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Sila-difenidol (6b), a sila-analogue of the drug difenidol (6a), was synthesized according to Scheme 1. 6b and its new precursors 3 and 5 were characterized by their physical and chemical properties, and their structures confirmed by elementary analyses,  1 H NMR and mass spectroscopy. 6 b crystallizes orthorhombic P2 1 2 1 2 1  with a = 11.523(1), b = 14.366(4), c = 11.450(1) Å, Z = 4, D ber  = 1.14 gcm -3 . The structure was refined to R = 0.050 for 1897 reflexions. A strong nearly linear intramolecular O-H···N hydrogen bond of 2.685 Å is observed. The anticholinergic, histaminolytic and musculotropic spasmolytic activities of 6 a and 6 b are reported.

zeitschrift für naturforschung b

Sila-Pharmaka, 14. Mitt.  Darstellung und Eigenschaften sowie Kristall-und Molekülstruktur von Sila-Difenidol /Sila-Drugs,  14 th Communication Preparation and Properties as well as Crystal and Molecular Structure of Sila-Difenidol