 1-N-Boc-4-(4-Bromophenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4- (4-bromophenyl) piperidine-1-carboxylate (510 mg, 1.499 mmol) , 4, 4, 4′, 4′, 5, 5, 5′, 5′-octamethyl-2, 2′-bi (1, 3, 2-dioxaborolane) (761 mg, 3 mmol) and KOAc (441 mg, 4.5 mmol) in DME (20 ml) was degassed with N2 and PdCl2 (dppf) -CH2Cl2 (122 mg, 0.15 mmol) was added. The resulting mixture was degassed with N2 again and was heated to 80 overnight. After cooling to rt, the mixture was added with 10mL of NH4Cl (aq) , and extracted with EtOAc (20mL ¡Á 2) . The combined organic phase was washed with brine (20mL) , dried over Na2SO4 (anhydrous) , filtered and concentrated under reduced pressure. The residue was purified by flash chromatography (EA/Hexane 0: 100-1: 5) to give the title compound (500 mg , 86) . 1H NMR (400 MHz, CDCl3) delta ppm 1.27 (s, 9H) , 1.34 (s, 12H) , 1.57 -1.72 (m, 2H) , 1.82 (br d, J13.05 Hz, 2H) , 2.66 (br s, 1 H) , 2.80 (br t, J12.05 Hz, 2H) , 4.25 (br d, J12.80 Hz, 2H) , 7.11 -7.42 (m, 2H) , 7.77 (d, J8.03 Hz, 2H) . LC-MS: [M+H-100] + 288.2.

As the paragraph descriping shows that 769944-78-7 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA; MOTZ, Gregory; MAVRAKIAS, Konstantinos John; LIU, Jinbiao; LIU, Lei; ZHENG, Qiangang; XUN, Guoliang; XIAO, Qitao; (417 pag.)WO2017/114497; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24228-40-8,Ethyl N-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.,24228-40-8

Step 1. 1-Benzylpiperidine-4-carboxylic acid Ethyl 1-benzylpiperidine-4-carboxylate (13.73 g) in methanol (100 ml) was treated with 40% aqueous sodium hydroxide (8.3 ml) at room temperature 16 h. The solvent was removed in vacuo and the residue re-dissolved in water (100 ml), acidified with dilute hydrochloric acid to pH 4 and concentrated. The residue was extracted with hot ethanol (200 ml), filtered and concentrated again. Addition of dichloromethane resulted in crystallization giving the title compound as a colourless crystaline solid, (3.24 g, 27%). Removal of solvent from the filtrate and trituration with ether gave a second batch as an amorphous white solid, (9.24 g, 73%); numax (CH2 Cl2) 2496 (vbr), 1720 and 1604 (br) cm-1.

The synthetic route of 24228-40-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hinks; Jeremy David; Takle; Andrew Kenneth; Hunt; Eric; US6020368; (2000); A;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.73579-08-5,1-Methyl-4-(methylamino)piperidine,as a common compound, the synthetic route is as follows.

To a mixture of Scheme 43 compound 1 (1.0 g, 4.90 mmol), Scheme 43 compound 2 (630 mg, 4.90 mmol), Cs2C03 (4.8 g, 14.80 mmol) and Xantphos (286 mg, 0.49 mmol) in dry toluene (10 mL) was added Pd(OAc)2 (111 mg, 0.49 mmol) and the reaction mixture was heated to 100 ¡ãC for 4 h. After TLC showed the starting material was completely consumed, the reaction mixture was cooled to RT, passed through a pad of celite and washed with EtOAc. The filtrate was washed with water and brine, dried over Na2S04 and concentrated to give a residue which was purified by flash chromatography on silica gel (eluting with CH2Cl2/MeOH 100/0 gradually increasing to 95/5) to give Scheme 43 compound 3 (1.0 g, 83percent) as a yellow solid. MS [ESI, MH+] = 251.15., 73579-08-5

The synthetic route of 73579-08-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MANNKIND CORPORATION; TOLERO PHARMACEUTICALS, INC.; ZENG, Qingping; FARIS, Mary; MOLLARD, Alexis; WARNER, Steven L.; FLYNN, Gary A.; WO2014/52365; (2014); A1;,
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