Tag: M.W:100-200

85908-96-9, N-Boc-2-Piperidone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,85908-96-9

General procedure: Based on the procedure by Bogle.1 To a solution of the amide 11 in THF at – 78 C was added dropwise a solution of lithium hexamethyldisilazide (1.0 M in THF, 2.1 eq) and the mixture stirred at – 78 C for 10 min. Benzylchloroformate (1.0 eq) was then added dropwise and the resulting mixture stirred at – 78 C for 1 h. The reaction was quenched at – 78 C with aq. NH4Cl (10 mL) and allowed to warm to room temperature. The aqueous layer was extracted with EtOAc (3 x 25 mL), the combined organic extracts washed with brine (10 mL), dried (Na2SO4) and concentrated in vacuo. The crude mixture was loaded onto a silica column and eluted with a PE/ethyl acetate mixture to yield the ester 12. NB. Deviations from this procedure are noted.

As the paragraph descriping shows that 85908-96-9 is playing an increasingly important role.

Reference：
Article; Moody, Catherine L.; Franckevi?ius, Vilius; Drouhin, Pauline; Klein, Johannes E.M.N.; Taylor, Richard J.K.; Tetrahedron Letters; vol. 53; 15; (2012); p. 1897 – 1899;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.14813-01-5,1-Benzylpiperidin-3-ol,as a common compound, the synthetic route is as follows.

Step 3: To a solution of [3](1.00 g, 5.23 mmol) in benzene (90 mL),sodium (1 10 mg) was added. After refluxing for 2.5 h, a solution of methylbenzilate (1.27 g, 5.23 mmol) was added and the reaction refluxed overnight. The benzene was evaporated in vacuo and the residue purified by flash chromatography (eluted first with 20% EtOAc/Hexane, then 5%MeOH/CH2Cl2) to give [1O04] as transparent liquid (981 mg,46%).Analytical Data: [1004] ESIMS: 402[M++1]

14813-01-5, As the paragraph descriping shows that 14813-01-5 is playing an increasingly important role.

Reference：
Patent; SPHAERA PHARMA PVT. LTD.; DRUG DISCOVERY RESEARCH CENTRE; DUGAR, Sundeep; MAHAJAN, Dinesh; RAI, Santosh Kumar; RAO, Kanury; SINGH, Varshneya; WO2015/181837; (2015); 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.10338-57-5,4-(Piperidin-1-yl)benzaldehyde,as a common compound, the synthetic route is as follows.

10338-57-5, General procedure: In a 100-mL round-bottom flask, ethyl 2-(7-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo- 2H-benzo[b][1,4]oxazin-4(3H)-yl)acetate (22) (1 g, 3.03 mmol, 1 equivalent) and triphenylphosphine (0.87 g, 3.33 mmol, 1.1 equivalent) were dissolved in ethanol (50 mL). After stirring at 25 C for 10-15 min, aromatic aldehyde (3.03 mmol, 1 equivalent) was added slowly along with stirring. The reaction mixture was allowed to stir for 24 h. The progress of the reaction was monitored by TLC (MeOH:CHCl3::1:19). On completion of the reaction, the solvent was evaporated under reduced pressure. The solid residue so obtained was purified by column chromatography (MeOH:CHCl3::1:49) to afford the desired benzoxazine-based arylidinyl succinimide derivative (23-36) in 64-80% isolated yield.

As the paragraph descriping shows that 10338-57-5 is playing an increasingly important role.

Reference：
Article; Sharma, Atul K.; Prasad, Suchita; Sharma, Sunil K.; Synthetic Communications; vol. 47; 20; (2017); p. 1854 – 1863;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 10 ; 3-[({4-[(3-chloro-2-fluorophenyl) amino]-7-methoxyquinazolin-6- yl} methyl) amino] piperidin-2-one; (Process (a)); 4- [ (3-Chloro-2-fluorophenyl) amino]-7-methoxyquinazoline-6-carbaldehyde was coupled with 3-amino-piperidin-2-one (prepared by converting 3-amino-piperidin-2-one hydrochloride to the free-base form) using an analogous method to that described for the equivalent step in Example 1 to give the title compound ; 1H NMR spectrum : (DMSO d6) 1. 5= (m, 1H), 1.68 (m, 1H), 1.84 (m, 1H), 2.16 (m, 1H), 2.73 (brs, 1H), 3.05 (dd, 1H), 3.13 (m, 2H), 3.84 (d, 1H), 3.93 (d, 1H), 3.98 (s, 3H), 7.21 (s, 1H), 7.28 (t, 1H), 7.48 (t, 1H), 7.53 (m, 2H), 8.35 (s, 1H), 8.44 (s, 1H), 9.80 (s, 1H); Mass Spectrum : (M+H) +430., 138377-80-7

