Pathway economy in cyclization of 1,n-enynes

• Hezhen Han,
• Wenjie Mao,
• Bin Lin,
• Maosheng Cheng,
• Lu Yang and
• Yongxiang Liu

Beilstein J. Org. Chem. 2025, 21, 2260–2282, doi:10.3762/bjoc.21.173

• synthesis; 1,n-enynes; pathway economy; small-molecule skeletons; Introduction As organic synthesis concepts continue to evolve, economical synthesis remains a foundational principle for synthetic chemists [1][2][3][4][5][6][7]. The essence of economical synthesis lies in the conservation of materials and

• copper-catalyzed tandem process initiated by endo-cyclization of indolyl homopropargyl amides, enabling atom-economical synthesis of therapeutically significant bridged aza[n.2.1] skeletons. Angle strain and configuration-controlled cyclization of 1,n-enynes In cyclization reactions, angle strain and

• accelerating reaction optimization. Furthermore, expanding this concept to other reaction manifolds – such as electrocyclic processes and photoredox catalysis – may uncover new avenues for molecular innovation. The pursuit of pathway-economical synthesis represents a paradigm shift toward sustainable and

Understanding the origin of stereoselectivity in the photochemical denitrogenation of 2,3-diazabicyclo[2.2.1]heptene and its derivatives with non-adiabatic molecular dynamics

• Leticia A. Gomes and
• Steven A. Lopez

Beilstein J. Org. Chem. 2025, 21, 2007–2020, doi:10.3762/bjoc.21.156

• ). Housane derivatives were also used in an atom-economical synthesis of the antibiotic [42][43][44] and potentially anti-obesity drug [45][46][47][48][49], (±)-vibralactone [42] (Scheme 1d). The thermolysis [50][51][52][53][54][55][56][57][58][59][60] and photolysis [57][58][60][61][62][63][64][65][66][67

Metal-catalyzed coupling/carbonylative cyclizations for accessing dibenzodiazepinones: an expedient route to clozapine and other drugs

• Amina Moutayakine and
• Anthony J. Burke

Beilstein J. Org. Chem. 2024, 20, 193–204, doi:10.3762/bjoc.20.19

• review in 2018 focused on a variety of routes to these compounds [8]. The well-known Buchwald–Hartwig (B–H) and Chan–Lam (C–L) reactions have proven to be highly useful procedures that allow the step-economical synthesis of diverse biologically relevant heterocycles through C–N bond formation [9]. These

Six-fold C–H borylation of hexa-peri-hexabenzocoronene

• Mai Nagase,
• Kenta Kato,
• Akiko Yagi,
• Yasutomo Segawa and
• Kenichiro Itami

Beilstein J. Org. Chem. 2020, 16, 391–397, doi:10.3762/bjoc.16.37

• showed that the boryl groups increased the energies of frontier molecular orbitals and decreased the HOMO–LUMO energy gap. Compound 1 will contribute to a step-economical synthesis of various HBC derivatives as a platform, and furthermore, the currently developed borylation method gives insight into the

A green, economical synthesis of β-ketonitriles and trifunctionalized building blocks from esters and lactones

• Daniel P. Pienaar,
• Kamogelo R. Butsi,
• Amanda L. Rousseau and
• Dean Brady

Beilstein J. Org. Chem. 2019, 15, 2930–2935, doi:10.3762/bjoc.15.287

Latest development in the synthesis of ursodeoxycholic acid (UDCA): a critical review

• Fabio Tonin and
• Isabel W. C. E. Arends

Beilstein J. Org. Chem. 2018, 14, 470–483, doi:10.3762/bjoc.14.33

• the purification processes necessary to eliminate byproducts formed at each step of reaction involved. All this extends the time, increases costs and decreases production yields. Therefore, research nowadays is geared towards more economical synthesis methods that are waste-free and safe to operate

Mechanochemical synthesis of small organic molecules

• Tapas Kumar Achar,
• Anima Bose and
• Prasenjit Mal

Beilstein J. Org. Chem. 2017, 13, 1907–1931, doi:10.3762/bjoc.13.186

• covers a wide range of research areas and generally deals with 12 principles [5][6] and few of them are: avoiding the use of volatile and toxic solvents, reducing the quantity of catalyst and reagents, using environmentally benign chemicals, atom-economical synthesis, minimization of chemical-waste

Recent advances in copper-catalyzed C–H bond amidation

• Jie-Ping Wan and
• Yanfeng Jing

Beilstein J. Org. Chem. 2015, 11, 2209–2222, doi:10.3762/bjoc.11.240

• ideal model of modern organic synthesis, the direct functionalization of inactivated C–H bonds has been proved to be a promising tool to enable atom and step economical synthesis. Inspired by the splendid advances that have taken place in the chemistry of C–H activation, the synthesis of amides has

Copolymerization and terpolymerization of carbon dioxide/propylene oxide/phthalic anhydride using a (salen)Co(III) complex tethering four quaternary ammonium salts

• Jong Yeob Jeon,
• Seong Chan Eo,
• Jobi Kodiyan Varghese and
• Bun Yeoul Lee

Beilstein J. Org. Chem. 2014, 10, 1787–1795, doi:10.3762/bjoc.10.187

• the preparation of 1 on a large scale have been overcome, and an economical synthesis on the 100 kg scale has been achieved [14][15][16], along with precise control of the molecular weight and chain topology, facilitating the applications of these attractive materials [14][17][18][19]. Now, the

Copper-catalyzed CuAAC/intramolecular C–H arylation sequence: Synthesis of annulated 1,2,3-triazoles

• Rajkumar Jeyachandran,
• Harish Kumar Potukuchi and
• Lutz Ackermann

Beilstein J. Org. Chem. 2012, 8, 1771–1777, doi:10.3762/bjoc.8.202

• only accomplished with more expensive palladium [55][56][57][58][59][60][61][62] or ruthenium [63][64][65][66] catalysts. Notably, this strategy allowed for the atom-economical synthesis of fully substituted 1,2,3-triazoles in a highly regioselective fashion [54][67]. While the research groups of

N-Heterocyclic carbene-catalyzed direct cross-aza-benzoin reaction: Efficient synthesis of α-amino-β-keto esters

• Takuya Uno,
• Yusuke Kobayashi and
• Yoshiji Takemoto

Beilstein J. Org. Chem. 2012, 8, 1499–1504, doi:10.3762/bjoc.8.169

• , and atom-economical synthesis of the α-amino-β-keto esters by NHC-catalyzed cross-aza-benzoin reaction of aldehydes with α-imino esters under mild basic conditions. Results and Discussion First we initiated the cross-aza-benzoin reaction of benzaldehyde (1a) by employing 20 mol % of commercially

2-Allylphenyl glycosides as complementary building blocks for oligosaccharide and glycoconjugate synthesis

• Hemali D. Premathilake and
• Alexei V. Demchenko

Beilstein J. Org. Chem. 2012, 8, 597–605, doi:10.3762/bjoc.8.66

• ]. Additionally, 4-pentenol is rather expensive ($ 323/50 g, Aldrich), and although O-pentenyl can be introduced from the anomeric acetate directly, the most economical synthesis includes a three-step protocol, with halide, orthoester, and the rearrangement of the latter to glycoside. Results and Discussion As a