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The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula wherein the combination of R1 and R2 are as defined herein, and pharmaceutically acceptable salts thereof.

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Piperidine – Wikipedia,
Piperidine | C5H18095N – PubChem

 

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A chemoselective, one-pot transformation of aldehydes to nitriles

This paper describes a procedure for direct conversion of aldehydes to nitriles using O-(diphenylphosphinyl)hydroxylamine (DPPH). Aldehydes are smoothly transformed to their corresponding nitriles by heating with DPPH in toluene. The reaction can be accomplished in the presence of alcohol, ketone, ester, or amine functionality.

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Piperidine – Wikipedia,
Piperidine | C5H18057N – PubChem

 

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A chemoselective, one-pot transformation of aldehydes to nitriles

This paper describes a procedure for direct conversion of aldehydes to nitriles using O-(diphenylphosphinyl)hydroxylamine (DPPH). Aldehydes are smoothly transformed to their corresponding nitriles by heating with DPPH in toluene. The reaction can be accomplished in the presence of alcohol, ketone, ester, or amine functionality.

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Piperidine – Wikipedia,
Piperidine | C5H18057N – PubChem

 

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Enantioselective organo-singly occupied molecular orbital catalysis: The carbo-oxidation of styrenes

The first enantioselective organocatalytic carbo-oxidation of styrenes has been accomplished using singly occupied molecular orbital (SOMO) catalysis. Geometrically constrained radical cations are generated from the one-electron oxidation of enamines formed from the condensation of aldehydes with a secondary amine catalyst. These SOMO-activated radical cations are susceptible to attack by commercially available styrenes, forming gamma-oxyaldehyde products with uniformly high levels of asymmetric induction. Broad latitude in both the aldehyde and styrene scope is readily tolerated. This report highlights the potential of SOMO catalysis to enable the development of entirely new classes of asymmetric reactions that have no traditional catalytic equivalents. Copyright

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Piperidine – Wikipedia,
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A chemoselective, one-pot transformation of aldehydes to nitriles

This paper describes a procedure for direct conversion of aldehydes to nitriles using O-(diphenylphosphinyl)hydroxylamine (DPPH). Aldehydes are smoothly transformed to their corresponding nitriles by heating with DPPH in toluene. The reaction can be accomplished in the presence of alcohol, ketone, ester, or amine functionality.

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Piperidine – Wikipedia,
Piperidine | C5H18056N – PubChem

 

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PIPERIDINE DERIVATIVES FOR USE IN THE TREATMENT OF PANCREATIC CANCER

The present invention relates to novel piperidine derivatives having better cell growth inhibitory activities toward cancer cell cultures and, more particularly, PANC-1 cancer cell cultures than FK866. Accordingly, the present invention relates to compounds of formula (I), wherein Ar1 is aryl or heteroaryl, which are optionally substituted by one, two or three substituents selected from lower alkyl; lower alkoxy; formyl; hydroxyl; lower alkyl substituted by lower alkoxy or hydroxyl; A is CnH2n, CnH2n-2 or CnH2n-4, wherein n=4,5,6,7; B is =N-CN, oxo (=0), thio (=S); D is NH, -CH=CH-; Ar2 is aryl or heteroaryl which are optionally substituted by one, two or three halogen substituents; wherein, if B is oxo (=0), Ar1 and Ar2 are not simultaneously phenyl and pyridine-3-yl; B and D are not simultaneously =N-CN and -CH=CH-, or a pharmaceutically acceptable salt, a racemic mixture or its corresponding enantiomers and/or optical isomers. The compounds of formula (I) and their pharmaceutically usable addition salts possess valuable pharmacological properties. Specifically, it has been found that the compounds of the present invention, alone or in combination with other therapeutic active compounds, have an activity as chemotherapeutic agents against cancer and, more particularly, pancreatic cancers.

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Piperidine – Wikipedia,
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Enantioselective Formal alpha-Methylation and alpha-Benzylation of Aldehydes by Means of Photo-organocatalysis

Detailed herein is the photochemical organocatalytic enantioselective alpha-alkylation of aldehydes with (phenylsulfonyl)alkyl iodides. The chemistry relies on the direct photoexcitation of enamines to trigger the formation of reactive carbon-centered radicals from iodosulfones, while the ground-state chiral enamines provide effective stereochemical control over the radical trapping process. The phenylsulfonyl moiety, acting as a redox auxiliary group, facilitates the generation of radicals. In addition, it can eventually be removed under mild reducing conditions to reveal methyl and benzyl groups.

