| 摘要 |
1527497 Phosphoric acid diamide derivatives SHIONOGI & CO Ltd 17 Nov 1975 [20 Nov 1974] 47320/75 Heading C2P The invention comprises compounds of the general formula wherein one of X and Y is halogen, e.g. Cl, Br or I, and the other of X and Y is an alkanesulphonyloxy group, R is alkyl and either A is hydrogen and B is a group -CH=C(R 1 )(R 2 ) wherein each of R 1 and R 2 is independently a group which does not interfere with ozone oxidation of the adjacent double bond, or A and B taken together represent the group >CH-OOH. Compounds of the latter type having the Formula I wherein one of X and Y is halogen and the other is a C 1 -C 5 alkane sulphonyloxy group and R is C 1 -C 5 alkyl are therapeutically useful compounds as antitumour agents and as immunosuppressive agents and may be obtained by oxidation with ozone (suitably in the presence of a peroxide, e.g. H 2 O 2 ) of compounds having the Formula II wherein X, Y and R are as defined for (I) and R 1 and R 2 are each independently H, alkyl, aryl or aralkyl. The ozone oxidation may be carried out in a suitable inert solvent using ozone, or oxygen or air containing ozone. Analogous compounds of Formula I but in which R is any alkyl radical and one of X and Y is any alkane sulphonyloxy group may be obtained similarly from the corresponding comnounds in which A is H and B is -CH=C(R 1 )(R 2 ). The compounds II where X is Cl and Y is CH 3 SO 3 , may be prepared by the following reaction scheme and compounds II in which X is CH 3 SO 3 and Y is Cl may be obtained by the following reaction scheme Other compounds II may be prepared similarly. The compounds having the Formula I may be used as active ingredients in pharmaceutical or veterinary compositions in conjunction with appropriate diluents, carriers or excipients. |
