Analyzing the synthesis route of 2510-36-3

The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 3,5-dimethylisoxazole-4-carboxylic acid (8c, 2.0 g, 14.17 mmol) in THF (50 mL) was added N,O-dimethylhydroxylamine hydrochloride (4.25 g, 43.61 mmol), HATU (16.6 g, 43.66 mmol) and DIPA (36.9 g, 118.98 mmol). The reaction mixture was stirred at room temperature overnight. After the reaction was completed, water was added and the aqueous layer was extracted with ethyl acetate (50 mL ¡Á 4). The organic layer was dried over sodium sulfate, and concentrated. The crude product was chromatographed on silica gel to give compound 9c (2.2 g, 84%)., 2510-36-3

The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chang, Shaohua; Guo, Zhuang; Li, Xue; Sun, Tianwen; Wang, Hai; Wang, Xiaowei; Wang, Yazhou; Xu, Guofeng; Xu, Tianwei; Yu, Wenying; Yu, Zhuangzhuang; Zhang, Yan; Zhao, Liwen; European Journal of Medicinal Chemistry; vol. 198; (2020);,
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Downstream synthetic route of 2510-36-3

As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

2510-36-3, 3,5-Dimethylisoxasole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 1f (R1=4-Cl, R2=6-Br, X=O) (70 mg, 0.16 mmol),3,5-Dimethylisoxazole-4-carboxylic acid (31 mg, 0.22 mmol),1-hydroxybenzotriazole (HOBt) (30 mg, 0.22 mmol) and1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI) (42 mg, 0.22 mmol),in room temperature,The reaction was carried out in anhydrous dichloromethane (5 ml) for 12 hours.Wash with saturated brine,Extracted with dichloromethane,Dry over anhydrous sodium sulfate,The organic layer was separated by silica gel column chromatography.Obtained a pale yellow powder of 37 mg.The yield was 41%., 2510-36-3

As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; Sun Yat-sen University; Zhang Hui; Bai Chuan; Pan Ting; Wu Liyang; (17 pag.)CN108610301; (2018); A;,
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New learning discoveries about 2510-36-3

As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

2-(2-(3,5-dimethylisoxazole-4-carbonyl)benzofuran-5-yl)-N-((2,4-dimethylphenyl)(phenyl)methyl) acetamidea) methyl 3,5-dimethylisoxazol -4-carboxylateTo a solution of 3,5-dimethylisoxazole-4-carboxylic acid (9.2 g, 65.2 mmol) in MeOH (50 mL) was added SOCI2 (15.3 g, 130.4 mmol) very slowly. The reaction mixture was heated to 70 C overnight. The reaction mixture was then cooled to rt, concentrated, and purified by column chromatography (10% EtO Ac/petroleum ether) to afford the title compound (9.0 g, 89%). LCMS- Pl : 156 [M+H]+; Rt: 1.404 min., 2510-36-3

As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; TEMPERO PHARMACEUTICALS, INC.; BALOGLU, Erkan; BOHNERT, Gary, J.; GHOSH, Shomir; LOBERA, Mercedes; SCHMIDT, Darby, R.; SUNG, Leonard; WO2013/19682; (2013); A1;,
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Analyzing the synthesis route of 2510-36-3

2510-36-3, The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

General procedure: The aldehyde (0.8 equivalent) and amine (0.7 equivalent) were dissolved in methanol (2.0 mL) and stirred for two to 3 h depending upon the starting material. The acid (100 mg, 1 equivalent) and isocyanide (0.7 equivalent) were added in the reaction mixture and further stirred. The reaction mixture was monitored using TLC analysis.Water (4 mL) was added upon completion of the reaction.The resulted solid was filtered off and dissolved in ethyl acetate(10 mL), washed with water (2 3 mL) and dried over sodium sulphate. The crude product was purified using silica gel column chromatography. The ethyl acetate:hexane (6:4) solvent system was used for the purification of these compounds.

2510-36-3, The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Makane, Vitthal B.; Krishna, Vagolu Siva; Krishna, E. Vamshi; Shukla, Manjulika; Mahizhaveni; Misra, Sunil; Chopra, Sidharth; Sriram, Dharmarajan; Dusthackeer, V.N. Azger; Rode, Haridas B.; European Journal of Medicinal Chemistry; vol. 164; (2019); p. 665 – 677;,
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New learning discoveries about 2510-36-3

