Copper-Catalyzed Regioselective C-H Amination of Phenol Derivatives with Assistance of Phenanthroline-Based Bidentate Auxiliary

A copper-catalyzed regioselective direct amination of phenol derivatives with diarylamines via phenanthroline-based bidentate auxiliary-directed C-H cleavage has been developed. This reaction proceeds smoothly with only a copper salt and air as a terminal oxidant to produce the corresponding o-aminophenols in good yields. Moreover, the directing group can be easily attached, detached, and recycled. Additionally, preliminary computational studies of the reaction with DFT have also been performed.Takamatsu K., Hayashi Y., Kawauchi S., et al. Copper-Catalyzed Regioselective C-H Amination of Phenol Derivatives with Assistance of Phenanthroline-Based Bidentate Auxiliary. ACS Catalysis. 9(6), 5336-5344 (2019), 7 June 2019; © 2019 American Chemical Society. https://doi.org/10.1021/acscatal.9b01145

Identification of a Novel ACVRL1 Gene Mutation (c.100T>A, p.Cys34Ser) in a Japanese Patient with Possible Hereditary Hemorrhagic Telangiectasia (Osler-Weber-Rendu Disease)

Hereditary hemorrhagic telangiectasia (HHT; also known as Osler-Weber-Rendu disease) is an autosomal dominant genetic disorder that causes frequent epistaxis, mucocutaneous telangiectasia, and visceral arteriovenous malformations. Four genes (ENG, ACVRL1, SMAD4, and GDF2) have been identified as pathogenic in HHT. We describe the case of a 50-year-old Japanese man highly suspected of having HHT due to recurrent epistaxis, mucocutaneous telangiectasia, and a family history. Genomic analysis revealed a novel missense mutation of c.100T>A, p.Cys34Ser in the patient’s ACVRL1 gene. We used 6 freeware programs to perform an in silico analysis of this mutation. The results demonstrated the mutation’s high pathogenicity

Copper-Mediated Decarboxylative C–H Arylation of Phenol Derivatives with ortho-Nitrobenzoic Acids Using Phenanthroline-Based Bidentate Auxiliary

A copper-mediated decarboxylative C–H arylation of phenol derivatives with ortho-nitrobenzoic acid salts via phenanthroline-directed C–H cleavage has been developed. The N,N-bidentate phenanthroline auxiliary uniquely promotes the reaction only in the presence of a copper salt to produce the corresponding biaryls in acceptable yields. Moreover, the directing group can be easily introduced and removed. Additionally, preliminary computational mechanistic studies with DFT have also been performed.Takamatsu K., Hayashi Y., Kawauchi S., et al. Copper-Mediated Decarboxylative C–H Arylation of Phenol Derivatives with ortho-Nitrobenzoic Acids Using Phenanthroline-Based Bidentate Auxiliary. ChemistrySelect 4, 11833 (2019); https://doi.org/10.1002/slct.201902860