摘要 |
<p>New malonylurea derivs. are complexes of formula (I). In this formula, R1 and R2 are -CH2CHAB in which A is H and B is OH, or A is -CH2OX (X = H or 1-5C alkyl) adn B is -OY (Y = H, opt. substd. carbamol, or carbalkoxy); R3, R4, R5, R6, R7 and R8 are H or aliphatic, araliphatic or aryl and the broken lines indicate H bonds. Unlike the barbiturates to which tey are related, (I) have minimal hypnotic activity, low toxicity, and reduced risk of addiction. Specific. complexes (I) inlcude those in which R1 and R2 are each -CH2CH(OCONH2)-CH2OCH-CH3)2, R3, R5 and R7 are ethyl, and R4, R6 and R8 are phenyl. In an example, this is prepd. by mixing phenobarbital, 5-ethyl-5-phenyl-N-(3-isopropoxy-2-carbamoyloxypropyl)malonylure and 5-ethyl-5-phenyl-N-N'-di-(3-isopropoxy-2-carbamoyloxypropyl)maloy- lurea in a molar ratio of 1:2:1 in a mortar, melting the mixture, and pouring the melt into water.</p> |