- Heterocyclic compound having oxime group
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The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2— and the like; and X represents a sulphur atom and the like.]or a salt thereof, or a hydrate thereof.
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- Nucleophilic Addition of 2-, 3-, or 4-pyridine to the Aziridine, 7-Methyl-7-azabicycloheptane
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The synthesis of trans-(+/-)-N-methyl-N-amino>cyclohexyl>-4-benzofuranacetamide dihydrochloride, 1 which is a 3-pyridyl derivative of the kappa opioid analgesic trans-(+/-)-N-methyl-N-benzofuran-4-acetamide monohydrochloride, 2 is described.The key intermediate is trans-(+/-)-N,N'-dimethyl-N--1,2-cyclohexanediamine, 9 which is formed by nucleophilic addition of 3-pyridine 6 to the aziridine, 7-methyl-7-azabicycloheptane, 4.During attempts to prepare the 2- or 4-isomeric pyridyl derivatives of 1 it was discovered that both 2- or 4-pyridine, 5 or 7 are converted to N-methyl-N,N-di- 11 and N-methyl-N,N-di 13 respectively by refluxing in toluene in the presence of ammonium chloride.The 3-isomer, 6 is unchanged after treatment under identical conditions.Careful control of the reaction conditions enabled the aziridine 4 to be ring opened with the pyridyl amines 5 or 7 to give the 1,2-diamines trans-(+/-)-N,N'-dimethyl-N--1,2-cyclohexanediamine, 8 or trans-(+/-)-N,N'-dimethyl-N--1,2-cyclohexane diamine 10 respectively.
- Rees, David C
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p. 147 - 150
(2007/10/02)
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