- Thiazine (or oxazine) derivatives and preparation thereof
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Thiazine derivatives of the formula [I]: STR1 wherein R1, R2, R4 and R5 are each hydrogen atom; R3 is hydrogen atom or a halogen atom; X is sulfur atom; R6 is naphthyl, a sulfur-containing monoheterocyclic group or a substituted phenyl; Z1 is two hydrogen atoms; Z2 is oxygen atom; A is a lower alkylene; R7 and R8 are the same or different and are each i) hydrogen atom, ii) a lower alkyl, iii) a lower alkenyl, iv) a lower alkynyl, or v) a lower alkyl which is substituted by a substituted phenyl, or both form together with the adjacent nitrogen atom a nitrogen-containing monoheterocyclic group; except for the compound [I] wherein R1, R2, R3, R4 and R5 are each hydrogen atom, X is sulfur atom, R6 is a halogenophenyl, Z1 is two hydrogen atoms, Z2 is oxygen atom, A is a lower alkylene, R7 and R8 are the same or different and each a lower alkyl; or a pharmaceutically acceptable salt thereof, which have calcium antagonistic activity within the cerebral tissues and are useful for prophylaxis and treatment of ischemic encephalopathia.
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- Naphtho thiazine (or oxaline) derivatives and preparations thereof
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Thiazine (or oxazine) derivatives of the formula [I]: STR1 wherein R1 and R2 are both H or form a naphthalene ring together with the benzene ring; R3 and R4 are both H, or one of them is halogen and another is H; X is S or O; R5 and R6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z1 and Z2 is O and another is H2 ; A is lower alkylene; R7 and R8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R1 and R2 are H, Z2 is O and either one of R5 and R6 is substituted phenyl, naphthyl or S-containing heterocyclic group, or their salts, which have calcium antagonistic activity within the cerebral tissues and are useful for prophylaxis and treatment of ischemic encephalopathia and/or cerebral neurocyte dyscrasia, and process for preparing said compounds.
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- A Convenient and General Synthesis of 2-Aryl- and 2-Pyridyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazines
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The reaction of bis(2-aminophenyl) disulphide 1 with methyl or ethyl aryl- or pyridylacetates and sodium hydride gives the title compounds in good yield and high purity.The reaction is general, the starting materials easily available and the workup is simple and rapid.
- Jacobsen, Niels,Kolind-Andersen, Hans
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p. 911 - 914
(2007/10/02)
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