Process for the preparation of unsymmetrically 1,3-disubstituted nitroso ureas

DETAILED DESCRIPTION What I claim is: 1.
A compound of the formula: R--NH CO N (NO) CH.
sub.
2 --CH.
sub.
2 --Cl wherein (1) R is an alkyl group of from two to six carbon atoms, which may be substituted with at least one --O--CO--R' or --O--SO.
sub.
2 --R' group wherein R' is lower alkyl, or R is a straight-chain alkyl group of from two to six carbon atoms, which may be substituted with at least one --OH group, or (2) R is an alkyl group of from two to six carbon atoms and substituted with a --COOH or --COOMe group or with one or more --COOR' or --CONH.
sub.
2 groups, wherein Me is a metal and R' is lower alkyl, and may be additionally substituted with at least an --OH, --O--CO--R' or O--SO.
sub.
2 R' group, and wherein in (1) or (2) R may also be substituted with a further --NH CO N (NO) CH.
sub.
2 CH.
sub.
2 Cl residue.
2.
An ester of the compound of claim 1.
3.
A salt of the compound of claim 1.
4.
1-(2-hydroxyethyl)-3-(2-chloroethyl)-3-nitroso urea.
5.
An ester of the compound of claim 4.
6.
1,1-'-tetramethylene-bis-3-(2-chloroethyl)-3-nitroso urea.
7.
1-(2-methanesulfonyloxyethyl)-3-(2-chloroethyl)-3-nitroso urea.
8.
2-(3-(2-chloroethyl)-3-nitrosoureido-acetamide.
9.
1,1'-(polyalkylene)-bis-3-(2-chloroethyl)-3-nitrosourea wherein the alkylene group has from two to six carbon atoms.
10.
1,1'-(polymethylene)-bis-3-(2-chloroethyl)-3-nitrosourea.
11.
A therapeutic composition containing, as the active ingredient, the compound of claim 9.
12.
A therapeutic composition containing, as the active ingredient, the compound of claim 1 together with a pharmaceutically acceptable carrier or auxiliary agent.
13.
A therapeutic composition containing, as the active ingredient, the compound of claim 4 together with a pharmaceutically acceptable carrier or auxiliary agent.




Description:
The present invention relates to a new process for the preparation of unsymmetrically 1,3-disubstituted nitroso ureas, its esters and salts, to novel unsymmetrically 1,3-disubstituted nitroso ureas, its esters and salts prepared thereby and to new intermediate compounds for their preparation