Tag: M.W:300-400

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 some cases, the catalyzed mechanism may include additional steps.In a article, 1283095-48-6, molcular formula is C16H23NO3S, introducing its new discovery. 1283095-48-6

COMPOUNDS USEFUL FOR INHIBITING ROR-GAMMA-T

The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof, formula (A).

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 1283095-48-6, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 1283095-48-6

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Piperidine | C5H23360N – PubChem

 

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 159634-59-0, name is tert-Butyl 3-oxo-2,3-dihydrospiro[indene-1,4′-piperidine]-1′-carboxylate, introducing its new discovery. 159634-59-0

BICYCLIC HETEROCYCLES, DRUGS CONTAINING SAID COMPOUNDS, USE THEREOF, AND METHOD FOR PRODUCTION THEREOF

The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids and bases, which have valuable pharmacological properties, in particular an inhibitory action on the signal transduction mediated by tyrosine kinases, their use for the treatment of illnesses, in particular of tumoral diseases and of benign prostatic hyperplasia (BPH), of diseases of the lung and of the airways, and the preparation thereof.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.159634-59-0, you can also check out more blogs about159634-59-0

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167414-75-7, Benzyl 4-(3-ethoxy-3-oxopropanoyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

167414-75-7, Intermediate 5, 3.8 g (20 mmol), intermediate 3 7.99 g (24 mmol) was added to a 50 mL round bottom flask. Add 20 mL of acetic acid to dissolve, and react at 130 ¡ãC overnight. After the reaction is completed, the acetic acid is removed by rotary evaporation. 1M NaOH was added dropwise to precipitate a large amount of off-white solid, which was filtered. Washing with a small amount of MeOH gave a white solid M086. Yield 75.0percent.

The synthetic route of 167414-75-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kunming Xianghao Technology Co., Ltd.; Luo Huairong; Hong Xuechuan; Zhu Xi; Zhu Jinmei; Wu Guisheng; Deng Zixin; Zhu Yingmin; Lu Yungang; Deng Ke; Qu Chunrong; (25 pag.)CN103694242; (2016); B;,
Piperidine – Wikipedia
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149353-75-3, 4-(1-(tert-Butoxycarbonyl)piperidin-4-yl)benzoic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Production Example 1-8 tert-Butyl 4-(4-((4-((6-methoxy-1-(methylcarbamoyl)-1H-indol-5-yl)oxy)pyridin-2-yl)carbamoyl)phenyl)piperidine-1-carboxylate Benzotriazole (2.32 g, 19.5 mmol) was dissolved in dichloromethane (100 mL), thionyl chloride (1.4 mL, 19.2 mmol) was added under nitrogen atmosphere at room temperature, and the mixture was stirred for 5 minutes. 4-(1-(tert-Butoxycarbonyl)piperidin-4-yl)benzoic acid described in Production Example 1-12 (5.4 g, 17.7 mmol) was added to the reaction mixture at mom temperature, and the mixture was stirred for 25 minutes. The reaction mixture was filtered through a glass filter entirely covered with anhydrous sodium sulfate and then washed with dichloromethane, then the filtrate was added to a mixture of 5-((2-aminopyridin-4-yl)oxy)-6-methoxy-N-methyl-1H-indole-1-carboxamide described in Production Example 1-6 (2.5 g, 8.01 mmol), triethylamine (11 mL, 79.4 mmol), and 4-dimethylaminopyridine (101 mg, 0.827 mmol) in tetrahydrofuran (80 mL) at 0 C. The resultant was stirred at mom temperature for 5 hours and then the reaction mixture was concentrated under vacuum. Water and ethyl acetate were added to the residue for partition, and the organic layer was washed with a saturated saline solution, and then dried over anhydrous magnesium sulfate and filtered. The filtrate was concentrated under vacuum, the residue was dissolved in tetrahydrofuran, an excessive quantity of 9.8 M methylamine methanol solution was added at room temperature, and the mixture was stirred for 50 minutes. The reaction mixture was concentrated under vacuum, the residue was dissolved in dichloromethane, and the resultant was purified with NH silica gel column chromatography (n-heptane:ethyl acetate=1:1-1:3-0:1). The target fraction was concentrated under vacuum and the precipitate was collected by filteration and washed with diethyl ether and ethyl acetate to obtain the title compound (3.15 g, 66%). The filtrate was combined with the mixture fraction and the resultant was concentrated under vacuum and dissolved in dichloromethane, and the resultant was purified with NH silica gel column chromatography (n-heptane:ethyl acetate=1:1-1:3-0:1). The target fraction was concentrated under vacuum and the precipitate was collected by filteration and washed with diethyl ether and ethyl acetate to obtain the title compound (264 mg, 5.5%). 1H-NMR Spectrum (CDCl3) delta (ppm): 1.48 (9H, s), 1.55-1.69 (2H, m), 1.77-1.87 (2H, m), 2.64-2.89 (3H, m), 3.02-3.07 (3H, m), 3.86 (3H, s), 4.26 (2H, brs), 5.62 (1H, brs), 6.50-6.55 (1H, m), 6.61 (1H, dd, J=5.9, 2.2 Hz), 7.22 (1H, d, J=3.7 Hz), 7.27-7.33 (3H, m), 7.80 (2H, d, J=8.4 Hz), 7.90 (1H, d, J=2.2 Hz), 8.04 (1H, s), 8.09 (1H, d, J=5.9 Hz), 8.54 (1H, brs)., 149353-75-3

As the paragraph descriping shows that 149353-75-3 is playing an increasingly important role.

