| 摘要 |
<p>Prepn. of glucopyranose-nitrosourea cpds. of formula (I) comprises reacting an amino-glucopyranose cpd. of formula (II), or its acid-addn. salt with an N-nitrosocarbamate of formula (III) (where R1 is OH, 1-4C alkyl or NH-CO-N(NO)-R8, and R2 and R3 are OH or NH-CO-N(NO)-R8, but R1-3 are not all the same; R4 is OH, 1-4C alkoxy or NH2, and R5 and R6 are OH or N2, but R4-6 are not all the same R7 is NO2 or CN; R8 is 1-4C alkyl or CH2CH2Cl). Also claimed are new cpds. of formula (I) where R1 and R3 are OH and R2 is NH-CO-N(NO)-R8. Cpds. (I) are tumour inhibitors. In particular, the new cpd. 3-(D-glucopyranos-6-yl)-1-(2-chloroethyl)-1-nitrosourea (Ia) has higher anti-leukaemia activity and lower diabetogenic activity than selected examples of known cpds. (I). In an example, (Ia) is prepd. from 6-amino-6-desoxy-D-glucopyranose and o-nitrophenyl N-(2-chloroethyl)-N-nitrosocarbamate.</p> |
