Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.148763-41-1,Methyl N-Boc-piperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

Step-1: Preparation of intermediate-43a; To a stirred solution of intermediate 42 (750 mg, 3.08 mmol) in THF (10 mL) was added a solution of lithium aluminum hydride in THF (1 M in THF, 2.16 mL) at 0 C. The reaction mass was stirred at 0 C. for 2 h. The reaction mass was quenched with sodium sulfate decahydrate. The reaction mass was filtered through a bed of celite and washed with ethyl acetate. The filtrate was evaporated to dryness. The residue was purified by flash column chromatography to afford intermediate 43a (660 mg, >99%)., 148763-41-1

The synthetic route of 148763-41-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; H. LUNDBECK A/S; US2011/92475; (2011); A1;,
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136624-42-5, 4-Amino-1-benzylpiperidine-4-carbonitrile is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

STEP B: 4-Amino-1 -benzylpiperidine-4-carboxamide To a solution of 4-amino-1 -benzylpiperidine-4-carbonitrile (6.15 g, 28.6 mmol) in DCM (70 mL) at -5C was added 95-97% sulfuric acid (50 mL). The reaction mixture was stirred at 0 to 5C overnight and the organic layer was discarded. The resulting mixture was poured onto crushed ice (1000 mL) and the pH adjusted to pH 9 with aqueous 5N NaOH, keeping the temperature below 10C. The resulting mixture was partitioned between water and EtOAc (3 x 500 mL). The organic phase was dried over MgS04, filtered and concentrated in vacuo to yield a residue. The residue was purified by flash chromatography (silica gel, 5% MeOH in DCM) to yield 2-(4-bromophenyl)-1 ,3- diazaspiro[4.4]non-1 -en-4-one (5.06 g, 76%). 1 H NMR (300 MHz, CDCI3) delta ppm 1 .29 – 1 .57 (m, 4 H), 2.14 – 2.39 (m, 4 H), 2.71 – 2.84 (m, 2 H), 3.55 (s, 2 H), 5.41 (br. s., 1 H), 7.20 – 7.38 (m, 5 H), 7.45 (br. s., 1 H); MS m/z 234 (M+H)+.

136624-42-5, 136624-42-5 4-Amino-1-benzylpiperidine-4-carbonitrile 10680206, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; BIGNAN, Gilles C.; CONNOLLY, Peter J.; LU, Tianbao L.; PARKER, Michael H.; LUDOVICI, Donald; MEYER, Christophe; MEERPOEL, Lieven; SMANS, Karine; ROCABOY, Christian; WO2014/39769; (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.255051-14-0,4-(2-(Trifluoromethyl)phenyl)piperidine hydrochloride,as a common compound, the synthetic route is as follows.

255051-14-0, Example 4: Preparation of ( 6-Fluoro- [1,2,4] triazolo [4, 3-a]pyridin-3- (trifluoromethyl)phenyl)piperidin-1-yl>methanone Step B: To a solution of ethyl 6-fluoro- [1, 2, 4] triazolo [4, 3- a]pyridine-3-carboxylate (0.100 g, 0.478 mmol) in THF (5 mL) was added a solution of LiOH hydrate (0.040 g, 0.956 mmol) in 0 (2 mL) . The mixture stirred for 20 minutes and was then acidified to pH 6 with 2 N HC1 followed by subsequent concentration under reduced pressure. The resulting residue was added to a mixture of 4-(2- (trifluoromethyl) henyl) iperidine hydrochloride (5, 0.127 g, 0.478 mmol) , benzotriazole-l-yl-oxy-tris- (dimethylamino) -phosphonium hexafluorophosphate (0.423 g, 0.956 mmol), i-Pr2NEt (0.185 g, 1.43 ntmol) in DMF (4 mL) . The mixture stirred at ambient temperature for 16 hours and was then poured into 0 and extracted with EtOAc (30 mL) . The organic layer was washed with brine (2 x 30 raL) , dried over Na;SO , filtered, and concentrated under reduced pressure. The resulting residue was chromatographed over silica gel (0-50% E CAc in hexar.ee) and freeze dried to give ( 6-fluoro- [ 1 , 2,4] triazolo [4, 3- a]pyridin-3-yl ) ( 4- ( 2- (trifluoromethyl) henyl) piperidin-l- yDmethanone as a white solid (0.101 g, 53%); mp 168-170 C; NMR (300 MHz, CDCli) 8 9.18 (s, 1H) , 7.88 (m, 1H) , 7.66 (d, J = 7.5 Hz, 1H , 7.55-7.30 (m, 4H) , 5.76 (m, 1H) , 4.99 (m, 1H) , 3.40-3.30 (m, 2H) , 2.98 (m, 1H) , 2.03-1.76 (m, 4H) ; MS (ESI+ ) ra/z 393 [M>H] * .

As the paragraph descriping shows that 255051-14-0 is playing an increasingly important role.

