Quinoline and quinoxaline compounds
A compound, polymer technology, applied in the Lck tyrosine kinase activity inhibitor of quinoxaline can be used in the field of treatment, can solve the problems such as no reports
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[0054] Preferred compounds of the invention are compounds of formula I as defined below, wherein R 1a is an optionally substituted lower alkoxy group, an optionally substituted monocyclic cycloalkoxy group, an optionally substituted heterocyclylcarbonyloxy group, or an optionally substituted monoepoxyheteroheterooxyloxy group; more preferably R 1a is methoxy, ethoxy, 2-(ethoxy)ethoxy, 2-(4-morpholinyl)ethoxy or furyloxy.
[0055] Further preferred compounds of the invention are compounds of formula I as defined below, wherein R 1b is hydrogen, optionally substituted lower alkoxy, optionally substituted monocyclic cycloalkoxy, optionally substituted or optionally substituted lower alkoxy; still more preferably R 1b is methoxy or ethoxy.
[0056] Further preferred compounds of the invention are compounds of formula I as defined below, wherein R 1a and R 1b is lower alkoxy; more preferably lower alkoxy is methoxy or ethoxy.
[0057] Further preferred compounds of the inventi...
Embodiment 1
[0157] Example 1 2-(3-fluorophenylamino)-6,7-diethoxyquinoxaline
[0158] To 0.25 g (0.989 mmol) of 2-chloro-6,7-diethoxyquinoxaline was added 2 ml of m-fluoroaniline. The mixture was heated at 120° C. overnight under nitrogen atmosphere. The obtained mixture was separated by chromatography (30:1 CH 2 Cl 2 : EtOH), a partially purified product was obtained. The solid was triturated with ethyl acetate to give 0.175 g of product as a brownish yellow solid, 54.1% yield (m.p. 193°C).
[0159] Elemental Analysis C 18 h 18 N 3 o 2 F 0.25H 2 o
[0160] Calculated: C, 65.15; H, 5.62; N, 12.66;
[0161] Found: C, 65.30; H, 5.30; N, 12.41.
Embodiment 2
[0162] Example 2 2-anilino-6-methoxyquinoxaline hydrochloride
[0163] To 2-chloro-6-methoxyquinoxaline (0.93 g, 4.8 mmol) was added aniline (1.3 ml, 14.3 mmol) under argon atmosphere. The reaction mixture was heated at 120°C for 2 hours, then at 150°C for 1.5 hours. The mixture was cooled and CH was added 2 Cl 2 . The obtained suspension was stirred, the orange solid was filtered off and washed with CH 2 Cl 2 / Et 2 O washed, then vigorously stirred in water for 40 min, filtered, and washed with Et 2 O washes afforded a bright yellow solid.
[0164] The following compounds were prepared analogously starting from appropriate starting materials.
[0165] 2-(3-Carbamoylphenylamino)-6-methoxyquinoxaline, m.p. 2.47°C. Elemental Analysis C 16 h 14 N 4 o 2 0.25H 2 O, calculated: C, 64.31; H, 4.89; N, 18.75;
[0166] Found values: C, 64.24; H, 5.04; N, 18.75;
[0167] 2-(2-Fluorophenylamino)-6,7-diethoxyquinoxaline, m.p. 184°C. Elemental Analysis C 18 h 18 FN 3 ...
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