Nitrosourea derivative

Details Nitrosourea derivative Nitrosourea derivative

1974-11-25

1977-01-18

Gallagher, Richard J.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260239BC, 260250R, 260250BN, 2602564Q, 2602564R, 260288R, 26029387, 260295E, 260302F, 260302A, 260307D, 260307H, 260307R, 2603096, 260310R, C07D23942

Patent

active

040039013

ABSTRACT:
Nitrosourea derivatives represented by the formula ##STR1## wherein A represents a group of the formula B--Y-- in which
B is an unsaturated 5- or 6-membered heterocyclic group which has the as hetero atom at least one nitrogen atom, an unsaturated 9-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring or an unsaturated 10-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring, the heterocyclic groups optionally having alkyl, alkoxy, hydroxyl, amino, hydroxyalkyl or halogen as ring substituent and
Y represents a group of the formula --(CH.sub.2).sub.m -- in which m is an integer of 1 or 2, the group optionally having alkyl as a substituent;
A group of the formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may be the same or different and each represents a hydrogen atom or an alkyl group; or a group of the formula ##STR3## in which R's may be the same or different and each represents a halogen atom or an alkyl group, n is an integer of 0 to 3 inclusive and Z is an ethylene group which may be substituted with alkyl; and
X represents a halogen atom and acid addition salts thereof. The Compounds of the present invention are prepared from the corresponding 2-halogeno-ethylurea derivatives by means of conventional nitrosation procedures and useful as an antileukemic drug for various types of leukemia.

REFERENCES:
smith, P. A. S., "Open Chain Nitrogen Compounds," vol. 1, 1965, W. A. Benjamin, Inc. pp. 272-273.
Johnson, et al. (I), "J. Med. Chem." vol. 6, 1963, pp. 669-675.
Johnson, et al. (II), "J. Med. Chem.," vol. 9, 1966, pp. 892, 898- 899, 907 and 909-910.

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