The dearomatization of 2‐naphthols represents a simple method for the construction of complex 3D structures from simple planar starting materials. We describe a cyclopropanation of 2‐naphthols that proceeds via cyclopropene ring‐opening using rhodium and acid catalysis under mild conditions. The vinyl cyclopropane molecules were formed with high chemoselectivity and scalability, which could be further functionalized at different sites. Both computational and experimental evidence were used to elucidate the reaction mechanism.

Nematode parasites of humans and livestock pose a significant burden to human health, economic development, and food security. Anthelmintic drug resistance is widespread among parasites of livestock and many nematode parasites of humans lack effective treatments. Here, we present a nitrophenyl-piperazine scaffold that induces motor defects rapidly in the model nematode Caenorhabditis elegans. We call this scaffold Nemacol and show that it inhibits the vesicular acetylcholine transporter (VAChT), a target recognized by commercial animal and crop health groups as a viable anthelmintic target. We demonstrate that it is possible to create Nemacol analogs that maintain potent in vivo activity whilst lowering their affinity to the mammalian VAChT 10-fold. We also show that Nemacol enhances the ability of the anthelmintic Ivermectin to paralyze C. elegans and the ruminant nematode parasite Haemonchus contortus. Hence, Nemacol represents a promising new anthelmintic scaffold that acts through a validated anthelmintic target.

A dual metal approach enables the use of unsymmetrical diallyl carbonates as viable enolate precursors for allylic alkylation reactions, allowing facile access to various α-quaternary allylated aldehydes and ketones. This methodology features a regioselective Pd-catalyzed decarboxylative oxidative addition, forming an electrophilic Pd π-allyl species and releasing an allylic alkoxide, which undergoes a Rh-catalyzed isomerization to an enolate in situ. Recombination of the Pd π-allyl species and Rhenolate nucleophile then affords the α-quaternary carbonyl compound.

The dearomatization of 2‐naphthols represents a simple method for the construction of complex 3D structures from simple planar starting materials. We describe a cyclopropanation of 2‐naphthols that proceeds via cyclopropene ring‐opening using rhodium and acid catalysis under mild conditions. The vinyl cyclopropane molecules were formed with high chemoselectivity and scalability, which could be further functionalized at different sites. Both computational and experimental evidence were used to elucidate the reaction mechanism.

Objectives: We aimed to investigate if the use of read-out segmented echo planar imaging with additional two-dimensional navigator correction (RESOLVE) for acquiring prostate diffusion weighted imaging (DWI) improves image quality, compared to single-shot echo planar imaging (ss-EPI). Methods: : This IRB-approved, HIPAA-compliant study cohort included 162 consecutive males with suspected prostate cancer, who underwent 3 Tesla multiparametric MRI (3T-mpMRI). Two abdominal radiologists, blinded to clinical information, separately reviewed each 3T-mpMRI study to score geometrical distortion, volume of rectal gas, lesion conspicuity and anatomic details delineation first on ss-EPI and subsequently RESOLVE images using five-point scales (1 = excellent, 5 = poor). Results: There was good-to-excellent inter reader agreement for scoring image quality parameters on both ss-EPI and RESOLVE. Geometrical distortion scores > 3 was seen in 12.3% (20/162) of ss-EPI images, with all having geometrical distortion score <3 on RESOLVE (p < .001). Mean image distortion score was significantly less on RESOLVE than ss-EPI (1.16 vs 1.61, p < .01 regardless of rectal gas, p.05 when stratified by volume of rectal gas degree). RESOLVE was superior to ss-EPI for lesion conspicuity (mean 1.35 vs 1.53, p:.002) and anatomic delineation (2.60 vs 2.68, p:.001). Conclusion: Compared to conventional ss-EPI, the use of RESOLVE for acquisition of prostate DWI resulted in significantly enhanced image quality and reduced geometrical distortion. Advances in knowledge: Readout segmented-EPI could be an alternative or replacement of single shot-EPI for acquiring prostate diffusion-weighted imaging with significantly less geometrical distortion and significantly improved lesion conspicuity and anatomic delineation.