- 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.
- -
-
-
- A stereoselective synthesis of (E)-1-halo-6,6-dimethyl-2-hepten-4-yne: A key intermediate for terbinafine
-
A study of the stereoselective halogenation of 6,6-dimethyl-1-hepten-4- yn-3-ol (1) using a series of halogenating agents is described. Of the many agents investigated, boron trichloride is the most successful reagent for stereoselective halogenation (E:Z=9:1(max)). The resulting (E)-1-halo-6,6- dimethyl-2-hepten-4-yne (2), a key intermediate for terbinafine, an antifungal agent, is obtained in good yield and stereoselectivity. Two structurally related enyne alcohols have been studied likewise and shown similar versatility. (C) 2000 Elsevier Science Ltd.
- Chou, Shan-Yen,Tseng, Chin-Lu,Chen, Shyh-Fong
-
p. 3895 - 3898
(2007/10/03)
-
- Propenylamines, pharmaceutical compositions containing them and their use as pharmaceuticals
-
A compound of the formula: STR1 wherein the double bond is in the trans configuration and R1 is a radical of formula IIa, STR2 R2, R3, R5, R7 and R8 are each hydrogen, R4 is methyl, and R6 is a radical of formula IIIa where R11 is n-butyl, tertiary butyl or phenyl or a chemotherapeutically acceptable acid addition salt thereof; processes for their production, their use as pharmaceuticals and pharmaceutical compositions containing them.
- -
-
-
- Synthesis and Antifungal Activity of (E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethanamine (SF 86-327) and Related Allylamine Derivatives with Enhanced Oral Activity
-
The allylamine derivatives are a new class of synthetic antifungal agents inhibiting fungal squalene epoxidase.A new subclass, which features an acetylene group conjugated with the allylamine double bond, is characterized by enhanced antifungal activity, especially on oral treatment of guinea pig dermatophytoses.Increased branching of the alkyl group next to the triple bond led to the tert-butylacetylene derivative SF 86-327, a compound with strikingly increased activity in vitro and in vivo, which is now under clinical evaluation.Versatile synthetic routes, comparative biological data, and structure-activity relationship are presented.
- Stuetz, Anton,Petranyi, Gabor
-
p. 1539 - 1543
(2007/10/02)
-
- Benzopyrane and benzothiopyrane derivatives useful as anti-mycotic agents
-
Benzopyrane and benzothiopyrane derivatives which possess pharmaceutical in particular anti-mycotic activity.
- -
-
-
- THE STRUCTURE OF SAFFLOMIN-A, A COMPONENT OF SAFFLOWER YELLOW
-
The structure of safflomin-A, a yellow component of the flowers of Safflower (Carthamus tinctorius L.), was investigated.
- Onodera, Jun-ichi,Obara, Heitaro,Osone, Masahide,Maruyama, Yasunobu,Sato, Shingo
-
p. 433 - 436
(2007/10/02)
-
