The cyclohexane dicarboxylate unit
of BMS-986251 (1), a potent and efficacious RORγt
inverse agonist, was synthesized
starting from Hagemann’s ester in seven chemical transformations
with five isolated intermediates. The synthesis involved an enzymatic
kinetic resolution, a two-step telescoped enol tosylation followed
by carboxylation using a benign CO surrogate for the installation
of the second carboxylate functionality, and a Crabtree catalyst-mediated
diastereoselective olefin hydrogenation. This process was successfully
demonstrated to produce 3.6 kg of compound 3.
Cu(I)
salts have been shown to improve the regioselectivity and
rate of the Ru-catalyzed alkyne–azide click reaction of internal
alkynes with azides. While Cu and Ru individually provide complementary
regioselectivity in the case of terminal alkynes, the synergistic
effect of these two species in situ significantly improves regiochemical
outcomes in the case of internal alkynes. The substrate scope of these
new reaction conditions is also reported.
In the field of developmental biology embryonic growth is accelerated by specific doses of biological and chemical factors. In the developing countries like India, contamination of metallic components like copper sulphate through food chain became serious issue to disturb developmental features of animals. Among vertebrates, chick embryo of Gallus gallus has dynamic features during development. Copper sulphate has been found to contaminate and bio-concentrate in the embryological tissues of experimental model Gallus gallus. A time-dependent exposure of copper sulphate up to five days of incubation showed prominent alterations in vascularisation and angiogenesis of developing embryo. The present investigation focus about egg weight and altered angiogenesis of avian embryo Gallus gallus after exposure to copper sulphate.
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