Reference£º
Patent; Eisai R&D Management Co., Ltd.; Funasaka, Setsuo; Okada, Toshimi; Tanaka, Keigo; Nagao, Satoshi; Ohashi, Isao; Yamane, Yoshinobu; Nakatani, Yusuke; Karoji, Yuki; US2014/235614; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

877399-73-0, 1-Boc-4-(4-Iodo-1H-pyrazol-1-yl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

877399-73-0, The compoundTert-Butyl 4- (4-iodo-1H-pyrazol-1- yl) nicardine- 1 -carboxylate (1.00 g, 2.650 mmol)Dissolved in DMSO (llmL)Then, bis (pinacolato) diboron (942.5 mg, 3.710 mmol)And CH3C00K (1.04 g, 10.60 mmol),After pumping gas (N2) three times,Pd (PPh3) 2Cl2 (93.0 mg, 0.130 mmol) was added.After the reaction was stirred at 80 C for 2 hours,The mixture was cooled to room temperature and filtered off with suction. The filtrate was washed with brine (100 mL ¡Á 3), dried over anhydrous Na 2 SO 4 and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (PE / EtOAc (v / v) = 5/1) The title compound was obtained as a white solid (878.6 mg, 87.9%).

The synthetic route of 877399-73-0 has been constantly updated, and we look forward to future research findings.

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Patent; (88 pag.)CN104119331; (2018); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120014-07-5,2-((1-Benzylpiperidin-4-yl)methylene)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one,as a common compound, the synthetic route is as follows.

Preparation of l-Benzyl-4-[(5, 6-dimethoxy-l-indanon)-2-v? methylpiperidine hydrochloride (Donepezil Hydrochloride) l-Benzyl-4-[5, 6-dimethoxy-l-indanon)-2-ylidenyl] methyl piperidine was taken in tetrahydrofuran (200ml) followed by addition of palladium-carbon (Ig). The mixture was hydrogenated at 20-30 0C under 1,5 atmospheric pressure for 8 hours, monitored by HPLC analysis and analysis shows ~ 38.5% of debenzylated impurity in the reaction mass.

120014-07-5, 120014-07-5 2-((1-Benzylpiperidin-4-yl)methylene)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one 10762160, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; WO2007/108011; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

287953-54-2, Benzyl 4-(chlorosulfonyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 190 mg (0.6 mmol) of benzyl 4-(chlorosulfonyl)-1-piperidinecarboxylate in 10 mL THF was treated with a 10-fold excess of 40% aq. dimethylamine and the mixture was stirred at room temperature for 2 hrs. The THF was removed under vacuum. The residue was diluted with water, extracted with CH2Cl2, and dried. Chromatography on alumina, eluting with CH2Cl2, gave 175 mg (89% yield) of benzyl 4-[(dimethylamino)sulfonyl]-1-piperidinecarboxylate as an oil: 1H NMR (CDCl3) delta 7.40-7.30 (m, 5H), 5.13 (s, 2H), 4.31 (m, 2H), 3.10 (tt, J=12.0, 3.7 Hz, 1H), 2.92 (s, 6H), 2.85-2.75 (m, 2H), 2.04 (br d, J=13.7 Hz, 2H), 1.76 (dq, J=12.6, 4.5 Hz, 2H).

287953-54-2, The synthetic route of 287953-54-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Pathway Therapeutics Limited; US2010/249099; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

385425-15-0, 1-(4-Iodophenyl)piperidin-2-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under room temperature, will be sequentially 1 – (piperidin-2-oxo-1-yl) – 4-iodophenylamino (2.5 g, 8.3 mmol), 1 – (3-fluoro-4-ethoxy phenyl) – 7-oxo -4, 5, 6, 7-tetrahydro -1H-pyrazolo [3,4-c] pyridine-3-carboxylic acid ethyl ester (2.4 g, 6.9 mmol) and potassium carbonate (2.1 g, 15.1 mmol) by adding DMSO in (35 ml). Under the protection of nitrogen is added in the mixture of the obtained CuI (650 mg, 3.4 mmol) and 1,10-phenanthrene (613 mg, 3.4 mmol). The obtained mixture is heated to 120 C, reaction 12 hours. After the completion of the reaction, the obtained cooling to room temperature the mixture, adding water. The resulting mixture is extracted with ethyl acetate. The resulting organic phase is concentrated under reduced pressure to obtain crude products. Crude product is purified by silica gel column chromatography (PE:EA=1:1) to obtain 1.0 g (yield: 26.7%) of the product., 385425-15-0

The synthetic route of 385425-15-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CSPC Weisheng Pharmaceutical Technology (Shijiahuang) Co., Ltd.; Shi, Ying; Gao, Qingzhi; Mi, Yi; Wang, Xuliang; (129 pag.)CN105384739; (2016); 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.385425-15-0,1-(4-Iodophenyl)piperidin-2-one,as a common compound, the synthetic route is as follows.