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To a solution of compound F1 (15 g, 66 mmol) in THF (50 mL) was added phenyltrimethylammonium tribromide (37.2 g, 99 mmol) at 0. The mixture was stirred at 0 under N 2 for 1 hours. The mixture was quenched with water (50 mL) and extracted with EtOAc (200 mL ¡Á 2) . The organic phase was washed with brine (100 mL) , dried over anhydrous Na 2SO 4, concentrated to give the residue (7.5 g) . The residue was dissolved in ethanol (200 mL) was added compound F2 (7.5 g, 99 mmol) . The mixture was stirred at 80 for 3 h. The mixture was cooled to room temperature and concentrated under reduced pressure to afford the crude product, which was purified by silica gel chromatography (elution gradient: EA/PE, 1/1, v/v) . Pure fractions were evaporated to dryness to afford compound F3 (10 g) as a pale-yellow solid, yield: 53.5%. 1H NMR (400 MHz, CDCl 3) : delta ppm 1.48 (s, 9H) , 1.53-1.60 (m, 2H) , 1.90-1.96 (m, 2H) , 2.77-2.85 (m, 3H) , 4.17 (s, 2H) , 6.78 (s, 1H) . LCMS: Rt = 1.20 min, MS Calcd.: 283.1, MS Found: 283.9 [M+H] +.

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Reference£º
Patent; ZHUHAI YUFAN BIOTECHNOLOGIES CO., LTD; LIAO, Xuebin; (208 pag.)WO2019/206049; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

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a. 4-(6-Fluoro-[1,2,4]triazolo[4,3-a]pyridin-3-ylmethyl)-piperidine-1-carboxylic acid tert-butyl ester (Intermediate 22a) A dark brown solution of (5-fluoro-pyridin-2-yl)-hydrazine (549 mg, 4.32 mmol) and N-Boc-4-piperidine acetaldehyde (Aldrich, 982 mg, 4.32 mmol) in EtOH (10 mL) was stirred at reflux for 30 min, then cooled to 0 C., diluted with DCM (25 mL) and then (diacetoxyiodo)benzene (1.67 g, 5.18 mmol) was added portionwise over 1 min. The purple solution was stirred at RT for 30 min, then aqueous NaOH (1M, 20 mL) was added and the mixture shaken. The aqueous layer was extracted with DCM (2*20 mL), then the combined organics passed through a hydrophobic frit and concentrated in vacuo to leave an orange solid. FCC, using 3% MeOH in DCM, gave the title compound as a pale orange solid (1.53 g, 90%). LCMS (Method 3): Rt 3.15, m/z 235 [M-CO2C4H9+H+].

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Reference£º
Patent; Chiesi Farmaceutici S.p.A.; VAN NIEL, Monique Bodil; Ray, Nicholas Charles; Alcaraz, Lilian; Panchal, Terry Aaron; Jennings, Andrew Stephen Robert; Armani, Elisabetta; Cridland, Andrew Peter; Hurley, Christopher; US2013/150343; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

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142374-19-4, To a solution of tert-butyl 4-(oxoethyl)piperidine-l-carboxylate as obtained in step 1 in dichloromethane (50 mL) was added DAST (1.2 g, 7.8 mmol) at 0 0C. The reaction mixture was warmed to room temperature and stirred for 17 h. A 5% aqueous solution of sodium bicarbonate was added and the layers were separated. The organic layer was washed with saturated sodium bicarbonate, and brine, dried over sodium sulfate, filtered and concentrated to provide tert-butyl 4-(2,2-difluoroethyl)piperidine-l-carboxylate that was used directly without further purification.

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Reference£º
Patent; EXELIXIS, INC.; AAY, Naing; ARCALAS, Arlyn; BOWLES, Owen, Joseph; BUSSENIUS, Joerg; CURTIS, Jeffry, Kimo; DEFINA, Steven, Charles; DUBENKO, Larisa; HARRIS, Jason, R.; JACKSON-UGUETO, Eileen, E.; MANALO, Jean-Claire, Limun; KIM, Angie, Inyoung; PACK, Michael; PETO, Csaba, J.; RICE, Kenneth, D.; TSANG, Tsze, H.; WO2010/138487; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem