Day: October 30, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1188032-12-3,5-(3-Fluorophenyl)isoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

1188032-12-3, Example 126 Synthesis of 5-(3-Fluoro-phenyl)-isoxazole-3-carboxylic acid {2-oxo-2-[4-(3-trifluoromethyl-phenoxy)-piperidin-1-yl]-ethyl}-amide DIPEA (131 mg, 1.0 mmol) was added to a stirred solution of 5-(3-fluoro-phenyl)-isoxazole-3-carboxylic acid (60 mg, 0.29 mmol) (prepared by the method used for the synthesis of Intermediate 25, starting from 3′-fluoroacetophenone) in DMF (2 mL) followed by HOBt (41 mg, 0.3 mmol) and EDCI.HCl (58 mg, 0.3 mmol). After 2 minutes 2-amino-1-[4-(3-trifluoromethyl-phenoxy)-piperidin-1-yl]-ethanone hydrochloride (125 mg, 0.37 mmol) (prepared according to Step 1 and 5 of the General Scheme) was added to the reaction mixture and stirring was continued at ambient temperature overnight. The reaction mixture was diluted with cold water, extracted with ethyl acetate, dried over sodium sulfate and concentrated under reduced pressure. Purification by recrystallisation from methanol afforded 84 mg (59.15% Yield) of 5-(3-fluoro-phenyl)-isoxazole-3-carboxylic acid {2-oxo-2-[4-(3-trifluoromethyl-phenoxy)-piperidin-1-yl]-ethyl}-amide. LC/MS [M+H]+: 492, 70.25%. 1H NMR (300 MHz, DMSO-d6): delta8.6 (t, 1H), 7.8 (m, 2H), 7.5 (m, 3H), 7.24 (m, 4H), 4.7 (m, 1H), 4.2 (d, 2H), 3.9 (m, 1H), 3.7 (m, 1H), 3.4 (m, 2H), 2.0 (m, 2H), 1.6 (m, 2H).

1188032-12-3 5-(3-Fluorophenyl)isoxazole-3-carboxylic acid 66591590, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; Forest Laboratories Holdings Limited; US2009/239810; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

33282-23-4, 5-(4-Bromophenyl)isoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of carboxylic acid 21-29 (1 equiv) in anhydrous CH2Cl2 were successively added HBTU (1.5 equiv), HOBt (0.5 equiv) and DIPEA (2 equiv). The mixture was stirred for 45 min at room temperature. Then, the appropriate amine (1.1 equiv) was introduced and the stirring was continued for 24 h. At the end of the reaction, the mixture was filtered off and the filtrate was successively washed with saturated aqueous NaHCO3 solution, 1N aqueous HCl and distilled water. The organic layer was dried over MgSO4 and was concentrated in vacuo. The resulting residue was purified by TLC (cyclohexane/AcOEt, 7:3) and crystallized in absolute EtOH to give carboxamide 30-48.

33282-23-4, The synthetic route of 33282-23-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Andrzejak, Virginie; Muccioli, Giulio G.; Body-Malapel, Mathilde; El Bakali, Jamal; Djouina, Madjid; Renault, Nicolas; Chavatte, Philippe; Desreumaux, Pierre; Lambert, Didier M.; Millet, Regis; Bioorganic and Medicinal Chemistry; vol. 19; 12; (2011); p. 3777 – 3786;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

21169-71-1, Isoxazole-5-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Isoxazole-5-carboxylic acid (0.500 g, 4.4 mmol) was dissolved in a solution of hydrochloric acid in ethanol (5 M) and refluxed for 5 hours. The mixture was concentrated under reduced pressure giving isoxazole-5-carboxylic acid ethyl ester, which was used immediately in the following step.

21169-71-1, As the paragraph descriping shows that 21169-71-1 is playing an increasingly important role.

Reference£º
Patent; AKZO NOBEL N.V.; WO2005/102998; (2005); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1072-67-9,5-Methylisoxazol-3-amine,as a common compound, the synthetic route is as follows.

3-amino-5-methylisooxazole (326 mg, 3.3 mmol) was dissolved in dichloromethane (6.5 mL), and ice-cooled. Thiophosgene (0.278 mL, 3.3×1.1 mmol) and sodium carbonate aqueous solution (769 mg, 3.3×2.2 mmol, 4 mL) were added, and stirred at room temperature for 2.5 hours. After the reaction, chloroform was added and washed with the saturated sodium chloride solution, dried with magnesium sulfate and the solvent was distilled off. The obtained residue was purified by Silica gel column chromatography (Biotage Isolera One, SANP 10 g, chloroform/methanol)to obtain title compound (yellow oil, 255 mg, 55.1%) ., 1072-67-9

As the paragraph descriping shows that 1072-67-9 is playing an increasingly important role.

