- Pd/Cu-catalyzed oxidative C-H alkenylation of imidazo[1,2-α]pyridines
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A novel direct and regioselective Pd/Cu-catalyzed intermolecular oxidative coupling of imidazo[1,2-α]pyridines with alkenes was successfully developed. The scope and limitations of the reaction were further studied by using various alkenes. This method pr
- Koubachi, Jamal,Berteina-Raboin, Sabine,Mouaddib, Abderrahim,Guillaumet, Gerald
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experimental part
p. 271 - 276
(2009/06/27)
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- Studies on novel bone resorption inhibitors. ii.1 synthesis and pharmacological activities of fused aza-heteroarylbisphosphonate derivatives2
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Two new series of fused aza-heteroarylbisphosphonates (5, 8), which are structurally quite different from incadronate (YM175), and related compounds were synthesized and evaluated for antiresorptive activity using a parathyroid hormone(PTH)-induced hypercalcemia model in rats (PIH model). Among these compounds, several exhibited more potent antiresorptive activity than pamidronate. In particular, [l-hydroxy-2-(imidazo|l,2a)pyridin-3-yl)ethylidene|bisphosphonic acid (5b, minodronate) was 100-fold more potent than pamidronate in not only the PIH model, but also in an immobilization bone atrophy model in rats (DA model), and was selected for clinical development. The structure-activity relationships in these new series of bisphosphonates are discussed. 1998 Pharmaceutical Society of Japan.
- Takeuchi, Makoto,Sakamoto, Shuichi,Kawamuki, Kousei,Kurihara, Hiroyuki,Nakahara, Hideaki,Isomura, Yasuo
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p. 1703 - 1709
(2007/10/03)
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