Nitrosourea derivatives and process for their production

C - Chemistry – Metallurgy – 07 – D

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260/301, 260/308

C07D 285/12 (2006.01) C07C 275/68 (2006.01) C07D 285/135 (2006.01)

Patent

CA 1160233

ABSTRACT The specification describes a nitrosourea derivative having the general formula: C? - (CH2)2 - N(NO)CO - NHR, wherein -NHR represents a 2-(1,3,4-thiadiazolyl)amino group, an amino residue of a neutral .alpha.-amino acid, or an amino residue of a neutral .alpha.-amino acid whose carboxyl group is amidated with 2-(1,3,4-thiadiazolyl)amine, or a pharmaceu- tically acceptable acid addition salt thereof. The above nitrosourea derivative and its salt are useful as anti- tumor drugs. The above nitrosourea derivative may be prepared either by nitrosating a urea derivative of the general formula: C? - (CH2)2NHCONHR or by reacting N- (2-chloroethyl)-N-nitrosocarbamic acid or a reactive de- rivative thereof with an amino compound of the general formula: R-NH2.

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