Gpr17 receptor modulators.
A technology selected from compounds, applied in anti-inflammatory agents, non-central analgesics, allergic diseases, etc., can solve the problem of not being able to obtain the crystal structure of GPR17
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[0023] In a first embodiment, preferably, the compound of formula (I):
[0024]
[0025] Preferably selected from the group, wherein R is selected from the group comprising H, methyl, ethyl, phenyl, benzyl; R 2 selected from the group comprising H, naphthyl, phenyl, preferably 4-chlorophenyl, benzimidazole, preferably 2-methylbenzimidazole; R 3 Preferably selected from the group consisting of H, 4-methyl, 4-NHC(O)R 1 group, where R 1 is phenyl or monosubstituted, disubstituted or trisubstituted phenyl, wherein the substituents on the phenyl are independently selected from C1-C4 linear or branched chain alkyl, acetyl, C1-C4 alkoxy Group, carboxyl C1-C4 alkyl, F, Cl, Br, I, trifluoromethyl (triphluoromethyl), nitro, CN.
[0026] Preferably, R is H or methyl; R 2 Is H, naphthyl, phenyl, preferably 4-chlorophenyl, benzimidazole, preferably 2-methylbenzimidazole; R 3 is H, 4-methyl, 4-NHC(O)R 1 , where R 1 is phenyl, preferably 4-chlorophenyl.
[0027] Preferably, the co...
Embodiment 1
[0060] N-[4-[5-[[2-[(4-chlorophenyl)amino]-2-oxoethyl]thio]-4-methyl-4H-1,2 of formula (I), Synthesis of 4-triazol-3-yl]phenyl]-benzamide
[0061]
[0062] To a solution of a) in DCM / water and KOH was added an equimolar amount of benzoyl chloride in DCM to give product b), which was then reacted with NH in EtOH 2 NH 2 *H 2 O reaction to obtain N-[4-(hydrazinocarbonyl)phenyl]benzamide c):
[0063]
[0064] Then, c) was reacted with MeNCS in EtOH in the presence of KOH, followed by acidification with HCl, thus obtaining N-[4-(4-methyl-5-sulfanyl-4H-1,2,4 -triazol-3-yl)phenyl]benzamide d):
[0065]
[0066] By reacting d) with 2-chloro-N-(4-chlorophenyl)acetamide e) in EtOH, KOH and TEA:
[0067]
[0068] The desired product N-[4-[5-[[2-[(4-chlorophenyl)amino]-2-oxoethyl]thio]-4-methyl-4H-1,2 has been obtained, 4-Triazol-3-yl]phenyl]-benzamide.
Embodiment 2
[0069] Example 2. 1H-1,5-N-(2,4-dimethoxyphenyl)-2,3-dihydro-2-oxo-4-phenylbenzodiazepine of formula (II) miscellaneous -Synthesis of 1-acetamide
[0070]
[0071] [(2-Aminophenyl)amino]methyl 3-oxo-3-phenylpropionate a) has been reacted in xylene at 140°C to give 4-phenyl-1,3- Dihydro-2H-1,5-benzodiazepine -2-ketone b), then, in K 2 CO 3 , DMF, which is reacted with 2-chloro-N-(2,4-dimethoxyphenyl)acetamide c) to give the desired product, which is 1H-1,5-N-(2 ,4-dimethoxyphenyl)-2,3-dihydro-2-oxo-4-phenylbenzodiazepine -1-Acetamide. 2-Chloro-N-(2,4-dimethoxyphenyl)acetamide was obtained by reacting 2,4-dimethoxyaniline with chloroacetyl chloride in refluxing MeCN.
[0072]
PUM
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