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Acta Cryst. (1994). BS0, 746--762
The Influence of the Nitro Group on the Solid-State Structure of 4-Nitropyrazoles:
the Cases of Pyrazole, 3,5-Dimethylpyrazole, 3,5-Di-tert-butylpyrazole and
3,5-Diphenylpyrazole. I. Static Aspects (Crystallography and Thermodynamics)
BY ANTONIO L. LLAMAS-SAIZ, CONCEPCI6N FOCES-FOCES AND FI~LIX H. CANO
Departamento de Cristalograffa, Instituto de Qufmica-Ffsica 'Rocasolano', CSIC, Serrano 119,
E-28006 Madrid, Spain
PILAR JIMI~MEZ AND JOSI~ LAYNEZ
Instituto de Qulmica-Ffsica 'Rocasolano', CSIC, Serrano 199, E-28006 Madrid, Spain
WIM MEUTERMANS AND Josl~ ELGUERO
Instituto de Qufmica Mddica, CSIC, Juan de la Cierva 3, E-28006 Madrid, Spain
AND HANS-HEINRICH LIMBACH AND FRANCISCO AGUILAR-PARRILLA
Institut ffir Organische Chemie, Fachbereich Chemie, Freie Universitdt Berlin, Takustrasse 3,
D-14195 Berlin, Germany
(Received 31 January 1994; accepted 19 April 1994)
Abstract
We have determined the enthalpies of sublimation of
3,5-di-tert-butylpyrazole (3), 3,5-diphenylpyrazole
(4), 4-nitropyrazole (5), 3,5-dimethyl-4-nitropyrazole
(6), 3,5-di-tert-butyl-4-nitropyrazole (7) and 3,5-
diphenyl-4-nitropyrazole (8); those of pyrazole (1)
and 3,5-dimethylpyrazole (2) were already known.
The effect of the C-substituents (Me, Bu t, Ph and
NO2) on the enthalpies of sublimation of pyrazoles
and benzenes are additive and linearly related. More-
over, we report the structure of three of these 4-
nitropyrazole derivatives, (5), (7) and (8), which have
been solved by X-ray crystallography; those of the
remaining five compounds were already known.
Except for (8), there appears to be an opening of the
intramolecular angle at C(4) due to the presence of
the nitro group, that, on the other hand, seems to
have no correlation with the presence of the hydro-
gen H(I)/H(2) disorder. Crystal structure diagrams
and intermolecular contacts were analysed for either
© 1994 International Union of Crystallography
Printed in Great Britain - all rights reserved
pyrazole derivatives with and without nitro sub-
stituents. There appear to be two general modes of
packing: the first is based upon a secondary structure
of trimers in sheets, which distorts into helices; the
second is made of dimers, which then pack into
sheets. The nitro group seems to have no influence in
the packing, which is more controlled by the sub-
stituents at C(3) and C(5). Although only partly
successful, we have established some relationships
between crystallographic results and thermodynamic
properties. First, between the planarity or not of the
4-nitro group and the acid and basic pKa's, and
second, between some packing descriptors and the
sublimation enthalpies.
Introduction
We are in the process of carrying out a systematic
study of the properties of NH-pyrazoles in the solid
state by X-ray crystallography (Llamas-Saiz, Foces-
Acta Crvstallographica Section B
ISSN 0108-7681 ©1994