Residue:Article Title: Compounds and methods of use
Article Snippet: The mixture was concentrated under reduced pressure to give a crude product, which was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Waters Xbridge 150×50 mm×10 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 25% to 55% in 8.8 min, hold 100% B for 2 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to give N-[(2S)-3-[7-chloro-6-(oxazol-5-ylmethoxy)-3,4-dihydro-1H-isoquinolin-2-yl]-2-hydroxy-propyl]-2-(cyclobutylamino)pyridine-4-carboxamide (15 mg, 17.2% yield) as a yellow dry powder.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-215, Gilson 322 Pump, Gilson 156 UV Detector; Column: Xtimate C18 150*40 mm*5 μm; Mobile phase A: H2O with NH3—H2O and NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 23% to 53% in 20 min, hold 100% B for 5 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The crude product was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 75*40 mm*3 μm; Mobile phase A: [water (NH3H2O+NH4HCO3)-ACN]; Mobile phase B: MeCN; Gradient: B from 31% to 61% in 10.5 min, hold 100% B for 2 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm) to afford N-[2-amino-5-(p-tolyl)phenyl]-4-(3-methyl-1-oxo-4,5-dihydro-3H-isothiazol-1-yl)benzamide (45 mg, 70.2% yield) as white solid.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Durashell 150×25 mm×5 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 39% to 69% in 10 min, hold 100% B for 2.5 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(4-chlorophenyl)phenyl]-4-(methylsulfonimidoyl)benzamide (15.8 mg).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 80×40 mm×3 μm; Mobile phase A: water with 10 mmol NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 27% to 57% in 7.8 min, hold 100% B for 1 min; Flow Rate: 25 mL/min; Column Temperature: about 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(2-thienyl)phenyl]-4-(cyclopropylsulfonimidoyl)benzamide (about 61.7 mg).
Purification:Article Title: Compounds and methods of use
Article Snippet: The mixture was concentrated under reduced pressure to give a crude product, which was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Waters Xbridge 150×50 mm×10 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 25% to 55% in 8.8 min, hold 100% B for 2 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to give N-[(2S)-3-[7-chloro-6-(oxazol-5-ylmethoxy)-3,4-dihydro-1H-isoquinolin-2-yl]-2-hydroxy-propyl]-2-(cyclobutylamino)pyridine-4-carboxamide (15 mg, 17.2% yield) as a yellow dry powder.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-215, Gilson 322 Pump, Gilson 156 UV Detector; Column: Xtimate C18 150*40 mm*5 μm; Mobile phase A: H2O with NH3—H2O and NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 23% to 53% in 20 min, hold 100% B for 5 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The crude product was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 75*40 mm*3 μm; Mobile phase A: [water (NH3H2O+NH4HCO3)-ACN]; Mobile phase B: MeCN; Gradient: B from 31% to 61% in 10.5 min, hold 100% B for 2 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm) to afford N-[2-amino-5-(p-tolyl)phenyl]-4-(3-methyl-1-oxo-4,5-dihydro-3H-isothiazol-1-yl)benzamide (45 mg, 70.2% yield) as white solid.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Durashell 150×25 mm×5 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 39% to 69% in 10 min, hold 100% B for 2.5 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(4-chlorophenyl)phenyl]-4-(methylsulfonimidoyl)benzamide (15.8 mg).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 80×40 mm×3 μm; Mobile phase A: water with 10 mmol NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 27% to 57% in 7.8 min, hold 100% B for 1 min; Flow Rate: 25 mL/min; Column Temperature: about 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(2-thienyl)phenyl]-4-(cyclopropylsulfonimidoyl)benzamide (about 61.7 mg).
High Performance Liquid Chromatography:Article Title: Compounds and methods of use
Article Snippet: The mixture was concentrated under reduced pressure to give a crude product, which was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Waters Xbridge 150×50 mm×10 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 25% to 55% in 8.8 min, hold 100% B for 2 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to give N-[(2S)-3-[7-chloro-6-(oxazol-5-ylmethoxy)-3,4-dihydro-1H-isoquinolin-2-yl]-2-hydroxy-propyl]-2-(cyclobutylamino)pyridine-4-carboxamide (15 mg, 17.2% yield) as a yellow dry powder.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-215, Gilson 322 Pump, Gilson 156 UV Detector; Column: Xtimate C18 150*40 mm*5 μm; Mobile phase A: H2O with NH3—H2O and NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 23% to 53% in 20 min, hold 100% B for 5 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The crude product was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 75*40 mm*3 μm; Mobile phase A: [water (NH3H2O+NH4HCO3)-ACN]; Mobile phase B: MeCN; Gradient: B from 31% to 61% in 10.5 min, hold 100% B for 2 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm) to afford N-[2-amino-5-(p-tolyl)phenyl]-4-(3-methyl-1-oxo-4,5-dihydro-3H-isothiazol-1-yl)benzamide (45 mg, 70.2% yield) as white solid.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Durashell 150×25 mm×5 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 39% to 69% in 10 min, hold 100% B for 2.5 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(4-chlorophenyl)phenyl]-4-(methylsulfonimidoyl)benzamide (15.8 mg).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 80×40 mm×3 μm; Mobile phase A: water with 10 mmol NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 27% to 57% in 7.8 min, hold 100% B for 1 min; Flow Rate: 25 mL/min; Column Temperature: about 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(2-thienyl)phenyl]-4-(cyclopropylsulfonimidoyl)benzamide (about 61.7 mg).
Chromatography:Article Title: Compounds and methods of use
Article Snippet: The mixture was concentrated under reduced pressure to give a crude product, which was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Waters Xbridge 150×50 mm×10 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 25% to 55% in 8.8 min, hold 100% B for 2 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to give N-[(2S)-3-[7-chloro-6-(oxazol-5-ylmethoxy)-3,4-dihydro-1H-isoquinolin-2-yl]-2-hydroxy-propyl]-2-(cyclobutylamino)pyridine-4-carboxamide (15 mg, 17.2% yield) as a yellow dry powder.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-215, Gilson 322 Pump, Gilson 156 UV Detector; Column: Xtimate C18 150*40 mm*5 μm; Mobile phase A: H2O with NH3—H2O and NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 23% to 53% in 20 min, hold 100% B for 5 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The crude product was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 75*40 mm*3 μm; Mobile phase A: [water (NH3H2O+NH4HCO3)-ACN]; Mobile phase B: MeCN; Gradient: B from 31% to 61% in 10.5 min, hold 100% B for 2 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm) to afford N-[2-amino-5-(p-tolyl)phenyl]-4-(3-methyl-1-oxo-4,5-dihydro-3H-isothiazol-1-yl)benzamide (45 mg, 70.2% yield) as white solid.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Durashell 150×25 mm×5 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 39% to 69% in 10 min, hold 100% B for 2.5 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(4-chlorophenyl)phenyl]-4-(methylsulfonimidoyl)benzamide (15.8 mg).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 80×40 mm×3 μm; Mobile phase A: water with 10 mmol NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 27% to 57% in 7.8 min, hold 100% B for 1 min; Flow Rate: 25 mL/min; Column Temperature: about 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(2-thienyl)phenyl]-4-(cyclopropylsulfonimidoyl)benzamide (about 61.7 mg).
Column Chromatography:Article Title: Compounds and methods of use
Article Snippet: The mixture was concentrated under reduced pressure to give a crude product, which was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Waters Xbridge 150×50 mm×10 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 25% to 55% in 8.8 min, hold 100% B for 2 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to give N-[(2S)-3-[7-chloro-6-(oxazol-5-ylmethoxy)-3,4-dihydro-1H-isoquinolin-2-yl]-2-hydroxy-propyl]-2-(cyclobutylamino)pyridine-4-carboxamide (15 mg, 17.2% yield) as a yellow dry powder.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-215, Gilson 322 Pump, Gilson 156 UV Detector; Column: Xtimate C18 150*40 mm*5 μm; Mobile phase A: H2O with NH3—H2O and NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 23% to 53% in 20 min, hold 100% B for 5 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The crude product was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 75*40 mm*3 μm; Mobile phase A: [water (NH3H2O+NH4HCO3)-ACN]; Mobile phase B: MeCN; Gradient: B from 31% to 61% in 10.5 min, hold 100% B for 2 min; Flow Rate: 30 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm) to afford N-[2-amino-5-(p-tolyl)phenyl]-4-(3-methyl-1-oxo-4,5-dihydro-3H-isothiazol-1-yl)benzamide (45 mg, 70.2% yield) as white solid.
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Durashell 150×25 mm×5 μm; Mobile phase A: H2O with 0.05% NH3—H2O (v %); Mobile phase B: MeCN; Gradient: B from 39% to 69% in 10 min, hold 100% B for 2.5 min; Flow Rate: 25 mL/min; Column Temperature: 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(4-chlorophenyl)phenyl]-4-(methylsulfonimidoyl)benzamide (15.8 mg).
Article Title: HDAC inhibitors and therapeutic use thereof
Article Snippet: The residue was purified by preparative HPLC (Instrument: Gilson GX-281 Liquid Handler, Gilson 322 Pump, Gilson 156 UV Detector; Column: Phenomenex Gemini-NX 80×40 mm×3 μm; Mobile phase A: water with 10 mmol NH4HCO3 (v %); Mobile phase B: MeCN; Gradient: B from 27% to 57% in 7.8 min, hold 100% B for 1 min; Flow Rate: 25 mL/min; Column Temperature: about 30° C.; Wavelength: 220 nm, 254 nm) to afford N-[2-amino-5-(2-thienyl)phenyl]-4-(cyclopropylsulfonimidoyl)benzamide (about 61.7 mg).
| 
Gilson Inc is a verified supplier 
Gilson Inc manufactures this product 