Synthetic Efforts toward the Synthesis of a Fluorinated Analog of 5-Aminolevulinic Acid: Practical Synthesis of Racemic and Enantiomerically Defined 3-Fluoro-5-aminolevulinic Acid.

In 2017, the FDA authorized 5-aminolevulinic acid (5-ALA) for intraoperative optical imaging of suspected high-grade gliomas. This was the first authorized optical imaging agent for brain tumor surgery to enhance the visualization of malignant tissue. Herein we report the synthesis of a racemic and enantiopure fluorinated analog of 5-ALA, i.

Concise and Scalable Radiosynthesis of (+)-[F]MDL100907 as a Serotonin 5-HT Receptor Antagonist for PET.

5-Hydroxytryptamine (5-HT) receptors play an important role in several psychiatric disorders. In order to investigate the serotonin (5-HT) receptor , reliable syntheses are required for positron emission tomography (PET) 5-HT radioligands. Owing to the excellent properties of [F]MDL100907 for PET, there has been great interest to develop a novel synthetic route for [F]MDL100907.

Syntheses of 2-Aroyl Benzofurans through Cascade Annulation on Arynes.

The highly efficient and expedient route for the syntheses of 2-aroyl benzofurans has been developed via the cascade [2+2] followed by a [4+1] annulation on arynes. The overall transformation proceeded through the formation of ortho-quinone methide by the insertion of transient aryne into N, N-dimethylformamide and subsequent trapping with sulfur ylide. Moreover, this transformation has a broad range of substrate scope with a high functional-group tolerance.

Cp*Co(III)-Catalyzed C-H Functionalization Cascade of N-Methoxyamides with Alkynedione for the Synthesis of Indolizidines.

Cp*Co(III)-catalyzed C-H functionalization cascade of N-methoxyamides with alkynedione has been reported for the synthesis of indolizidine scaffolds under redox-neutral conditions. The reaction displays broad functional group tolerance along with excellent yield. The reaction proceeds with kinetically relevant C-H bond activation through carboxylate assistance with excellent diastereoselectivity and complete opposite selectivity with respect to alkyne insertion.