Reference£º
Patent; THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK; PETRUKHIN, Konstantin; CIOFFI, Christopher; JOHNSON, Graham; DOBRI, Nicoleta; FREEMAN, Emily; CHEN, Ping; CONLON, Michael; ZHU, Lei; WO2014/152013; (2014); A1;,
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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

A mixture of 3-(2-chloro-5-ethylpyrimidin-4-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole-6-carbonitrile (0.26 g, 707 umol, 1.00 eq), tert-butyl (S)-3-aminopiperidine-1-carboxylate (170 mg, 848 umol, 1.20 eq), Pd2(dba)3 (64.7 mg, 70.7 umol, 0.10 eq), BINAP (44.0 mg, 70.7 umol, 0.10 eq) and Cs2CO3 (461 mg, 1.41 mmol, 2.00 eq) in dioxane (10 mL) was degassed and purged with N2 for 3 times, and then the mixture was stirred at 120C for 5 hrs under N2 atmosphere. TLC (Petroleum ether: EtOAc = 1: 1, Rf = 0.24) and HPLC indicated one major new spot with larger polarity was detected. The reaction mixture was added silicone to remove Pd2(dba)3 (64.7 mg, 70.7 umol, 0.10 eq), the mixture was stirred 30 mins then was filtered and the solvent was concentrated under reduced pressure to give a residue. The residue was purified by prep-TLC (Petroleum ether: EOAc = 1: 1). tert-butyl (3S)-3-((4-(6-cyano-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-3-yl)-5-ethylpyrimidin-2-yl)amino)piperidine-1-carboxylate (0.15 g, 282 umol, 40percent yield) was obtained as red oil.

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.

Reference£º
Patent; MARINEAU, Jason, J.; ZAHLER, Robert; CIBLAT, Stephane; WINTER, Dana, K.; KABRO, Anzhelika; ROY, Stephanie; SCHMIDT, Darby; CHUAQUI, Claudio; MALOJCIC, Goran; PIRAS, Henri; WHITMORE, Kenneth, Matthew; LUND, Kate-Iyn; SINKO, Bill; SPROTT, Kevin; (418 pag.)WO2018/13867; (2018); A1;,
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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ 73874-95-0, Which mentioned a new discovery about 73874-95-0

TROPOMYOSIN-RELATED KINASE (TRK) INHIBITORS

Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 73874-95-0, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 73874-95-0

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 130250-54-3, molecular formula is C13H23NO4, introducing its new discovery., 130250-54-3

Quinoline derivatives as neurokinin receptor antagonists

The present invention relates to substituted quinoline hydrazides of Formula (I): wherein R1, R2, R3, R4, R5, X, Y and Z are defined herein, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-2 and/or neurokinin-3 (NK-3) receptors. These compounds can thus be used in methods of treatment to suppress and treat such disorders.

130250-54-3, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 130250-54-3

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143900-43-0, One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time.In a article, authors is Malmquist, Jonas, mentioned the application of 143900-43-0, Name is (R)-tert-Butyl 3-hydroxypiperidine-1-carboxylate, molecular formula is C10H19NO3

Discovery of a Novel Muscarinic Receptor PET Radioligand with Rapid Kinetics in the Monkey Brain

Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic neurotransmitter concentrations in vivo. The radioligand of choice for such measurements on the cholinergic system is the muscarinic receptor antagonist N-[1-11C]propyl-3-piperidyl benzilate (PPB). In an effort to overcome the shortcomings with the technically cumbersome synthesis of [11C]PPB, we designed and synthesized four structurally related analogues of PPB, of which (S,R)-1-methylpiperidin-3-yl)2-cyclopentyl-2-hydroxy-2-phenylacetate (1) was found to bind muscarinic receptors with similar affinity as PPB (3.5 vs 7.9 nM, respectively). (S,R)-1 was radiolabeled via N-11C-methylation at high radiochemical purity (>99%) and high specific radioactivity (>130 GBq/mumol). In vitro studies by autoradiography on human brain tissue and in vivo studies by PET in nonhuman primates demonstrated excellent signal-to-noise ratios and a kinetic profile in brain comparable to that of [11C]PBB. (S,R)-[11C]1 is a promising candidate for measuring changes in endogenous acetylcholine concentrations.

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 287192-97-6, molcular formula is C12H19NO2, introducing its new discovery. , 287192-97-6

2,5-DIOXOIMIDAZOLIDIN-4-YL ACETAMIDES AND ANALOGUES AS INHIBITORS OF METALLOPROTEINASE MMP12

The invention provides compounds of formula (I) in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds of the invention are inhibitors of metalloproteinase MMP12 and are among other things useful for the treatment of obstructive airways diseases, such as asthma and chronic obstructive pulmonary disease (COPD).

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 287192-97-6, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 287192-97-6

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Chemistry is traditionally divided into organic and inorganic chemistry. 183483-09-2. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 183483-09-2

HETEROCYCLIC ANALGESIC COMPOUNDS AND METHODS OF USE THEREOF

One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 183483-09-2 is helpful to your research. 183483-09-2

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 160809-38-1, molecular formula is C16H21NO4, introducing its new discovery., 160809-38-1

CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF

Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.

160809-38-1, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 160809-38-1

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Piperidine – Wikipedia,
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