The synthetic route of 138377-80-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/75439; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2,7-diazaspiro[4.5]decan-1 -one hydrochloride (0.572 g, 3mmol) and triethylamine (0.836 mL, 6.00 mmol) in dichloromethane (DCM) (15ml_), cooled in an ice-water bath, was added 4-bromo-2-(trifluoromethyl)benzenesulfonyl chloride (0.971 g, 3.00 mmol). The reaction was allowed to warm to room temperature and stirred for 18 hours.The reaction was diluted with DCM (35 ml), washed with water (30ml_), passed through a hydrophobic frit and reduced in vacuo. The residue was purified by silica chromatography (Biotage SP4) eluting with 60% EtOAc in iso-hexanes (3 column volumes), a gradient from 60-100% EtOAc (over 9 column volumes) then EtOAc (3 column volumes) to yield 7-{[4-bromo-2-(trifluoromethyl)phenyl]sulfonyl}-2,7- diazaspiro[4.5]decan-1 -one as a white solid (0.826g, 62%)1H NMR (400 MHz, Chloroform-d) d ppm 1.61 – 1 .67 (m, 1 H) 1.69 – 1 .84 (m, 3 H) 2.05 (s, 1 H) 2.43 (s, 1 H) 2.59 – 2.67 (m, 1 H) 2.85 (d, J=12.7 Hz, 1 H) 3.32 – 3.45(m, 2 H) 3.67 (d, J=12.5 Hz, 1 H) 3.80 – 3.87 (m, 1 H) 5.72 (br. s., 1 H) 7.80 – 7.88 (m, 2 H) 8.01 (d, J=1.5 Hz, 1 H)

1187173-43-8, As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

Reference：
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; GLEAVE, Robert James; HACHISU, Shuji; PAGE, Lee William; BESWICK, Paul John; WO2011/141728; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

768-66-1, 2,2,6,6-Tetramethylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,768-66-1

n-BuLi (2.5M in hexanes, 2.27 mL, 5.67mmol) was added to cold(-50 C) anhydrous THF (20 mL) under nitrogen. 2,2, 6, 6-Tetramethylpiperidine (0.957, 0.8 g, 5.67mmol) was then added and the mixture stirred at-78 C for 30 min. A solution of the title compound of Preparation 53 (0.5 g, 2.68mmol) in THF (5 mL) was added dropwise and the mixture was stirred at-78 C for 60 min. Then, iodine (1.51 g, 5.94mmol) was added and the mixture was stirred at that temperature for 90 min and then warmed to r. t. The mixture was quenched with methanol and the residual iodine destroyed with sat. sodiumthiosulphate (aq. ). The mixture was concentrated in vacuo, partitioned between ethyl acetate and water and the organic layer was washed with water, dried and evaporated to give an oil which was purified by column cromatography (n-Hex/EtOAc 4: 1) to afford the title compound (87% yield) as an oil which crystallised. 8 (CDCI3) : 4.22 (s, 3H), 7.47 (m, 3H), 7.96 (m, 2H), 8.29 (s,1 H).

768-66-1 2,2,6,6-Tetramethylpiperidine 13035, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ALMIRALL PRODESFARMA, S.A.; WO2005/49581; (2005); 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.4629-80-5,1,3-Dimethylpiperidin-4-one,as a common compound, the synthetic route is as follows.

B. Preparation of the Piperidinol The 3-bromo-i-propoxybenzene (200 g, 0.08703 mol) was combined with THF (tetrahydrofuran) (540 ml) under nitrogen and cooled to about -75 C. n-Butyllithium (565 ml, 0.8306 mol) was added dropwise while maintaining the mixture at less than -70 C. After 2 hours 1,3-dimethyl-4-piperidone (106.7 g, 0.8389 mol) was added while maintaining the temperature of the mixture between -80 C. and -70 C. After stirring for 2 hours at -70 C., the reaction mixture was then added to 6N HCl (280 ml) while maintaining the temperature at 20-25 C. The pH was adjusted to 1 with 12 N HCl. The aqueous layer was isolated and heptane (320 ml) was added to it along with 50% NaOH (48 ml, to pH of 13-14). The resulting mixture was allowed to stand overnight. The mixture was heated to 45-50 C. and the upper layer was separated. The remaining aqueous layer was extracted with heptane (320 ml) at 45-50 C. The combined organic fractions were washed with de-ionized water (120 ml) at 45-50 C. The resulting organic layer was vacuum distilled at a pot temperature of about 55 C. at 100 mmHg to remove part of the heptane. Crystallization from heptane provided 151.8 g of the named product. Melting point 75.0-76.0 C. Analysis: Calc. for (C16 H25 NO2): C, 72.97; H, 9.57; N, 5.32. Found: C, 72.87; H, 9.56; N, 5.25.

