| abstract |
1,234,935. Piperazine derivatives. NATIONAL RESEARCH DEVELOPMENT CORP. 2 Oct., 1968 [3 July, 1967], No. 30617/67. Heading C2C. [Also in Division A5] Compounds I (including optical isomers and salts thereof), some of which are novel, wherein R 1 and R 2 signify H or Me, or together constitute an ethylene bridging group, subject to the proviso that where R 1 and R 2 are both Me, the Me groups are in the meso relationship, are obtained: (a) by the interaction of the appropriate tetra-acetic acid and formamide, or (b) by cyclizing the appropriate N,N,N<SP>1</SP>,N<SP>1</SP>- tetracarbamoylmethyl - 1,2 - diamino - alkane utilizing polyphosphoric acid or phenol. The compounds I have activity in relation to certain forms of cancer. meso - 2,3 - Diaminobutane tetra-acetic acid dihydrate and trans - 1,2 - diaminocyclobutane tetra-acetic acid monohydrate are prepared similarly to the procedure of Dwyer and Garvan J. Amer. Chem. Soc., 1959, 81, 2956. N,N,N<SP>1</SP>N<SP>1</SP> - Tetracarbamoylmethyl - 1,2 - diaminopropane is prepared similarly to the procedure of Badinard et al., Bull. Soc. Chim., 1960, 382. meso - 2,3 - Diaminobutane is prepared by lithium aluminium hydride reduction of the dibenzyl ether of dimethyl glyoxime and is isolated as the dihydrochloride. |