On the application of 3d metals for C–H activation toward bioactive compounds: The key step for the synthesis of silver bullets

• Renato L. Carvalho,
• Amanda S. de Miranda,
• Mateus P. Nunes,
• Roberto S. Gomes,
• Guilherme A. M. Jardim and
• Eufrânio N. da Silva Júnior

Beilstein J. Org. Chem. 2021, 17, 1849–1938, doi:10.3762/bjoc.17.126

• site-selective C(sp3)−H bond functionalization strategy (Scheme 28B) [160]. Starting from the abundant feedstock chemical cedrol, oxidation of the gem-dimethyl group was achieved on a gram scale, with the formation of a strained tetrahydrofuran ring. The latter was methylated and eliminated via the

An atom-economical addition of methyl azaarenes with aromatic aldehydes via benzylic C(sp³)–H bond functionalization under solvent- and catalyst-free conditions

• Divya Rohini Yennamaneni,
• Vasu Amrutham,
• Krishna Sai Gajula,
• Rammurthy Banothu,
• Murali Boosa and
• Narender Nama

Beilstein J. Org. Chem. 2020, 16, 3093–3103, doi:10.3762/bjoc.16.259

• , Yaragorla et al. published a review on C(sp3)–H bond functionalization of 2-methylazaarenes [39]. These strategies are proficient, but due to the involvement of drastic reaction conditions, the use of expensive reagents, toxic metals, harmful solvents, and tedious workup procedures, they need to be

Aldehydes as powerful initiators for photochemical transformations

• Maria A. Theodoropoulou,
• Nikolaos F. Nikitas and
• Christoforos G. Kokotos

Beilstein J. Org. Chem. 2020, 16, 833–857, doi:10.3762/bjoc.16.76

• desired products 140n–t in moderate to good yields (Scheme 30). A few months later, the same research group extended this methodology to an α-C(sp3)–H bond functionalization of nitrogen-containing molecules and thioethers [58]. In order to achieve the highest yield, an optimum concentration of acetone (4

Oxidative dehydrogenation of C–C and C–N bonds: A convenient approach to access diverse (dihydro)heteroaromatic compounds

• Santanu Hati,
• Ulrike Holzgrabe and
• Subhabrata Sen

Beilstein J. Org. Chem. 2017, 13, 1670–1692, doi:10.3762/bjoc.13.162

• reacted with o-aminobenzylamine and substituted o-aminobenzylamines to provide the desired products in decent yields (Scheme 8b). Kumar et al. demonstrated transition metal-free α-C(sp3)–H bond functionalization of amines via an oxidative cross-dehydrogenative coupling reaction [44]. They reported a one

Enantioselective carbenoid insertion into C(sp³)–H bonds

• J. V. Santiago and
• A. H. L. Machado

Beilstein J. Org. Chem. 2016, 12, 882–902, doi:10.3762/bjoc.12.87

• primary C(sp3)–H activated bonds even in the presence of activated secondary C(sp3)–H bonds. Another important contribution addressed by this work was the C(sp3)–H bond functionalization of methyl ethers even in the presence of other activated C(sp3)–H bonds. A wide range of methyl ethers were

Recent advances in C(sp³)–H bond functionalization via metal–carbene insertions

• Bo Wang,
• Di Qiu,
• Yan Zhang and
• Jianbo Wang

Beilstein J. Org. Chem. 2016, 12, 796–804, doi:10.3762/bjoc.12.78

• prefer primary C–H bonds (Scheme 5). Such quantitative understanding is very useful for the design of reagent/catalyst combination to achieve high selectivity of unactivated C(sp3)–H bond functionalization. Metal carbene insertion into aliphatic C(sp3)–H bonds of light alkanes Site-selective metal

Cascade alkylarylation of substituted N-allylbenzamides for the construction of dihydroisoquinolin-1(2H)-ones and isoquinoline-1,3(2H,4H)-diones

• Ping Qian,
• Bingnan Du,
• Wei Jiao,
• Haibo Mei,
• Jianlin Han and
• Yi Pan

Beilstein J. Org. Chem. 2016, 12, 301–308, doi:10.3762/bjoc.12.32

• )-diones in good yield. Keywords: C(sp3)–H bond functionalization; cyclization; dihydroisoquinolin-1(2H)-one; N-allylbenzamides; oxidation; Introduction The direct and selective functionalization of an unactivated sp3 C–H bond, which belongs to an effective strategic approach in green and sustainable

Preparation of neuroprotective condensed 1,4-benzoxazepines by regio- and diastereoselective domino Knoevenagel–[1,5]-hydride shift cyclization reaction

• László Tóth,
• Yan Fu,
• Hai Yan Zhang,
• Attila Mándi,
• Katalin E. Kövér,
• Tünde-Zita Illyés,
• Attila Kiss-Szikszai,
• Balázs Balogh,
• Tibor Kurtán,
• Sándor Antus and
• Péter Mátyus

Beilstein J. Org. Chem. 2014, 10, 2594–2602, doi:10.3762/bjoc.10.272

• neuroprotective condensed 2-phenyl-1,4-benzoxazepines rac-7a,b through the diastereoselective domino Knoevenagel–1,5-hydride shift cyclization reaction rac-5→rac-7a,b from the readily available 4-aryl-2-phenyl-1,4-benzoxazepine derivative, rac-5 (Scheme 1). Ring-closure transformations involving C(sp3)–H bond

• functionalization in an internal redox process, particularly involving C–H bonds in α-position to a tertiary amine nitrogen atom, has attracted considerable attention due to its synthetic potential [7][8][9][10][11]. The intramolecular “tert-amino effect” induced cyclization consists in (1) the cleavage of the C