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Book Review Einfhrung in die Pharmazeutische Chemie (Introduction to Pharmaceutical Chemistry). By O. E. Schultz

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Experimental
(2a) from (3): Dry HCI is slowly introduced into a refluxed
suspension of 0.01 2 mol PI (R = Me) and 0.01 mol(3) in 60 ml
dry CHCI3 until all the PI has dissolved. The residue obtained
after evaporation of the solvent is distilled in a Kugelrohr
at 85-9ODC/O.0l torr; 2.03g (86%) of ( 2 a ) is obtained as
a colorless oil.-Similarly, with PI, R = C2H5and NR2 = pyrrolidino, 93 % of (2b) and 90 % of (2c), respectively, were
obtained.--(2u) from 1.5): A suspension of 0.045mol PI
(R=CH3) and 0.04mol dichloroacetonitrile in 100ml anhydrous CHC13 is refluxed in the presence of gaseous HC1 until
all the PI has dissolved. Yield after workup (see above): 88 %.
( 4 ) from (3): A solution of 0.01 mol of (3) in 20ml
anhydrous CH2C12 is added to a stirred solution of 0.01 mol
VHA in 40ml of the same solvent at O T , while anhydrous
HC1 is introduced slowly into the reaction mixture (about
one hour at 0°C). The solution is then refluxed for 30min,
the solvent is removed and the residue washed twice with
ether. The yellow powder so obtained is treated with a concentrated solution of K 2 C 0 3 and extracted with CH2CI2.After
drying and removal of the solvent, ( 4 ) is obtained as a white
powder. Yield: 65-75 %.-Hydrochloride of ( 4 ) from (5):
A solution of 0.03mol (5) in 50ml anhydrous CH2C12 is
added dropwise to a solution of 0.03 mol VHA in 80ml anhydrous CH2CI2saturated with dry HC1 and cooled to - 20°C.
After about two hours the mixture is allowed to slowly warm
to room temperature. The solvent is partially removed in
a rotary evaporator, whereupon yellowish needles crystallize
out; yield 60-65 %.
Received: January 30, 1979 [Z 181 lE]
German version: Angew. Chem. 91. 355 (1979)
CAS Registry numbers:
( 2 0 ) . 69668-53-7; ( Z b ) , 69687-68-9; (2c), 69668-54-8; (31, 53472-29-0; ( 4 ) .
69668-55-9; (4/-HCI, 69668-56-0; (S), 3018-12-0; ( 6 ) . HCI, 69668-57-1; (71,
69668-58-2; (X), 69668-59-3; P1.HCI (R=CH3), 69668-60-6; PI.HCI
lR=CzHs), 69668-61-7; PI’HCl (NR,=pyrrolidine), 69668-62-8; VHA’HCI,
3724-43-4; benzamidine, 618-39-3; hydrazine hydrate, 7803-57-8; m-methoxyaniline, 536-90-3
~
~~
~
[l] For a review see Z . Junousek, H . G . Viehe in H . BBhme, H . G . Viiehe:
Iminium Salts in Organic Chemistry. Wiley-Interscience, New York
1976.
[2] For a review see C. Jutz in [I]. p. 225.
[3] Such reactions of nitriles are well-known: B. Stelunder, H. G. Viehe,
Angew. Chem. 89, 182 (1977); Angew. Chem. Int. Ed. Engl. 16, I89
(1977); J . Liebscher, H . Hurtmunn, Collect. Czech. Chem. Commun.
41, 1565 (1976).
[4] J . Perronet, A . TechP, J . Chem. Res. (S) 1978, 43.
BOOK REVIEWS
Einfuhrung in die Pharmazeutische Chemie (Introduction to
Pharmaceutical Chemistry). By 0.E. Schultz. Verlag Chemie,
Weinheim 1978. xvi, 460 pp., 15 figs., 83 tables, bound,
DM 56.00.
New textbooks on pharmaceutical chemistry are welcome,
since there are not many of them in German. As is appropriate
for an introduction, the author has made a representative
selection of the most important pharmaceuticals. The book
is divided into six sections : Central Nervous System, Peripheral
Nervous System, Disinfectants, Substances for the Chemotherapy of Infections and Cytostatics, Organs, and Vitamins. Each
chapter in these sections is introduced by a brief pharmacodynamic or biological characterization of the group of pharmaceuticals, at times with notes on the action mechanism or
on structure-activity relationships. This is followed by a tabular
summary of the substances with tradename, chemical name,
formula, and international abbreviation; next come synthesis
or source (natural products), qualitative tests (identity and
purity), and quantitative determination, together with data
on activity and application.
Even though it is assumed that the reader has some basic
chemical knowledge, reference to the classical reactions of
organic chemistry (e.g. named reactions) is often missing,
as to a certain extent is the clear application of the concepts
of tautomerism and resonance. There is a note in the foreword
stating that in the analytical sections the procedures and
requirements of DAB 7, EuPharm, and some other national
pharmacopeias have been taken into account; nevertheless,
detailed information should still have been given in the text.
In the same way, notes on the areas of agreement and disagreement between the pharmacopeias mentioned would have been
desirable. Further important aspects of pharmaceutical
chemistry are the stability of pharmaceuticals and pharmacokinetic parameters; the latter could stimulate the synthesis
of derivatives.
334
The development of pharmaceutical chemistry from a collection of random observations to a system of systematic research
is not taken into account, though from the didactic viewpoint
this is just as important as the listing of research workers
who have made fundamental contributions to this multidisciplinary field of research. This type of information could have
been included as footnotes or in a table.
There are also some inorganic pharmaceuticals (e.g. lithium
carbonate) that have not been mentioned. In addition (and
this is possibly due to the structure of the book), some important groups of pharmaceuticals get too short a mention (e. g.
anticoagulants) or no mention at all (e. g. analeptics, pentetrazole).
The style of the book is good; the few errors in structural
formulae could easily be corrected in a later edition. The
over-all impression is that this “Introduction” has successfully
extended the range of textbooks in the field of chemistry.
K . E. Schulte [NB 462 IE]
Transient Techniquesin Electrochemistry. By D. D. MacDonald.
Plenum Press, New York-London 1977. 1st edit., xii, 329
pp., numerous illustrations, bound, $45.00.
This book deals with the relaxation phenomena that may
be observed at the electrodes of galvanic cells as the voltage
or current changes with time. Since one can specify either
the current or the voltage as external parameters in a large
number of ways, a variety of experimental techniques has
sprung up, so that it is difficult even for the expert to remember
them all. In this book the author gives an ordered presentation
of such techniques, and in particular chronoamperometry,
chrono-potentiometry, cyclic voltammetry, and alternatingcurrent methods. He places special emphasis on an explanation
of the mathematical principles for the analysis of the reaction
couplings that lead to relaxation phenomena. A good summary
of the expected time lapses is provided, and this will prove
Angew. Chem. Int. Ed. Engl. 18 (1979) N o . 4
0 Verlay Chrmie, CmbH, 6940 Weinheim, 1979
0570-0833/79G404-0334 $ 02.50/0
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