Example 52 1-(4-Methoxy-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid (61). A solution of 1-(4-methoxy-phenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester (50, 2.0 g, 6.4 mmol), 1-(4-iodo-phenyl)-piperidin-2-one (60, 2.5 g, 8.3 mmol, 1.3 equiv), and K2CO3 (325 mesh powder, 1.80 g, 12.8 mmol, 2.0 equiv) in DMSO (35 mL) was degassed three times under a steady nitrogen stream before being treated with CuI (244 mg, 1.3 mmol, 20% equiv) and 8-hydroxyquinoline (189 mg, 1.3 mmol, 20% equiv) under N2. The resulting reaction mixture was subsequently degassed three times again before being warmed up to 125 C. for 10 h. When HPLC showed the coupling reaction was complete, the reaction mixture was cooled down to 5-10 C. before being treated with 14% NH4OH aqueous solution (30 mL) and ethyl acetate (30 mL) at 5-10 C. with good stirring. The mixture was stirred for an additional 1 h at 5-10 C. The mixture was filtered through a Celite bed and the Celite bed was washed with water (2*10 mL). The two layers of the filtrates were separated, and the aqueous layer was acidified by 1 N aqueous HCl solution to pH=4. The mixture was subsequently stirred at 5-10 C. for an additional 1 h. The solids were collected by filtration, washed with water (2*5 mL), and dried in vacuo at 40-45 C. for 12 h to afford the crude desired 1-(4-methoxy-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid (61, 2.0 g, 2.95 g theoretical, 68%), which was found to be pure enough to do the following reaction without further purification. For 61, CIMS m/z 461 (M++H, C25H24N4O5)., 385425-15-0

As the paragraph descriping shows that 385425-15-0 is playing an increasingly important role.

Reference£º
Patent; Zhou, Jiacheng; Oh, Lynette M.; Ma, Philip; Li, Hui-Yin; Confalone, Pasquale; US2003/181466; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

166815-96-9, tert-Butyl 4-((tosyloxy)methyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-hydroxy-4-(4-bromo-2-fiuoroanilino)-6-methoxyquinazoline (100 g) and potassium carbonate (113.8 g) were suspended in iV-methylpyrrolidinone (1070 ml) and stirred for 10 minutes prior to the addition of l-(fert-butoxycarbonyl)-4-(4- methylphenylsulfonyloxymethyl)piperidine (152.2 g). The reaction mixture was then heated to 950C for 4 hours before being cooled back to 7O0C. Water (1922 ml) was then added over a period of 15 minutes. The reaction mixture was held at 730C for 1 hour before being cooled to 4O0C and the product isolated by filtration. The product was washed with water (549 ml), slurry washed with ethyl acetate (549 ml) at 5O0C for 1 hour and then washed with ethyl acetate (275 ml) and dried at 500C. Yield: 137 g, 86%; NMR Spectrum (DMSOd6) 1.15-1.3 (m, 2H), 1.46 (s, 9H), 1.8 (d, 2H), 2.0-2.1 (m, IH), 2.65-2.9 (m, 2H) 3.95 (s, 3H), 4.02 (br s, 2H), 4.05 (d, 2H), 7.2 (s, IH), 7.48 (d, IH), 7.55 (t, IH), 7.65 (d, IH), 7.8 (d, IH), 8.35 (s, IH), 9.55 (br s, IH); Mass Spectrum [ESI] (M+H)+ = 561-563.; 7-hydroxy-4-(4-bromo-2-fluoroanilino)-6-methoxyquinazoline (5.0 g) and potassium carbonate (5.7 g) were suspended in N-methylpyrrolidinone (53.5ml) and stirred for 10 minutes. l-(tert-butoxycarbonyl)-4-(4-methylphenylsulfonyloxymethyl)pirhoeridine (7.6 g) was then added. The reaction mixture was then heated to 950C and stirred at that temperature for 3.5 hours before being cooled back to 7O0C. Isopropanol (25 ml) was added and then water (75 ml) was added over a period of 15 minutes. The reaction mixture was then stirred at 730C for 1 hour before cooling to 4O0C and isolation of the product by filtration. The product was washed with water (27.4 ml) and dried at 5O0C. Yield: 6.72 g, 87.2%; NMR Spectrum (DMSOd6) 1.15-1.3 (m, 2H), 1.46 (s, 9H), 1.8 (d, 2H), 2.0-2.1 (m, IH), 2.65-2.9 (m, 2H) 3.95 (s, 3H), 4.02 (br s, 2H), 4.05 (d, 2H), 7.2 (s, IH), 7.48 (d, IH), 7.55 (t, IH), 7.65 (d, IH), 7.8 (d, IH), 8.35 (s, IH), 9.55 (br s, IH); Mass Spectrum [ESI] (M+H)+ = 561-563.

166815-96-9, The synthetic route of 166815-96-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/36713; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem