Karoly Zauer

The synthesis of (3,4,5,6-tetrahydro-4-oxo-2h-1,3-thiazin-2-yl)-alkanoic acids, their derivatives and some related compounds

Abstract 5,6-Dihydro-2 H -1,3-thiazin-4(3 H )-ones 2–10 related to the natural antituberculytic Mycobacidine 1 , have been synthesised. Some of the compounds of types 2,3 and 5 proved highly active in vitro against Mycobacterium tuberculosis typ. humanus (H 37 R v ), but the in vitro activities are diminished or suspended in the presence of biotine.

The synthesis and some reactions OF 3-(2-aminophenyl)-2-iminothiazolidines. ring closure of n-(2-thiocyanaoethyl,)-ophenylenediamines; thiazolidine vs. 3,1,6-benzothiadiazocine formation

Abstract When treated with strong acids, the N -(2-thiocyanatoethyl)- o -phenylenediamines ( 1g - 1v ) are cyclized exclusively to 3-(2-aninophen- yl)-2-iminothiazolidines ( 6 ) while the related tertiary amines ( 1a - 1f ) gave, under the same conditions, benzothiadiazocines of types ( 2 ) or ( 3 ). Some of the type ( 6 ) compounds are highly active antidepressants of low toxicity. Thermal reactions of compound ( 6b ) and its conversion into tricyclic compounds of types ( 22 ) and ( 24 ) are also reported.

Benzoxadiazocines, benzothiadiazocines and benzotriazocines—II : The synthesis of 3,4,5,6-tetrahydro- and 1,2,3,4,5,6-hexa-hydro-1,3,6-benzotriazocines

Abstract The general method devised by two of the authors for the synthesis of derivatives of the novel 3,1,6-benzoxadiazocine, 3,1,6-benzothiadiazocine and 1,3,6-benzotriazocine ring systems has been applied to the preparation of a series of 3,4,5,6-tetrahydro- and 1,2,3,4,5,6-hexahydro-1,3,6-benzotriazocines for pharmacological screening.

Benzoxadiazocines, benzothiadiazocines and benzotriazocines—III : The synthesis of 2-(subst.)amino- and 2-(2-subst.hydrazino)-6-(alkylsulfonyl and arylsulfonyl)-5,6-dihydro-4H-3,1,6-benzothiadiazocines

Abstract A series of derivatives of the novel 5,6-dihydro-4H-3,1,6-benzothiadiazocine ring system has been synthesised for pharmacological screening by application of a method devised earlier by two of the authors. The proof of structure of the benzothiadiazocine derivatives is based on chemical and spectroscopic evidence.

Simple and condensed β-lactams. Part 13. Synthesis of some 1-(3-acylamino-2-oxoazetidin-1-yl)-cyclopentane- and -cyclohexanecarboxylic acids

The synthesis of the-title compounds 9a, b, c′, f and of the sodium salts 10d, e, g starting with phthaloylglycyl chloride and the trimers 4a–d of methyleneamino-cyclopentane and -cyclohexane-carboxylic esters 3a–d is described. The products were devoid of any antibacterial activity.