Reference£º
Patent; CHIBA UNIVERSITY; YAKULTHONSHA COMPANY LIMITED; TAKAYAMA, HIROMITSU; YASOBU, NAOKO; KITAJIMA, MARIKO; YAEGASHI, TAKASHI; MATSUZAKI, TAKESHI; NAGAOKA, MASATO; HASHIMOTO, SHUSUKE; NISHIYAMA, HIROYUKI; SUGIMOTO, TAKUYA; ONO, MASAHIRO; (176 pag.)JP5829520; (2015); B2;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1750-42-1, Isoxazol-3-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of 1 mmol aldehyde, 3 volume of acetonitrile and 1 equivalent volume of aminewere added to 0.6 equivalent of quinoline derivatives and 1% (v/v) formic acid. The reaction mixturewas stirred at higher temperature (75 C). The reaction was monitored by TLC (eluent: hexaneisomeric mixture:acetone). If the product precipitated, it was filtered, washed with hexane, and dried.If the reaction mixture was homogeneous, it was evaporated to dryness and was purified by columnchromatography (eluent: hexane:acetone from 20:1 to 4:1, v/v). The crude product was crystallizedfrom hexane/ethyl-acetate. The molecular structures were determined by means of 1D and 2D-NMRtechnologies (see Supplementary Materials), 1750-42-1

Big data shows that 1750-42-1 is playing an increasingly important role.

Reference£º
Article; Kanizsai, Ivan; Madacsi, Ramona; Hackler, Laszlo; Gyuris, Mario; Szebeni, Gabor J.; Huzian, Orsolya; Puskas, Laszlo G.; Molecules; vol. 23; 8; (2018);,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.19788-37-5,4-(Chloromethyl)-3,5-dimethylisoxazole,as a common compound, the synthetic route is as follows.

To a stirred solution of 4-Hydroxy-2,6-dimethyl-benzoic acid methyl ester (12) (100 mg, 0.556 mmol) in DMF (2 mL), K2C03 (153 mg, 1.111 mmol) and 4-Chloromethyl-3,5- dimethyl-isoxazole (4) (0.07 mL, 0.556 mmol) were added and the reaction was stirred at RT for 16 hours. The reaction mixture was diluted with ethyl acetate, washed with water and brine, dried over sodium sulfate and concentrated. The crude was purified by column chromatography (silica, gradient: 20-30% EtOAc in Hexane) to afford the Intermediate 13 130 mg, 80%) as off white solid.

19788-37-5, The synthetic route of 19788-37-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THE BROAD INSTITUTE, INC.; THE GENERAL HOSPITAL CORPORATION; INSTITUTO CARLOS SLIM DE LA SALUD; BURNS, Sean, M.; WAGNER, Bridget, K.; VETERE, Amedeo; (189 pag.)WO2018/175324; (2018); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 0¡ã C. solution of (054) and 5-methyl-isoxazole-3-carboxylic acid (009) (127 mg, 1.0 mmol), HOBT (135 mg, 1.0 mmol) and HBTU (350 mg, 1.0 mmol) in tetrahydrofuran (100 mL) was added a solution of N,N-diisopropylethylamine (0.5 mL) in tetrahydrofuran (2 mL). The mixture was stirred at room temperature for 5 hours. It was then diluted with ethyl acetate (200 mL) and washed with saturated aqueous sodium bicarbonate (2.x.10 mL) and brine (10 mL). The organic layers were dried over sodium sulfate and filtered through Celite-545, the solvents were removed under reduced pressure and the residue was purified by HPLC (aqueous ammonium acetate and acetonitrile) to provide (055) (40 mg) which was characterized by LC/MS (LCRS (MH) m/z: 576.27); >80percent proteasome CT-L inhibition at 20 mg/kg PO.

3405-77-4, As the paragraph descriping shows that 3405-77-4 is playing an increasingly important role.

Reference£º
Patent; Proteolix, Inc.; US2007/105786; (2007); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

42831-50-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.42831-50-5,5-Methylisoxazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

The 5-methylisoxazole-4-carboxylic acid (1) (1 g, 7.86 mmol) inSOCl2 (3 mL) was heated at 50 C until compound 1 disappeared inTLC. After reaction was terminated, the mixture was cooled toambient temperature and solvent was evaporated under reducedpressure. 5-methylisoxazole-4-carbonyl chloride, a crude yellow oil(2) (96%)was used for the next step without additional purification;1H NMR (400 MHz, DMSO) d 8.77 (1H, s), 2.64 (3H, s).

