1687-64-5Relevant articles and documents
Miller,Stedman
, p. 1135,1137,1140 (1971)
Synthesis of Highly Substituted Phenols and Benzenes with Complete Regiochemical Control
Zhang, Xiaojie,Beaudry, Christopher M.
supporting information, p. 6086 - 6090 (2020/08/12)
Substituted phenols are requisite molecules for human health, agriculture, and diverse synthetic materials. We report a chemical synthesis of phenols, including penta-substituted phenols, that accommodates programmable substitution at any position. This method uses a one-step conversion of readily available hydroxypyrone and nitroalkene starting materials to give phenols with complete regiochemical control and in high chemical yield. Additionally, the phenols can be converted into highly and even fully substituted benzenes.
PYRIDIN-4-YL DERIVATIVES
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Page/Page column 15, (2014/09/29)
The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immuno
Novel S1P1 receptor agonists - Part 1: From pyrazoles to thiophenes
Bolli, Martin H.,Müller, Claus,Mathys, Boris,Abele, Stefan,Birker, Magdalena,Bravo, Roberto,Bur, Daniel,Hess, Patrick,Kohl, Christopher,Lehmann, David,Nayler, Oliver,Rey, Markus,Meyer, Solange,Scherz, Michael,Schmidt, Gunther,Steiner, Beat,Treiber, Alexander,Velker, J?rg,Weller, Thomas
, p. 9737 - 9755 (2014/01/06)
From a high-throughput screening campaign aiming at the identification of novel S1P1 receptor agonists, the pyrazole derivative 2 emerged as a hit structure. Medicinal chemistry efforts focused not only on improving the potency of the compound but in particular also on resolving its inherent instability issue. This led to the discovery of novel bicyclo[3.1.0]hexane fused thiophene derivatives. Compounds with high affinity and selectivity for S1P1 efficiently reducing the blood lymphocyte count in the rat were identified. For instance, compound 85 showed EC50 values of 7 and 2880 nM on S1P1 and S1P3, respectively, had favorable pharmacokinetic properties in rat and dog, distributed well into brain tissue, and efficiently and dose dependently reduced the blood lymphocyte count in the rat. After oral administration to spontaneously hypertensive rats, the S1P 1 selective compound 85 showed no effect on mean arterial blood pressure and affected the heart rate during the wake phase of the animals only.