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 2; N-[(3,5-dimethylisoxazol-4-yl)carbonyl]-3-{5-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]thiophen-2-yl}-L-alanine; O-benzotriazol-1-yl-N,N,N’,N’-tetramethyluronium tetrafluoroborate (268 mg, 0.83 mmol), 4-methylmorpholine (0.084 ml, 0.76 mmol) and 3,5-dimethylisoxazole-4-carboxylic acid (98 mg, 0.70 mmol) were added under an argon atmosphere to a stirred solution of methyl 3-{5-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]thiophen-2-yl}-L-alaninate (250 mg, 0.70 mmol) dissolved in DMF (2.5 mL). The resulting solution was stirred at 25 C. for 2 hours. Then NaOH 6N (0.464 ml, 2.78 mmol) was added to the stirred mixture. The resulting solution was stirred at 25 C. for 1 hour. The reaction mixture was purified by C18 reverse phase chromatography (basic conditions). The fractions containing the desired compound were evaporated to dryness to afford the title compound as a beige solid (157 mg, 48.2%); Mass spectrum [M+H]+=467; 1H NMR Spectrum (DMSOd6) 1.70-1.78 (m, 2H), 1.81-1.90 (m, 2H), 2.18 (s, 3H), 2.39 (s, 3H), 2.45 (t, 2H), 2.60 (t, 2H), 2.70 (t, 2H), 3.15 (dd, 1H), 3.20-3.26 (m, 2H), 3.32 (dd partially hidden by H2O, 1H), 4.49 (ddd, 1H), 6.23 (d, 1H), 6.42 (bs, 1H), 6.64 (d, 1H), 6.71 (d, 1H), 7.03 (d, 1H), 8.27 (d, 1H).

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; US2008/255183; (2008); A1;,
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New learning discoveries about 2510-36-3

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

A vial was charged with 3-fluoro-4- [[(3S)-3-methyl- 1,1 -dioxo-6-phenyl-thiazinan-2- ylimethyllaniline hydrochloride (75 mg, 0.19 mmol), 3,5-dimethylisoxazole-4-carboxylic acid (41 mg, 0.29 mmol), triethylamine (0.14 mL, 0.97 mmol) and N,N-dimethylformamide (1 mL), followed by O-(7-azabenzotriazol- 1 -yl)-N,N,N?,N?-tetramethyluronium hexafluorophosphate (92 mg, 0.23 mmol) and the reaction was stirred at room temperature for 2 hours. The reaction was then partitioned between dichloromethane and saturated sodium bicarbonate in water. The organic layer was separated, concentrated and purified by preparative HPLC to give N-[3-fluoro- 4- [[(3S)-3-methyl- 1,1 -dioxo-6-phenyl-thiazinan-2-yllmethyllphenyll -3,5 -dimethyl-isoxazole-4- carboxamide Stereoisomer A (23.6 mg, 0.050 mmol, 26% yield). ?H NMR (400 MHz, DMSO)o 10.22 – 10.18 (s, 1H), 7.67 – 7.60 (m, 1H), 7.51 – 7.44 (m, 3H), 7.44 – 7.34 (m, 4H), 4.54 – 4.46 (m, 2H), 4.39 – 4.33 (m, 1H), 4.17 – 4.07 (m, 1H), 2.57 – 2.52 (s, 3H), 2.47 – 2.39 (m, 1H),2.34- 2.29 (s, 3H), 2.16 -2.06 (m, 1H), 1.90- 1.75 (m, 1H), 1.71 – 1.61 (m, 1H), 1.13 – 1.07 (d, J = 6.8 Hz, 3H); LCMS [M+1j = 472.2.

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; FAUBER, Benjamin; RENE, Olivier; WO2014/202741; (2014); A1;,
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Downstream synthetic route of 2510-36-3

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

2510-36-3, 3,5-Dimethylisoxasole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 6-(5-aminomethyl-pyridin-3-yl)-1-methyl-3,4-dihydro-1H-quinolin-2-one (example 36, 0.047 g, 0.177 mmol) in DMF (1 mL) were added 3,5-dimethylisoxazole-4-carboxylic acid (0.037 g, 0.266 mmol) and TBTU (0.063 g, 0.195 mmol) followed by Huenig’s base (0.048 g, 0.372 mmol) and the reaction mixture was stirred at room temperature over night. The mixture was purified directly by reverse phase HPLC on a Gemini-NX column, eluting with a 20 to 98% MeOH-H2O (0.05% TEA) gradient to give the title compound (0.041 g, 59%) as a colorless solid. MS: 391.3 (M+H+)

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; Aebi, Johannes; Amrein, Kurt; Hornsperger, Benoit; Knust, Henner; Kuhn, Bernd; Liu, Yongfu; Maerki, Hans P.; Mayweg, Alexander V.; Mohr, Peter; Tan, Xuefei; Zhou, Mingwei; US2013/72679; (2013); A1;,
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Brief introduction of 2510-36-3

