Copyright © 1996, 1997, 2001
by Galen Daryl Knight and VitaleTherapeutics, Inc.
PITFALLS IN SYNTHESIZING VITALETHEINE MODULATORS
by Galen D. Knight, Ph. D., President of VitaleTherapeutics, Inc.
This is a draft of a paper designed to clear up some misconceptions
about the vitaletheine modulators and their syntheses. Evolution of this
paper to its final form will demonstrate the versatility of this approach
to scientific publication in which corrections for inaccuracies and new
insights can be readily incorporated into the existing framework of the
article.
Abstract
The expected controversy over the vitaletheine modulators has finally emerged
with some largely unsupported allegations that the exemplary compounds
are sulfonates. This is offset to some extent by reports from another group
and by a local chemical company that they have succeeded in repeating the
synthesis of at least some of the vitaletheine modulators. In addition,
evidence confirming the structural assignments has been generated on samples
of the authentic compounds by scientists at Los Alamos National Laboratories.
While these studies confirming the biological activities of these compounds
at a major university and at a national cancer center are being readied
for publication, salient features of these compounds and their activities
will be mentioned in this report to help researchers overcome any difficulties
they may have with their production, characterization, and study of these
compounds. By necessity, the major focus of this article will be upon the
controversial structures for the sulfenate-linked benzyl derivative and
vitaletheine V4, but difficulties in synthesizing and characterizing vitalethine
also will be addressed. Since it took approximately five years to develop
a synthetic protocol that makes vitalethine, including attempts in about
30 different solvent systems, even minor departures from the established
protocol must be considered as something other than a serious effort to
make the compound. In developing an understanding of the pitfalls for their
syntheses and of other inadvertent interconversions and decompositions
by these three substances, one can begin to appreciate their full potential
for therapeutic intervention and their value in estimating the environmental
hazards of biological and chemical agents that interfere with the activities
of the vitaletheine modulators.
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