Tag: 78967-07-4

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78967-07-4,Mofezolac,as a common compound, the synthetic route is as follows.,78967-07-4

To a stirred solution of mofezolac (500 mg, 1.47 mmol) in dry CH2Cl2 (25 mL) , kept at 0C by an ice-bath, HOBt monohydrate (253 mg, 1.48 mmol) and EDC hydrochloride (303 mg, 1.58 mmol) were added. Separately a stirred solution of methyl 11-aminoundecanoate hydrochloride (370 mg, 1.38 mmol) in dry CH2Cl2 (13 mL) was mixed with DIEA (0.45 mL, 2.6 mmol) at room temperature. After 2h, this solution was dropwise added to the reaction mixture and stirred overnight at room temperature. Then, sat. aq. NaHCO3 was added and the aqueous solution extracted three times with EtOAc. The combined organic layers were dried over anhydrous Na2SO4, and the solvent distilled under reduced pressure. Column chromatography (silica gel; CHCls/MeOH = 5:5) of the crude residue afforded the product as a white solid (573 mg, 72% yield). NMR (300 MHz, CDCl3, delta) : 7.41- 7.26 (m, 2H aromatic protons) ; 7.25-7.13 (m, 2H aromatic protons) ; 6.93-6.71 (m, 4H aromatic protons), 5.80 (bs, 1H, exchanges with D20) , 3.82 (s, 3H, OC) , 3.80 ( s, 3H, OCH3) , 3.67 (s, 2H, CH2) , 3.65 (s, 3H, COOC) , 3.23- 3.21 (m, 2H, NHC), 2.31-2.26 (t, 2H, CCO) , 1.62-1.57 (m, 2H, CCH2CO) , 1.49-1.45 (m, 2H, CCH2NH) ; 1.25-1.10 (m, 12H, CH2) . ESI/MS m/z: C3iH4oN206 (M + Na)+: 559.

78967-07-4 Mofezolac 4237, aIsoxazoles compound, is more and more widely used in various.

Reference£º
Patent; UNIVERSITA’ DEGLI STUDI DI BARI “ALDO MORO”; SCILIMATI, Antonio; PERRONE, Maria Grazia; VITALE, Paola; (114 pag.)WO2017/187352; (2017); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

78967-07-4,78967-07-4, Mofezolac is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-Diisopropyl-N-ethylamine (DIEA, 0.215 mL, 1.237 mmol) andmethyl 5-aminopentanoate hydrochloride (6) (100 mg, 0.60 mmol)were solubilized in anhydrous CH2Cl2 (5 mL) and stirred at 0 C for1 h. Then, this solution was dropwise added to a stirred solution ofN,N’-dicyclohexylcarbodiimide (DCC, 170 mg, 0.825 mmol), 1-hydroxybenzotriazole monohydrate (HOBt H2O, 180 mg,1.05 mmol) and 2-[3,4-bis(4-methoxyphenyl)isoxazol-5-yl]aceticacid (mofezolac) (200 mg, 0.59 mmol) in anhydrous CH2Cl2 (20 mL)kept at 0 C. The reaction mixture was stirred for 19h at roomtemperature. Then, H2O was added and the aqueous solutionextracted with CH2Cl2. The combined organic layers were washedwith a sat. aqueous solution of K2CO3, dried over anhydrousNa2SO4, and the solvent was removed under reduced pressure.Column chromatography of the crude residue (silica gel; EtOAc/Hexane 3:7) allowed to isolated 8 (107 mg, 40% yield). FT-IR(KBr): 3458, 3089, 2987, 2948, 2849, 1737, 1652, 1609, 1562, 1516,1455, 1441, 1426, 1253, 1233, 1175, 1108, 1029, 1019, 949, 831,729 cm1. 1H NMR (300 MHz, CDCl3, delta): 7.41e7.37 (m, 2H, aromaticprotons); 7.17e7.14 (m, 2H, aromatic protons); 6.92e6.89 (m, 4H,aromatic protons); 5.95e5.90 (bs, 1H, NH: exchanges with D2O);3.83 (s, 3H, OCH3); 3.80 (s, 3H, OCH3); 3.67 (s, 2H, CH2COONH); 3.65(s, 3H, OCH3); 3.27 (q, 2H, J 6.9 Hz, NHCH2); 2.33 (t, 2H, J 6.9 Hz,CH2COO); 1.65e1.50 (m, 4H). 13C NMR (75 MHz, CDCl3, delta): 174.1,166.8, 162.8, 161.4, 160.8, 159.7, 131.2, 130.0, 121.6, 121.2, 117.8, 114.6,114.2, 55.5, 55.4, 39.7, 34.4, 33.6, 29.0, 22.2. ESI-MS: m/z (%):C25H28N2O6 (M + Na)+: 475.

78967-07-4 Mofezolac 4237, aIsoxazoles compound, is more and more widely used in various.

Reference£º
Article; Perrone, Maria Grazia; Vitale, Paola; Ferorelli, Savina; Boccarelli, Angelina; Coluccia, Mauro; Pannunzio, Alessandra; Campanella, Federica; Di Mauro, Giuseppe; Bonaccorso, Carmela; Fortuna, Cosimo G.; Scilimati, Antonio; European Journal of Medicinal Chemistry; vol. 141; (2017); p. 404 – 416;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78967-07-4,Mofezolac,as a common compound, the synthetic route is as follows.

Diisopropyl ethylamine (DIEA, 0.215 mL, 1.237 mmol) and methyl 5-aminopentanoate hydrochloride (100 mg, 0.60 mmol) were solubilized in dry CH2Cl2 (5 mL) and stirred at 0 C for 1h. Then, this solution was dropwise added to a stirred solution of N,N’-dicyclohexylcarbodiimide (DCC, 170 mg, 0.825 mmol), 1-hydroxybenzotriazole monohydrate (HOBt H2O, 180 mg, 1.05 mmol) and 2-[3,4-bis(4-methoxyphenyl)isoxazol-5-yl]acetic acid (mofezolac) (200 mg, 0.59 mmol) in dry CH2Cl2 (20 mL) kept at 0 C. The reaction was stirred for 19h at room temperature. Then, H2O was added and the aqueous solution extracted with CH2Cl2. The combined organic layers were washed with a sat. solution of K2CO3, dried over anhydrous Na2SO4, and the solvent was removed under reduced pressure. Column chromatography of the crude residue (silica gel; EtOAc/Hexane = 3:7) afforded the product as a solid (107 mg, 40% yield). FT- IR (KBr): 3458, 3089, 2987, 2948, 1737, 1652, 1609, 1562, 1516, 1455, 1441, 1426, 1253, 1233, 1175, 1108, 1029, 1019, 949, 831, 729 cnf1. NMR (300 MHz, CDCl3, delta) : 7.41-7.37 (m, 2H, aromatic protons), 7.17-7.14 (m, 2H, aromatic protons), 6.92-6.89 (m, 4H, aromatic protons), 5.9 (bs, 1H, NJJ: exchanges with D2O) , 3.83 (s, 3H, OCH3) , 3.80 (s, 3H, OCH3) , 3.67 (s, 2H, CJJ2CONH) , 3.65 (s, 3H, OCH3) , 3.27 (q, 2H, J= 6.9 Hz, NHCJJ2), 2.33 (t, 2H, J= 6.9 Hz, CJJ2CO2), 1.65-1.50 (m, 4H, CH2CH2). 13C NMR (75 MHz, CDC13, delta) : 174.1, 166.8, 162.8, 161.4, 160.8, 159.7, 131.2, 130.0, 121.6, 121.2, 117.8, 114.6, 114.2, 55.5, 55.4, 39.7, 34.4, 33.6, 29.0, 22.2. ESI-MS: m/z (%) : C25H28 206 (M + Na) +: 475.

As the paragraph descriping shows that 78967-07-4 is playing an increasingly important role.

Reference£º
Patent; UNIVERSITA’ DEGLI STUDI DI BARI “ALDO MORO”; SCILIMATI, Antonio; PERRONE, Maria Grazia; VITALE, Paola; (114 pag.)WO2017/187352; (2017); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

78967-07-4, Mofezolac is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of 3,4-bis(4-methoxyphenyl)-5-hydroxyethylisoxazole (X) To a solution of mofezolac (VII) (200 mg, 0.589 mmol), in anhydrous THF (2 mL) kept at 0 C by a bath of ice, 1M BMS in THF (1.16 mL, 1.16 mmol) was added dropwise, and the mixture was stirred overnight at room temperature to give a pale yellow homogeneous solution. Distilled water (1 mL), 20% NaOH (I mL) and 35% H202 (1 mL) were added and the obtained reaction mixture was stirred for 1 hour. Then, the solution was extracted with ethyl acetate. The organic layer was dried over anhydrous Na2S04 and the solvent removed under reduced pressure. The product (X) was isolated as a white solid (68% yield) by flash chromatography on silica gel (hexane/ethyl acetate 6:4) of the reaction crude, the NMR (400 MHZ, CDC13, delta): 3.81 (s, 3H, CH3), 3.85 (s, 3H, CH3); 4.44 (t, 2H, J- 6.6 Hz CH2), 4.26 (t, 2H, J= 6.6 Hz CH2 6.85 (d, 2H, J= 9.0 Hz, ArH), 6.95 (d, 2H, J= 9.0 Hz, ArH), 7.21 (d, 2H, J= 9.0 Hz, ArH); 7.39 (d, 2H, J= 9.0 Hz, ArH). ESI-MS: m/z (%): C18H20NO4 (M)+, 325.

The synthetic route of 78967-07-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; UNIVERSITA’ DEGLI STUDI DI BARI; SCILIMATI, Antonio; PERRONE, Maria, Grazia; VITALE, Paola; WO2014/115020; (2014); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem