- Antifungal amine derivatives and processing for producing the same
-
Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1represents a C1-5alkyl group which may be halogenated, R2represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3represents oxygen atom or a methylene group which may be substituted by a C1-4alkyl group; and R4represents 1-or 2 naphthyl group or a phenyl group which may be substituted.
- -
-
-
- Highly selective TFAA-cleavage of tertiary 2,4-dimethoxybenzylamines and its use in the synthesis of secondary amines
-
TFAA-treatment of allylic, propargylic, homopropargylic and some benzylic tert. 2, 4-dimethoxybenzylamines leads to highly selective cleavage of their dimethoxybenzylic C-N bonds. The resultant trifluoroacetamides can then readily be converted to the corresponding secondary amines.
- Nussbaumer,Baumann,Dechat,Harasek
-
p. 4591 - 4602
(2007/10/02)
-
- Synthesis and Structure-Activity Relationship of Benzothienylallylamine Antimycotics
-
Benzothiophene analogues of the allylamine antimycotic terbinafine (2) bearing the side chain at various positions and optionally substituted by halogen have been prepared and their antifungal activity studied.Derivatives bearing the side chain at positions 3, 4, or 7 are bioequivalents of 2.Compounds containing the allylamine side chain at position 7, with a further substituent at position 3, showed significantly enhanced activity against Candida albicans, an effect which appears to be specifically linked only to this particular substitution pattern. 3-Chloro-7-benzothienyl derivative 7m was found to be the most potent allylamine antimycotic identified so far.In general, substituted benzothiophenes can be used not only as potential equivalents of naphthalene in bioactive compoudns but also as a tool to selectively modify biological activities.
- Nussbaumer, Peter,Petranyi, Gabor,Stuetz, Anton
-
-
- Benzothienylallylamines processes for their production and their use as pharmaceuticals
-
Benzothienyldialkylallylamines wherein the amine side chain is attached to the ring via an alkyl radical and is either in 4-, 5-, 6- or 7-position or if not bears tertiary alkylethynyl or alkenylethynyl as its terminal group, which are useful, in particular, as anti-mycotic agents.
- -
-
-
- Benzopyrane and benzothiopyrane derivatives useful as anti-mycotic agents
-
Benzopyrane and benzothiopyrane derivatives which possess pharmaceutical in particular anti-mycotic activity.
- -
-
-
