Re: poster 17 : solubility and purification of final compounds

David Riddick (
Thu, 22 Jun 1995 08:22:42 +0000 (GMT)

Dear Martine

There appears to be no solubility problems of either the last intermediate
or eilatin itself. The last intermediate is readily soluble in at least the
following solvents :-

ethyl acetate, chloroform, acetonitrile, THF, xylene, ethanol

Purification of this intermediate is a simple matter of column
chromatography using 10% methanol-chloroform mix.

Note however that clean up of the previous step (DIBAL removal of benzoyl)
is difficult, the compound is extremely unstable to silica gel. Recent
experience (yesterday!!) suggests that for a large scale prep. the product
should immediately be oxidised to the more stable pyridoquinoline.

As yet the biological testing has not been performed, but we expect no
solubility problems, since the compounds are readily soluble in
acetonitrile/water and aqueous ethanol. The initial tests which are
proposed to be carried out are based on DNA unwinding as a test for
intercalator activity.

I hope you find this information useful.

Dave Riddick
Dept. Chemistry
Loughborough University of Technology
LE11 3TU

01509 222589 (work)
01509 265987 (home)
01509 233163 (fax)

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