4629-80-5, Big data shows that 4629-80-5 is playing an increasingly important role.

Reference：
Patent; Eli Lilly and Company; US5136040; (1992); 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.5773-58-0,3-Methylpiperidin-4-one,as a common compound, the synthetic route is as follows.

1-(3-Chloropyridin-2-yl)-3-methylpiperidin-4-one was prepared by dissolving 19.2 g 3-methylpiperidin-4-one (168.9 mmol) and 25 g of Compound of Formula A (168.9 mmol) in DMSO (400 mL) under a nitrogen atmosphere to form a reaction mixture. The reaction mixture was stirred at 85 C for 12 hours. Therefter, the solvent was removed under reduced pressure. The residue was purified by column chromatography on a silica gel column, using a gradient of from 10:90 to 98:2 (by volume) ethyl acetate:hexane as an eluent, to provide 9 g of l-(3-chloropyridin-2-yl)-3-methylpiperidin-4-one., 5773-58-0

The synthetic route of 5773-58-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EURO-CELTIQUE, S.A.; WO2005/4866; (2005); 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.4801-58-5,Piperidin-1-ol,as a common compound, the synthetic route is as follows.

A mixture of N-hydroxypiperidine (1.01 g, 10 mmol), azodicarbonamide (1.39 g, 12 mmol) and methanol (10 ml) was heated to reflux for 50 minutes. During this period the solid, initially orange in colour, changed into a whitish precipitate. After cooling to ambient temperature, said precipitate was separated by suction and washed twice with methanol (2 x 5 ml). All the methanol fractions were combined and under agitation 5,5-dimethylcyclohexane-1,3-dione (10 mmol) was added. After 10 minutes, the methanol was removed under vacuum (water bath temperature 50?C) to give a crude compound of formula (3). This crude compound was dissolved in a methanol solution (15 ml) containing acetyl chloride (0.86 g, 11 mmol). The methanol was removed under vacuum and the residue of formula (3) in hydrochloride form was ground in acetone. Yield: 62% Formula: C13H22CINO3 MW: 275.8 g/mol Acid dissociation constants: pKa1 = 3.47, pKa2 = 6.92 m.p.: 174.5-175.5?C 1H-NMR (DMSO-ds): delta 0.98 (6H, s), 1.48 (1H, m), 1.66 (2H, d, J=12.5 Hz), 1.83 (2H, broad s), 1.94-2.07 (1H, m), 2.33 (4H, broad s), 3.23 (1H, broad s), 3.67 (1H, d, J=11.0 Hz), 4.36 (1H, d, J=11.5 Hz), 10.93 (1H, broad s), 11.32 (1H, broad s). 13C-NMR (DMSO-d6): delta 21.9, 23.6, 27.9, 28.7, 32.0, 46.2 (broad), 59.4, 64.4, 107.4.

4801-58-5, As the paragraph descriping shows that 4801-58-5 is playing an increasingly important role.

Reference：
Patent; ABIOGEN PHARMA S.p.A.; EP2345639; (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.25137-01-3,(R)-Ethyl piperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

Example 15 (R)-1-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)methyl)-3-piperidinecarboxylic Acid Hydrochloride Sodium cyano borohydride (314 mg, 5 mmol) was dissolved in dry methanol (6 ml) and added dropwise under stirring to a mixture of 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylmethanal (1.11 g, 5 mmol, prepared similarly as described in Ger. Offen 2,106 165, 1971, CA 75, 129 687), (R)-3-piperidinecarboxylic acid ethyl ester (1.57 g, 10 mmol) and zinc chloride (0.34 g, 2.5 mmol) in dry methanol (15 ml) over 30 minutes at 25 C. The reaction mixture was stirred at room temperature for 3 h and left to stand overnight. The methanol was evaporated in vacuo and benzene (30 ml) and 1.2 N sodium bicarbonate (15 ml) were added. The phases were separated and the organic phase was washed with water (30 ml) and brine (2*30 ml) and dried (sodium sulfate). The solvent was evaporated in vacuo and the oily residue (1.68 g) was purified by column chromatography on silica gel (35 g) using benzene as eluent. This afforded 1.12 g (62%) of (R)-1-((10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)methyl)-3-piperidinecarboxylic acid ethyl ester. TLC: Rf=0.54 (SiO2:chloroform/methanol=30:1).

25137-01-3, As the paragraph descriping shows that 25137-01-3 is playing an increasingly important role.

Reference：
Patent; Novo Nordisk A/S; US6569849; (2003); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem