3-(2-Methylthio-2-tertiary aminoacetyl)-5-phenylisoxazoles
AssigneeShionogi & Co., Ltd.
InventorsShoichi Hirai, Kyozo Kawata
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AssigneeShionogi & Co., Ltd.
InventorsShoichi Hirai, Kyozo Kawata
Estimating the term…
A phenylisoxazole of the formula: ##SPC1## Wherein, Y represents a hydrogen atom, a halogen atom, an alkali metal atom or a tertiary amino group and Z represents a sulfur atom or a sulfoxide group. They are prepared by subjecting 3-alkoxycarbonyl-5-phenylisoxazole to a treatment with at least one agent selected from the group consisting where required and as necessary of dimethyl sulfoxide, a neutralizing agent, an agent capable of releasing a halogen ion and a secondary amine at a temperature ranging from about -5.degree.C to about 70.degree.C for a time period from several minutes up to about 4 hours. The phenylisoxazoles are useful as intermediates for preparing a 3-(2-tertiary amino-1-hydroxyethyl)-5-phenylisoxazole, any of which is known as useful medicaments having a remarkable analgesic, antispasmodic, antiphretic, antiallergic, antiinflammatory, antitussive activity or the like, each reflecting the species of the substituent tertiary amino groups and generally having a very low toxicity.
A phenylisoxazole of the formula:
3-(2-Methylthio-2-piperidinoacetyl)-5-phenylisoxazole.
3-(2-Methylthio-2-dimethylaminoacetyl)-5-phenylisoxazole.
3-(2-Methylthio-2-diethylaminoacetyl)-5-phenylisoxazole.
3-(2-Methylthio-2-dipropylaminoacetyl)-5-phenylisoxazole.
3-(2-Methylthio-2-methylethylaminoacetyl)-5-phenylisoxazole.
3-(2-Methylthio-2-methylisopropylaminoacetyl)-5-phenylisoxazole.
3-(2-Methylthio-2-pyrrolidinoacetyl)-5-phenylisoxazole.
Dependencies are inferred from the claim text.