Process for preparing bis(3,5-dioxopiperazinyl) alkanes or...

C - Chemistry – Metallurgy – 07 – D

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260/266.2

C07D 241/08 (2006.01)

Patent

CA 1303614

Abstract A process for preparing a compound of the formula (I) Image (I) wherein R1 and R2 are individually selected from the group consisting of hydrogen and methyl or R1 and R2 together represent an ethylene bridge group comprising: reacting a diamine of the formula (II) H2N-CHR1-CHR2-NH2 (II) where R1 and R2 are defined as above with formaldehyde and an alkaline metal cyanide at a pH in the range of about 0 to 2 to produce a tetranitrlle of the formula (III): (NCCH2)2N-CHR1-CHR2-N(CH2CN)2 (III) hydrating said tetranitrile to yield an acid addition salt of a tetraamide of the formula (IV): (H2NOCCH2)2N-CHR1-CHR2-N(CH2CONH2)2 .2HX (IV) where R1 and R2 are defined as in formula (I) and X is an acid anion such as fluoride, chloride, bromide or sulfate but preferably chloride; and reacting said acid addition salt of said tetraamide in a cyclization reaction to yield said compound of the formula (I).

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