[reaction: see text] The enantioselective [2 + 2] cycloaddition of alkynes possessing an ester functionality and norbornene derivatives proceeded efficiently using a chiral rhodium catalyst. The chiral tri- and tetracyclic cyclobutenes were obtained in moderate to high ee.

A highly enantioselective intermolecular [2 + 2 + 2] cycloaddition of alkynes was catalyzed by a chiral iridium complex. Symmetrical and unsymmetrical diynes, and monoalkynes possessing functional group(s) were subjected to the reaction and various types of axially chiral compounds possessing biaryl skeletons were obtained in good to excellent enantiomeric excesses.

The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases regulates multiple biological processes, such as cell proliferation, migration, apoptosis, and differentiation. Various genetic alterations that drive activation of the receptors and the pathway are associated with tumor growth and survival; therefore, the FGFR family represents an attractive therapeutic target for treating cancer. Here, we report the discovery and the pharmacological profiles of 8 (CH5183284/Debio 1347), an orally available and selective inhibitor of FGFR1, FGFR2, and FGFR3. The chemical modifications, which were guided by 3D-modeling analyses of the inhibitor and FGFRs, led to identifying an inhibitor that is selective to FGFR1, FGFR2, and FGFR3. In in vitro studies and xenograft models in mice, 8 shows antitumor activity against cancer cell lines that harbor genetically altered FGFRs. These results support the potential therapeutic use of 8 as a new anticancer agent.

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Organo-silicon compounds S 0060The Reaction of Butatrienolates with Aldehydes for the Syntheses of α-Vinylidene Acylsilanes.-The addition reaction of lithium butatrienolates, in situ prepared by the 1,4-elimination from 2-butynyl trimethylsilyl ethers (I) along with a retro-Brook rearrangement, with aldehydes (II) affords the β-hydroxy-α-vinylidene acylsilanes (III).-(SHIBATA*, T.; TAKAMI, K.; ARAI, Y.; TSUCHIKAMA, K.; MAEKAWA, S.; Bull. Chem.