| 摘要 |
The invention comprises compounds of the general formula: <FORM:0843602/IV(b)/1> wherein R is hydrogen or an alkyl or dialkylaminomethyl group, and a process for the preparation of N-(5-nitro-2-furfurylidene)-3-amino-2-thio-oxazolidones by condensing 5-nitro-2-furaldehyde or a functional derivative thereof with a 3-amino-2-thio-oxazolidone, which may suitably be employed in the form of a condensation product with an aldehyde or ketone. The 3-amino-2-thio-oxazalidone used as a starting material is suitably prepared by reacting a hydrazine-2-hydroxy-alkane or a 1-hydrazino-3-dialkylamino-3-propanol with carbon disulphide or thiophosgene in the presence of an alkali. The products are used as chemotheraputic agents. In examples (1) 2-hydroxypropyl-hydrazine, salicaldehyde and carbon disulphide are refluxed with aqueous sodium hydroxide to give N-(salicylidene)-3-amino 5-methyl-2-thio-oxazolidone together with some 2-salicylidene-1-(2-hydroxypropyl) dithiocarbazic acid which is also converted to N-salicylidene-3-amino-5-methyl-2-thiooxazolidone by pyrolysis of the lead salt, and the combined yield of salicylidene thio-oxazolidone is condensed with 5-nitro-2-fufural to give N-nitro-2-(5-furfurylidene)-3-amino-5-methyl-2-thio-oxazolidone; (2) hydroxyethyl hydrazine is condensed with thiophosgene and the product is reacted with 5-nitro-2-furfural to give N-(5-nitro-2-furfurylidene)-3-amino-2-thio-oxazolidone and (3) 1-hydrazino-3-dimethylamino-2-propanol is condensed with thiophosgene and the product is reacted with 5-nitro-2-furfural to give N-(5-nitro-2-furfurylidene) -3-amino-5-dimethylaminomethyl-2-thio-oxazolidone.ALSO:Pharmaceutical preparations having antiprotozoal activity comprise N-(5-nitro-2-furfurylidene)-3-amino-2-thiooxazolidones (see Group IV(b)) optionally bearing an alkyl or dialkylaminomethyl substituent in the 5-position of the oxazolidine ring, and a pharmaceutical carrier. Preparations for oral administration may take the form of gelatine capsules, suspensions, tablets or lozenges. |