The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

2510-36-3, 3,5-Dimethylisoxasole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 3,5-dimethylisoxazole-4-carboxylic acid (0.3 mmol), oxalyl chloride (125 ? ) and catalytic amount of DMF was stirred at room temperature for 2h. After evaporating to dryness, the residual crude acid chloride was dissolved in 2 mL DCM. To the solution was added 3 (26 mg, 0.1 mmol) and DIEA (52 ??^). After stirring overnight at room temperature, the reaction mixture was worked up with aq. NaHCOs/DCM. DCM phase was washed with brine and concentrated to dryness. The residue was dissolved in 2 mL THF/MeOH/H20 (5:4: 1) and stirred with IN NaOH (100 ??) at room temperature for 2h before worked up with EA/ aq. NaHC03. Silica gel flash chromatography furnished (3,5-dimethylisoxazol-4-yl)-N-{3-fluoro-4- [l-methyl-3-(trifluoromethyl)pyrazol-5-yl]phenyl}carboxamide 92 (16 mg, yield: 41.9%, purity >95%) as a colorless gel. MS (ESI) [M+H]+ 383.1., 2510-36-3

The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CALCIMEDICA, INC.; CAO, Jianguo; WHITTEN, Jeffrey, P.; WANG, Zhijun; ROGERS, Evan; GREY, Jonathan; WO2013/59666; (2013); A1;,
Isoxazole – Wikipedia
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Downstream synthetic route of 2510-36-3

As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

2510-36-3, 3,5-Dimethylisoxasole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3,5-dimethylisoxazole-4-carboxylic acid (58 mg, 2.5 equiv.) in DMF (3 mL) was added D/PEA (202 uL, 7 equiv.), followed by TBTU (160 mg, 3 equiv.). The reaction mixture was stirred at RT for one hour, and then 4-[[4-(lH-pyrrolo[2,3-?]pyridin- 3-yl)-l-piperidyl]sulfonyl]aniline (59 mg, 1 equiv.) was added. The reaction mixture was stirred at RT for 30 min, and at 100 C for 2 h. The reaction mixture was cooled to RT, and the solvent was removed in vacuo. The residue was partitioned betweed EtOAc and water, organic phase was washed with brine, dried over Na2S04, filtered, and the solvent was removed in vacuo to yield the crude product. The crude product was purified by column chromatography, followed by preparative HPLC-MS to yield the expected product (11.5 mg). LCMS: MW (calc’d): 479.5; MS (ES+, m/z): 480.7 [M+H]+., 2510-36-3

As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; E-THERAPEUTICS PLC; JURKOVIC, Mihaela; LANDEK, Ivana Ozimec; POLJAK, Tanja; RO?CIC, Maja; STUBBERFIELD, Colin; VADLAMUDI, Srinivasamurthy; (228 pag.)WO2019/43372; (2019); A1;,
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Analyzing the synthesis route of 2510-36-3

2510-36-3, The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

INTERMEDIATE 34: (S)-dibenzyl 2-(2-(2-(benzyloxy)-2-oxoethoxy)-4-(5-((((R)-2-((R)-1 – (N-((3,5-dimethylisoxazole-4- carbonyl)oxy)formamido)propyl)heptanamido)methyl)carbamoyl)furan-2- yl)benzamido)succinate DI PEA (84 muIota, 0.482 mmol) was added to a solution containing (S)-dibenzyl 2-(2-(2- (benzyloxy)-2-oxoethoxy)-4-(5-((((R)-2-((R)-1 -(N- hydroxyformamido)propyl)heptanamido)methyl)carbamoyl)furan-2-yl)benzamido)succinate (150 mg, 0.161 mmol) and 3,5-dimethylisoxazole-4-carboxylic acid (24.96 mg, 0.177 mmol), and HATU (73.4 mg, 0.193 mmol) in DMF (1072 muIota). The resulting mixture was stirred for 2 days at RT. Purification of the crude reaction mixture by reverse phase HPLC afforded the title compound as a colorless solid. (98 mg, 52 % yield). MS (m/z) 1056.6 (M+H)+

2510-36-3, The synthetic route of 2510-36-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; DONATELLI, Carla A.; DOWDELL, Sarah E.; ELBAN, Mark; HILFIKER, Mark A.; HOANG, Tram H.; HOLT, Dennis Alan; MANNS, Sharada; MARCUS, Andrew; POTTEIGER, Craig; SHENJE, Raynold; WASHBURN, David G.; (364 pag.)WO2017/6296; (2017); A1;,
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