The synthetic route of 42831-50-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Im, Daseul; Jung, Kyungjin; Yang, Songyi; Aman, Waqar; Hah, Jung-Mi; European Journal of Medicinal Chemistry; vol. 102; (2015); p. 600 – 610;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1072-67-9, 5-Methylisoxazol-3-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 45 N-isoxazolyl enaminone 1 (1.0mmol, 0.800g), aryl glyoxal monohydrates 2 (1.0mmol, 0.552g) and 4-amino-3-methyl-5-styrylisoxazoles 320h,23 (1.0mmol, 0.727g) in 4.5mL 46 water and 18 AcOH 0.5mL was refluxed at 100C for 1h. After completion of the reaction (monitored by TLC), the mixture was cooled to room temperature and poured into ice-cold water. The precipitate that formed was filtered off, washed with ice cold water and the crude product was purified by recrystallization from methanol to give pure bis-isoxazolyl amino dihydro-1H-indol-4(5H)-ones 42 4., 1072-67-9

As the paragraph descriping shows that 1072-67-9 is playing an increasingly important role.

Reference£º
Article; Nagi Reddy, Modugu; Praveen Kumar, Pittala; Tetrahedron Letters; vol. 58; 51; (2017); p. 4790 – 4795;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.19788-37-5,4-(Chloromethyl)-3,5-dimethylisoxazole,as a common compound, the synthetic route is as follows.

The allyl alcohol (20 mg, 0.035 mmol, Example 952) was dissolved in THF (1.00 rnL) and cooled to 0 C. Sodium hydride (60% dispersion; 840 rng, 0.350 rnmoi) was added and the mixture was stirred for 30 minutes. 4-(chloromethvi)-3.5-dimethviisoxazole (0022 mL. 0.175 rnrnoi) was then addedand the resulting mixture was stirred for 4,5 hours, Three more aliquol of reagents were added and the slurry was stirred at room temperature for 4.5 days. Thereaction was quenched with water and acidified with IN HC1 to pH5. The mixture was extracted with ethyl acetate (2 x 30 mL). The combined organiclayers were washed with brine (1 x 20 mL) and dried over magnesium sulfate.The crude material was purified by reverse-phase preparative HPLC using aPhenomenex Luna column. 10 micron. C8(2), 100 A. 150x 30mm. 0.1% TFA inCH3CN/H20, gradient 50% to 80% over 25 mm to provide (IS,3R,6],7R,8E)- 15Wspiro [naphthaIene 1,22-[2Oioxa[ 131 thia[ 1, i4ldiazatetracycio[1 47.203?6.0?924ipentacosa[8, 16,1 8,24itetrae nj-IS-one 13,13-dioxide (10mg, 0.015 mmol, 42 /yleId). ?HNMR (400MHz. CDCIs) oe 816 (s, 1 H), 7.71 (d, J=8.4 Hz, 1 H), 7.30 (s, I H), 7.18 (dd. 3=8.4, 2.3 Flz. I H), 7.09 (d. J::::2.3 Hz. I H), 695 (s, 2 Fl), 572 (dt, j:::16,O Hz, 4.7 Hz, I H),5-46 (dd, J=158, 8.4 Hz, I H), 4.65 (d, J=12. 1 Hz, 1 H), 4,13-426 (m, 1 H). 4.11 (s, 2 H), 4.03 (d, J:::12 1 Hz, I H). 396 (d, j:::14.7 Hz, 1 H), 3.59-3.71 (m, 2 H),3.19-3.30 (m, I H), 3.16 (d, J=14.3 Hz, 1 H), 2.86-2.98 (rn, 1 H), 2.66-2.84 (rn,H), 2.42-2.58 (in, 2 H), 2.40 (s, 3 H), 2.32 (s, 3 H), 2.08-2.22 (in, 3 H), 1.85-2.07(iii. 4 H), 1.75-185 (iii. 1 H), 1.65-1.74 (iii. 1 H), 1.50-1.64 (in. 1 H), 1.38-147(m. 2 H). rn/z (ESI, +ve ion) 680.3 (M+H)t, 19788-37-5

The synthetic route of 19788-37-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMGEN INC.; BROWN, Sean P.; BEDKE, David Karl; DEGRAFFENREID, Michael R.; FU, Jiasheng; LI, Zhihong; GONZALEZ LOPEZ DE TURISO, Felix; GONZALEZ BUENROSTRO, Ana; GRIBBLE, Jr., Michael W.; JOHNSON, Michael G.; KOHN, Todd J.; LI, Kexue; LI, Yunxiao; LIZARZABURU, Mike Elias; REW, Yosup; TAYGERLY, Joshua; WANG, Yingcai; YAN, Xuelei; YU, Ming; ZHU, Jiang; ZANCANELLA, Manuel; JIAO, Xian Yun; ZHU, Liusheng; WANG, Xianghong; MEDINA, Julio C.; DUQUETTE, Jason A.; HOUZE, Jonathan B.; VIMOLRATANA, Marc; CARDOZO, Mario G.; CHENG, Alan C.; (2426 pag.)WO2017/147410; (2017); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem