Category: 10242-10-1

10242-10-1, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 10242-10-1, name is 5-Chlorobenzofuran-2-carboxylic acid. In an article£¬Which mentioned a new discovery about 10242-10-1

Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors

The development of reliable relationships between in vivo target engagement, pharmacodynamic activity, and efficacy in chronic disease models is beneficial for enabling hypothesis-driven drug discovery and facilitating the development of patient-focused candidate selection criteria. Toward those ends, osmotic infusion pumps can be useful for overcoming limitations in the PK properties of proof-of-concept (POC) compounds to accelerate the development of such relationships. In this report, we describe the application of this strategy to the development of hydantoin-derived aggrecanase inhibitors (eg, 3) for the treatment of osteoarthiritis (OA). Potent, selective inhibitors were efficacious in both chemical and surgical models of OA when exposures were sustained in excess of 10 times the plasma IC50. The use of these data for establishing patient-focused candidate selection criteria is exemplified with the characterization of compound 8, which is projected to sustain the desired level of target engagement at a dose of 45 mg qd.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 10242-10-1 is helpful to your research. 10242-10-1

Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H3199O – PubChem

10242-10-1, 5-Chlorobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-chlorobenzofuran-2-carboxylic acid (0.274 g, 1.4 mmol, 1.5 equiv) in DMF (10 mL) was added DIPEA (0.5 mL, 2.7 mmol, 3.0 equiv) followed by the addition of HATU (0.706 g, 1.8 mmol, 2.0 equiv) and the resultant reaction mixture was stirred for 30 min. Trans-tert-butyl (4-aminocyclohexyl)carbamate (0.200 g, 0.90 mmol, 1.0 equiv) was added and the reaction mixture was allowed to stir overnight at RT and the resulting precipitate was filtered off and washed with excess methanol to obtain trans-tert-butyl (4-(5-chlorobenzofuran-2-carboxamido)cyclohexyl)carbamate (350 mg, 64% Yield) as an off-white solid. LCMS: 393 [M+H]+., 10242-10-1

10242-10-1 5-Chlorobenzofuran-2-carboxylic acid 937838, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Praxis Biotech LLC; BERNALES, Sebastian; DELGADO OYARZO, Luz Marina; NUNEZ VASQUEZ, Gonzalo Esteban; URETA DIAZ, Gonzalo Andres; PUJALA, Brahmam; PANPATIL, Dayanand; BHATT, Bhawana; CHAKRAVARTY, Sarvajit; US2019/177310; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

10242-10-1, 5-Chlorobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: (5-Chloro-7-fluoro-1H-indole-2-yl)-carboxylic acid (5a) (50 mg, 0.23 mmol), N,N-diisopropylethylamine (82 mul, 0.47 mmol) and 2-(7-Aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (89 mg, 0.23 mmol) were dissolved in 550 mul N,N-dimethylformamide. After stirring for 10 min 4-methyl-piperazin 6a (26 mul, 0.23 mmol) was added and the reaction mixture was stirred for 16 h at 20 C. The solvent was evaporated under reduced pressure and the crude product was purified using chromatography method P1, yielding 37 mg (53%) of the title compound., 10242-10-1

As the paragraph descriping shows that 10242-10-1 is playing an increasingly important role.

Reference£º
Article; Engelhardt, Harald; De Esch, Iwan J.P.; Kuhn, Daniel; Smits, Rogier A.; Zuiderveld, Obbe P.; Dobler, Julia; Mayer, Moriz; Lips, Sebastian; Arnhof, Heribert; Scharn, Dirk; Haaksma, Eric E.J.; Leurs, Rob; European Journal of Medicinal Chemistry; vol. 54; (2012); p. 660 – 668;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10242-10-1,5-Chlorobenzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

5-chlorobenzofuran-2-carboxylic acid (500 mg, 2.5 mmol) was added to thionyl chloride (5 mL) and heated under reflux for 2 hrs. Solvent was removed under reduced pressure to obtain a white solid, which then used in the next reaction without further purification (510 mg). 1H NMR (400 MHz, Chloroform-d) delta 7.76 (d, J=0.9 Hz, 1H), 7.72 (dd, J=2.0, 0.7 Hz, 1H), 7.56-7.48 (m, 2H).

10242-10-1, As the paragraph descriping shows that 10242-10-1 is playing an increasingly important role.

Reference£º
Patent; The University of North Carolina at Chapel Hill; Juliano, Rudolph L.; Kreda, Silvia M.; Wang, Ling; Ming, Xin; James, Lindsey Ingerman; Ariyarathna, Ranathunga Arachchillage Yamuna Kumari; (53 pag.)US2019/343868; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10242-10-1,5-Chlorobenzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 4-aminopiperidine-l-carboxylate (1.02 g, 5.10 mmol, 1.0 equiv) in DMF (10 mL) was added 5-chlorobenzofuran-2 -carboxylic acid (1 .0 g, 5.1 mmol, 1.0 equiv) and HATU (3.800 g, 10.02 mmol, 2.0 equiv) at RT. The resulting reaction mixture was stirred for 10 minutes and DIPEA (2.5 mL, 15.00 mmol, 3.00 equiv) was added. The reaction mixture was allowed to stir at RT for overnight. Product formation was confirmed by LCMS. The reaction mixture was diluted with water (50 mL) and extracted with ethyl acetate (100 mL c 2). Combined organic extracts were washed with water (20 mL *4), dried over anhydrous NaaSOr and concentrated. The crude product obtained was treated w ith ether- hexane (50:50) to obtain tert-butyl 4-(5-chlorobenzofuran-2-carboxaniido)piperidine-1 – carboxylate (0.800 g, 43% yield) as an off-white solid. LCMS: 379.2 [M+H] 2

10242-10-1, The synthetic route of 10242-10-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRAXIS BIOTECH LLC; DELGADO OYARZO, Luz Marina; URETA DIAZ, Gonzalo Andres; PUJALA, Brahmam; PANPATIL, Dayanand; BERNALES, Sebastian; CHAKRAVARTY, Sarvajit; (0 pag.)WO2019/236710; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

10242-10-1, 5-Chlorobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Toa solution of (3S, 3aS) -3- (aminomethyl) -8- (3-oxomorpholino) -3, 3a, 4,5-tetrahydro-1H-benzo [b] oxazolo [3, 4-d] [1, 4] oxazepin-1-one (30 mg, 0.090mmol) and 5-chlorobenzofuran-2-carboxylic acid (20 mg, 0.10 mmol) indichloromethane (10 mL) were added 4-dimethylaminopyridine (28 mg, 0.23 mmol)and 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide hydrochloride (35 mg, 0.18mmol) . The mixture was reacted at rt for 10 hours. The reaction mixture wasconcentrated in vacuo to remove the solvent, and the residue was purified bysilica gel chromatography eluted with PE/EtOAc (V/V) 1/4 to give the titlecompound as a white solid (11 mg, 24) . The compound was characterized by thefollowing spectroscopic data: MS (ESI, pos. ion) m/z: 512.2 (M+1) and 1HNMR (400 MHz, CDCl3) : delta 7.68 (d, J 1.8 Hz, 1H) , 7.53 -7.40 (m,4H) , 7.15 (t, J 6.3 Hz, 1H) , 7.12 (d, J 2.3 Hz, 1H) , 7.02 (dd, J 8.6,2.4 Hz, 1H) , 4.55 -4.47 (m, 2H) , 4.33 (s, 2H) , 4.05 -4.00 (m, 2H) , 3.89 -3.69(m, 6H) , 2.35 -2.14 (m, 2H) ., 10242-10-1

10242-10-1 5-Chlorobenzofuran-2-carboxylic acid 937838, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZUO, Yinglin; ZHANG, Yingjun; WANG, Xiaojun; ZHANG, Jin; WEN, Liang; CHENG, Guanjun; WO2015/110024; (2015); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10242-10-1,5-Chlorobenzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of N-(l-aminopiperidin-4-yl)-2-(4-chloro-3-fluorophenoxy) acetamide (0.100 g, 0.33 mmol, 1.0 equiv) in DMF (5 mL) was added 5-chlorobenzofuran-2-carboxylic acid (0.065 g, 0.33 mmol, 1.0 equiv) and HATU (0.250 g, 0.66 mmol, 2.0 equiv) at RT. The resulting reaction mixture was stirred for 10 minutes DIPEA (0.28 mL, 0.99 mmol, 3.0 equiv) was added. The reaction mixture was allowed to stir at RT overnight. Product formation was confirmed by LCMS. The reaction mixture was diluted with water (25 mL) and extracted with ethyl acetate (50 mL x 2). Combined organic layer was washed with water (20 mL x 4), dried over anhydrous NaaSOr and concentrated. The crude product was purified by reverse phase HPLC to obtain 5-chloro-N-(4-(2-(4-chloro-3-fluorophenoxy)acetamido)piperidin-l- yl)benzofuran-2-carboxamide (Compound 2 – 20 mg, 12 % yield) as an off white solid. LCMS 480 i H | +; H NMR (400MHz, DMSG-de) d 9 79 (s, 1 H), 8.08 (d, J= 7.5 Hz, 1 H), 7.86 (s, 1 H), 7.70 (d, J= 9.2 Hz, 1 H), 7.54 – 7.38 (m, 3 H), 7.08 (d, J= 8 8 Hz, 1 H), 6.86 (d, .7= 11.8 Hz, 1 H), 4.53 (s, 2 H), 3.66 (br. s., I H), 2.99 (br. s., 2 H), 2.78 (br. s, 2 H), 1.75 (br. s., 2 H), 1.66 (br. s., 2 H)

10242-10-1, 10242-10-1 5-Chlorobenzofuran-2-carboxylic acid 937838, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; PRAXIS BIOTECH LLC; DELGADO OYARZO, Luz Marina; URETA DIAZ, Gonzalo Andres; PUJALA, Brahmam; PANPATIL, Dayanand; BERNALES, Sebastian; CHAKRAVARTY, Sarvajit; (0 pag.)WO2019/236710; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

10242-10-1, 5-Chlorobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 33 (General Procedure (A)) (5-Chlorobenzofuran-2-yl)-((S)-2-((pyrrolidin-1-yl)methyl)pyrrolidin-1-yl)methanone 400 mg of the title compound were synthesised as described for (E)-3-(4-bromophenyl)-1-((S)-2-((pyrrolidin-1-yl)methyl)pyrrolidin-1-yl)propenone, using 5-chlorobenzo[b]furane-2-carboxylic acid instead of (E)-4-bromocinnamic acid. 1H-NMR (CDCl3, 2 sets of signals) delta 1.70 (m, 4 H); 1.85-2.90 (m, 10 H); 3.65-4.10 (m, 2 H); 4.50 and 4.85(both m, together 1 H); 7.30-7.50 (m, 3 H); 7.65 (s, 1 H). HPLC method A: elution at 8.62 min. MS: calc. for [M+H]+: 333; found: 333.

10242-10-1, The synthetic route of 10242-10-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Peschke, Bernd; Pettersson, Ingrid; US2003/195190; (2003); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10242-10-1,5-Chlorobenzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

10242-10-1, LiAlH4 (0.12 g, 3.1 mmol) was weighed into a flask, THF (15.0 mL) was added,After stirring at 0 C for 10 minutes, 1-g (0.61 g, 3.1 mmol) was added, and the mixture was stirred at 0 C for 20 minutes.The reaction was quenched by adding H2O (5 mL) dropwise, diluted with ethyl acetate, filtered, washed with ethyl acetate, concentrated by rotary distillation and purified by silica gel column chromatography to give the product of formula 2-g.

10242-10-1 5-Chlorobenzofuran-2-carboxylic acid 937838, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Chinese Academy Of Sciences Chemical Institute; Shi Yian; Li Zequan; Tian Hua; (29 pag.)CN106588952; (2017); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

10242-10-1, 5-Chlorobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Synthesis Example 69 (0667) (5-Chloro-benzofuran-2-yl)methanol (0668) To a tetrahydrofuran solution (12 mL) of 5-chlorobenzofuran-2-carboxylic acid (620 mg, 3.15 mmol), borane-tetrahydrofuran complex (7.88 mL, 7.88 mmol, tetrahydrofuran solution) was added at 0 C. and the resultant solution was stirred at room temperature for 3 hours, at 60 C. for 1 day, and at room temperature for 1 day. After completion of the reaction, concentration under reduced pressure was carried out three times with adding methanol to the reaction solution and the concentrated solution was purified by silica gel column chromatography (hexane/ethyl acetate=3/1?1/1 (v/v)) to obtain the title compound (268 mg, yield 47%).

10242-10-1, The synthetic route of 10242-10-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NISSAN CHEMICAL INDUSTRIES, LTD.; Saito, Noriko; Egi, Jun; Nagai, Hiroshi; Ueno, Megumi; Shintani, Yusuke; Inaba, Yusuke; Adachi, Michiaki; Hirai, Yuichi; Kawazu, Takeshi; Yasutake, Koichi; Takahashi, Daiki; (220 pag.)US9403798; (2016); B2;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem