78967-07-4 | Page 5 of 5 | Heterocyclic Building Blocks-isoxazole

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Related Products of 78967-07-4, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.78967-07-4, Name is Mofezolac, molecular formula is C19H17NO5. In a article£¬once mentioned of 78967-07-4

Drugs for incontinence

Use in the incontinence of one or more of the following classes of drugs selected from the following: B) salified and non salified nitric oxide-donor drugs, of formula: A-X1?N(O)z, B?) nitrate salts of drugs used for the incontinence, and which do not contain in the molecule a nitric oxide donor group; C) organic or inorganic salts of compounds inhibiting phosphodiesterases.

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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 78967-07-4 is helpful to your research. Electric Literature of 78967-07-4

Electric Literature of 78967-07-4, 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, 78967-07-4, molcular formula is C19H17NO5, introducing its new discovery.

NITRILES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

The present invention relates to a compound of formula (I) wherein Y and Z each is independently N or C; ring A is a carbocyclic group or a heterocyclic group; ring B is a heterocyclic group containing at least one nitrogen atom; R is a hydrogen atom, a substituent, etc,; n is 0, or an integer of from 1 to 10, a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof. The compound of formula (I), a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof has an inhibitory activity against cysteine protease, and it is useful for the prophylaxis and/or treatment of a cysteine protease-related disease such as osteoporosis, etc.

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 78967-07-4. In my other articles, you can also check out more blogs about 78967-07-4

Electric Literature of 78967-07-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 78967-07-4, Mofezolac, introducing its new discovery.

Compositions comprising cyclodextrins and NO- releasing drugs

The present invention relates to composition comprising cyclodextrins and a NO-releasing drug of formulaA-X-L-NOnwhereinAis the radical deriving from a drug;Xis a divalent radical connecting A with the NO-releasing group L-NOn;Lis selected from the group consisting of: O and S;nis 1 or 2.

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

78967-07-4, To a cold (ice-bath) solution of 2-(3,4-bis(4-methoxyphenyl)isoxazol-5-yl)acetic acid (mofezolac, 300 mg, 0.885 mmol) and 1,2:3,4-Di-O-isopropylidene-D-galactose (230 mg, 0.885 mmol) in CH2Cl2 (5 mL) , 4-(dimethylamino)pyridine (DMAP) (27 mg, 0.22 mmol), and N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (EDC HCl, 680 mg, 3.56 mmol) were added in portions under argon atmosphere. The reaction mixture was stirred at room temperature for 24h and then quenched by adding distilled water. The aqueous phase was extracted three times with EtOAc. The combined organic phases were dried over anhydrous Na2SO4, filtered, and the solvent removed under reduced pressure. The product (375 mg) was isolated by column chromatography (silica gel; CHCl3/MeOH 95:5) of the reaction crude. 73% Yield. NMR (300 MHz, CDCl3, delta) : 7.41-7.36 (m, 2H, aromatic protons) ; 7.19-7.14 (m, 2H, aromatic protons) ; 6.94-6.89 (m, 2H, aromatic protons) ; 6.85-6.81 (m, 2H, aromatic protons) ; 5.53 (d, 1H, J = 4.95 Hz) ; 4.61 (dd, 1H, J = 8.0 Hz, J = 2.5 Hz) ; 4.34-4.25 (m, 2H) ; 4.18 (dd, 2H, J = 8.0 Hz, J = 1.9 Hz) ; 4.05-3.99 (m, 1H) ; 3.83 (s, 3H OCH3) ; 3.80 (s, 3H, OCH3) ; 3.79 (s, 2H, CH2) ; 1.45 (s, 6H, 2CH3) ; 1.32 (s, 3H) ; 1.31 (s, 3H) . ESI-MS m/z (%) : C31H35NO10 (M + Na)+: 604.

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Reference£º
Patent; UNIVERSITA’ DEGLI STUDI DI BARI “ALDO MORO”; SCILIMATI, Antonio; PERRONE, Maria Grazia; VITALE, Paola; (114 pag.)WO2017/187352; (2017); A1;,
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78967-07-4, Mofezolac is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78967-07-4, General procedure: 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).

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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;,
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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.

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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.

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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.

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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.

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