Continuous-flow carbonyl hydrogenation under subatmospheric to atmospheric hydrogen pressure enabled by robust heterogeneous Pt–Fe catalysts

• Hiroyuki Miyamura,
• Ryosuke Kajiyama,
• Shun-ya Onozawa,
• Yoshihiro Kon and
• Shū Kobayashi

Beilstein J. Org. Chem. 2026, 22, 575–582, doi:10.3762/bjoc.22.43

• as functional materials and pharmaceuticals [1][2][3][4]. While stoichiometric reagents and catalytic methods are widely developed for this transformation, one of the most ideal methods is heterogeneous catalysis using molecular hydrogen as a reductant, which realizes 100% atom economy [5][6][7][8][9

Experimental and DFT studies on the regioselective methanolysis of 5-azido-9-oxabicyclo[6.1.0]nonan-4-yl 4-nitrobenzoate isomers

• İlknur Polat,
• Selçuk Eşsiz and
• Emine Salamci

Beilstein J. Org. Chem. 2026, 22, 547–556, doi:10.3762/bjoc.22.40

• azidomorphine (4) are utilized as pharmaceuticals (Figure 1) [1][6][7][8][9]. Additionally, recent studies demonstrated that nonglycosyl azides hamper glycan acceptance by carbohydrate-processing enzymes [10][11]. Moreover, azido sugars are used directly in cell biology studies. Therefore, synthetic

Recent advances in the stereoselective synthesis of distal biaxially chiral molecules

• Fanxing Zhou,
• Chen Zhang,
• Lingyu Sun,
• Yiyun Fang,
• Siming Zheng,
• Lina Hu,
• Mengyang Shen,
• Zhen Zhao,
• Wei Xu,
• Yunqiang Sun and
• Zi-Qiang Rong

Beilstein J. Org. Chem. 2026, 22, 461–479, doi:10.3762/bjoc.22.34

• axes, it constitutes a bi- or multiaxial chiral system, significantly increasing structural complexity and stereochemical diversity, which endows the molecules with unique functionalities and excellent performance in catalysis, pharmaceuticals [33], and materials science [34]. In 1989, Hayashi

Dialkylaminoalkylation of β-ketosulfones via ring-opening of 3-sulfonylpyrrolidines

• Evgeny M. Buev,
• Alexander V. Pavlushin,
• Vladimir S. Moshkin and
• Vyacheslav Y. Sosnovskikh

Beilstein J. Org. Chem. 2026, 22, 383–389, doi:10.3762/bjoc.22.26

• broad spectrum of pharmacological activities [1][2][3] and synthetic potential [4][5]. Also noteworthy are γ-aminosulfones, which form the backbone of important pharmaceuticals including the antiglaucoma drug dorzolamide [6], acamprosate for alcohol craving suppression [7], and bicalutamide, an

• antiandrogen cancer treatment [8][9] (Figure 1). Moreover, aminosulfones remain a privileged scaffold in the ongoing development of new methods for the synthesis of pharmaceuticals [10][11][12], with multiple research compounds showing promising bioactivities such as MMP inhibition [13], antiinflammatory

Recent advances in the cleavage of non-activated amides

• Eun-Sol Choi and
• Hyo-Jun Lee

Beilstein J. Org. Chem. 2026, 22, 352–369, doi:10.3762/bjoc.22.23

• Eun-Sol Choi Hyo-Jun Lee Department of Chemistry, Kunsan National University, Gunsan 54150, Republic of Korea 10.3762/bjoc.22.23 Abstract The amide bond is one of the most fundamental and widely utilized functional groups in organic chemistry, central to the structures of pharmaceuticals

Arene activation via π-bond localization: concepts and opportunities

• Paul Meiners,
• Julian J. Melder and
• Tobias Morack

Beilstein J. Org. Chem. 2026, 22, 257–273, doi:10.3762/bjoc.22.19

• building blocks in pharmaceuticals, agrochemicals, and materials science (Figure 1B). In contrast, direct modification of the central aromatic core, i.e., controlled disruption of aromaticity, remains a fundamental challenge in synthetic chemistry and leaves the vast potential of planar arenes as

Circumventing Mukaiyama oxidation: selective S–O bond formation via sulfenamide–alcohol coupling

• Guoling Huang,
• Huarui Zhu,
• Shuting Zhou,
• Wanlin Zheng,
• Fangpeng Liang,
• Zhibo Zhao,
• Yifei Chen and
• Xunbo Lu

Beilstein J. Org. Chem. 2026, 22, 158–166, doi:10.3762/bjoc.22.9

• its multiple oxidation states and ability to form diverse bonds with carbon, nitrogen, and oxygen. This versatility underpins the pivotal roles of organosulfur compounds in pharmaceuticals, catalysis, and materials science [1][2][3][4]. Among these, sulfilimines (R2S=NR') have attracted growing

Asymmetric Mannich reaction of aromatic imines with malonates in the presence of multifunctional catalysts

• Kadri Kriis,
• Harry Martõnov,
• Annette Miller,
• Mia Peterson,
• Ivar Järving and
• Tõnis Kanger

Beilstein J. Org. Chem. 2026, 22, 151–157, doi:10.3762/bjoc.22.8

• been used in the synthesis of numerous pharmaceuticals and natural products [7]. The application of asymmetric synthesis enables access to enantiomerically pure targets. Earlier, metal catalysis was used for Mannich reactions [8][9], but in recent years, methods of asymmetric organocatalysis have been

Total synthesis of natural products based on hydrogenation of aromatic rings

• Haoxiang Wu and
• Xiangbing Qi

Beilstein J. Org. Chem. 2026, 22, 88–122, doi:10.3762/bjoc.22.4

• dehydrogenase type 1 (11-β-HSD-1), a key enzyme that alleviates insulin resistance by lowering cortisol production. Compound 157 emerged as a promising 11-β-HSD-1 inhibitor candidate. In 2016, researchers from Boehringer Ingelheim Pharmaceuticals and the University of Pennsylvania reported a concise and

Advances in Zr-mediated radical transformations and applications to total synthesis

• Hiroshige Ogawa and
• Hugh Nakamura

Beilstein J. Org. Chem. 2026, 22, 71–87, doi:10.3762/bjoc.22.3

• where organic synthesis plays a central role, including pharmaceuticals, agrochemicals, materials chemistry, organic semiconductors, and organic thin-film solar cells. These areas are intimately linked to human life; thus, advances in organic synthesis are essential for improving human well-being

Synthesis and applications of alkenyl chlorides (vinyl chlorides): a review

• Daniel S. Müller

Beilstein J. Org. Chem. 2026, 22, 1–63, doi:10.3762/bjoc.22.1

• caliche deposits in Chile [2]. This concentration of supply raises potential concerns regarding long-term availability and geopolitical vulnerability. Recent interest in alkenyl chlorides has been driven by their occurrence in bioactive natural products (Figure 1) [3][4][5], pharmaceuticals (Figure 2) [6

• Vertex Pharmaceuticals describes the synthesis of alkenyl chloride 21 on a 360 and 580 mmol scale (Scheme 6A) [51]. The addition of a few drops of DMF was not commented. Surprisingly a significant decrease in yield was observed at the larger 580 mmol scale compared to the 360 mmol scale. Scott reported a

Sustainable electrochemical synthesis of aliphatic nitro-NNO-azoxy compounds employing ammonium dinitramide and their in vitro evaluation as potential nitric oxide donors and fungicides

• Alexander S. Budnikov,
• Nikita E. Leonov,
• Michael S. Klenov,
• Andrey A. Kulikov,
• Igor B. Krylov,
• Timofey A. Kudryashev,
• Aleksandr M. Churakov,
• Alexander O. Terent’ev and
• Vladimir A. Tartakovsky

Beilstein J. Org. Chem. 2025, 21, 2739–2754, doi:10.3762/bjoc.21.211

• phytopathogenic fungi. Keywords: ammonium dinitramide; antifungal agents; azoxy compounds; electrosynthesis; NO donors; Introduction Organic compounds containing N–N and N–O bonds are ubiquitous in diverse fields, including pharmaceuticals, agrochemicals, natural products [1][2][3][4], as well as in

Synthesis of new tetra- and pentacyclic, methylenedioxy- and ethylenedioxy-substituted derivatives of the dibenzo[c,f][1,2]thiazepine ring system

• Gábor Berecz,
• András Dancsó,
• Mária Tóthné Lauritz,
• Loránd Kiss,
• Gyula Simig and
• Balázs Volk

Beilstein J. Org. Chem. 2025, 21, 2645–2656, doi:10.3762/bjoc.21.205

• Gabor Berecz Andras Dancso Maria Tothne Lauritz Lorand Kiss Gyula Simig Balazs Volk Egis Pharmaceuticals Plc., Directorate of Drug Substance Development, P. O. Box 100, H-1475 Budapest, Hungary HUN-REN Research Centre for Natural Sciences, Institute of Organic Chemistry, Stereochemistry Research

Visible-light-driven NHC and organophotoredox dual catalysis for the synthesis of carbonyl compounds

• Vasudevan Dhayalan

Beilstein J. Org. Chem. 2025, 21, 2584–2603, doi:10.3762/bjoc.21.200

• ; NHC; organic photocatalyst; radicals; visible-light; Introduction Over the last ten years, NHC-catalyzed visible-light-promoted radical chemistry has been extensively developed for the cost-effective and practical synthesis of bioactive intermediates, pharmaceuticals, drugs, and natural products [1

• continued integration of this versatile photocatalytic platform with sustainable methods such as visible-light harvesting and the use of earth-abundant catalysts is expected to further enhance its impact across diverse research fields, including chemical biology, pharmaceuticals, agrochemicals, polymers

• mild conditions, using sustainable methods with low-cost materials, and using non-toxic reagents. Its proven potential includes medicinal chemistry, pharmaceuticals, materials science, and the late-stage functionalization of complex bioactive molecules. Recent synthetic advances in methodology

Catalytic enantioselective synthesis of selenium-containing atropisomers via C–Se bond formations

• Qi-Sen Gao,
• Zheng-Wei Wei and
• Zhi-Min Chen

Beilstein J. Org. Chem. 2025, 21, 2447–2455, doi:10.3762/bjoc.21.186

• Atropisomers are not only prevalent in biologically active natural products and pharmaceuticals, but they have also garnered increasing attention for their effectiveness as ligands and catalysts in the field of catalytic asymmetric synthesis. Asymmetric catalysis serves as a key strategy for the

Insoluble methylene-bridged glycoluril dimers as sequestrants for dyes

• Suvenika Perera,
• Peter Y. Zavalij and
• Lyle Isaacs

Beilstein J. Org. Chem. 2025, 21, 2302–2314, doi:10.3762/bjoc.21.176

• textile, leather, paint, plastic, cosmetics, pharmaceuticals, and food industries [4]. It has been estimated that about 7 × 106 tons of dyes (e.g., methylene blue, rhodamine B, methyl orange, Congo red, disperse violet 26, methyl red, crystal violet) are produced annually worldwide [5]. Many dyes are

• functionalized and can flex their methylene-bridged glycoluril oligomer to accommodate guests of different size. Water-soluble acyclic CB[n] have been used as in vivo sequestrants for drugs of abuse, neuromuscular blockers, and anesthetics and as solubilizing agents for pharmaceuticals [31][32][33][34][35][36

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

• significant reaction, 1,n-enyne cyclization is capable of constructing a variety of complex small-molecule frameworks, including fused and bridged rings, thereby serving as a potent tool in the syntheses of natural products and pharmaceuticals. Our group has pioneered the concept of "pathway economy" by

Thiadiazino-indole, thiadiazino-carbazole and benzothiadiazino-carbazole dioxides: synthesis, physicochemical and early ADME characterization of representatives of new tri-, tetra- and pentacyclic ring systems and their intermediates

• Gyöngyvér Pusztai,
• László Poszávácz,
• Anna Vincze,
• András Marton,
• Ahmed Qasim Abdulhussein,
• Judit Halász,
• András Dancsó,
• Gyula Simig,
• György Tibor Balogh and
• Balázs Volk

Beilstein J. Org. Chem. 2025, 21, 2220–2233, doi:10.3762/bjoc.21.169

• Technology and Economics, Műegyetem rkp. 3, H-1111 Budapest, Hungary Egis Pharmaceuticals Plc., Directorate of Drug Substance Development, P.O. Box 100, H-1475 Budapest, Hungary Department of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre u. 9, H-1092 Budapest, Hungary Ambimass Ltd., Záhony u

Electrochemical cyclization of alkynes to construct five-membered nitrogen-heterocyclic rings

• Lifen Peng,
• Ting Wang,
• Zhiwen Yuan,
• Bin Li,
• Zilong Tang,
• Xirong Liu,
• Hui Li,
• Guofang Jiang,
• Chunling Zeng,
• Henry N. C. Wong and
• Xiao-Shui Peng

Beilstein J. Org. Chem. 2025, 21, 2173–2201, doi:10.3762/bjoc.21.166

• of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P. R. China 10.3762/bjoc.21.166 Abstract Organic five-membered rings have shown significant applications in the fields of organic synthesis, natural products, organic materials and pharmaceuticals for their unique

• organic synthesis [1][2][3][4][5][6][7][8][9][10][11][12][13][14] but also are critical moieties in natural products [15][16][17][18], organic materials [19] and pharmaceuticals [20][21][22][23][24] due to their unique chemical, electrical, optical, pharmacological and biological properties. Gracilioether

• alkynes bearing heteroatoms such as ynamides and thioalkynes would be enhanced in future research; (2) since axial chirality is critical in natural products and pharmaceuticals, it would be significant to apply the electrochemical annulation of alkynes in formation of organic rings with axial chirality

C2 to C6 biobased carbonyl platforms for fine chemistry

• Jingjing Jiang,
• Muhammad Noman Haider Tariq,
• Florence Popowycz,
• Yanlong Gu and
• Yves Queneau

Beilstein J. Org. Chem. 2025, 21, 2103–2172, doi:10.3762/bjoc.21.165

• -designed Pd@S-1 and H-beta zeolite catalytic system, exhibiting high resistance to coking in presence of NH3. Subsequent carboxylation with CO2 and hydrogenation over Rh/C as catalyst led to racemic proline, an important precursor for pharmaceuticals, in quantitative yield. ᴅ-Proline was then obtained in

• , pharmaceuticals or high added value chemicals [215][216][217][218][219][220][221][222][223]. Its first commercial production began in the 1940s. Its preparation from biomass involves several different possible pathways. One is the C5 sugar route starting from xylose as an example, relying on acid hydrolysis of

• , amides, lactones, acrylic acid, etc. (Scheme 72) and is therefore a key intermediate in the synthesis of pharmaceuticals, agrochemicals, and other specialty chemicals. Levulinate esters, used as a solvent or as biofuels, are obtained by esterification under acid catalysis, e.g., with a sulfuric acid

Measuring the stereogenic remoteness in non-central chirality: a stereocontrol connectivity index for asymmetric reactions

• Ivan Keng Wee On,
• Yu Kun Choo,
• Sambhav Baid and
• Ye Zhu

Beilstein J. Org. Chem. 2025, 21, 1995–2006, doi:10.3762/bjoc.21.155

• important in pharmaceuticals, catalysts, and advanced materials due to their unique stereogenic scaffolds and associated properties. Consequently, synthetic chemists have been pursuing molecules featuring these forms of non-central chirality, where the stereogenic elements are not localized on a single

Thermodynamics and polarity-driven properties of fluorinated cyclopropanes

• Matheus P. Freitas

Beilstein J. Org. Chem. 2025, 21, 1742–1747, doi:10.3762/bjoc.21.137

• to modulate properties that enhance the performance of pharmaceuticals and materials. This quantum-chemical study explores the energetic implications of fluorinating cyclopropane, providing insights into molecular characteristics arising from the polar C–F bond. Isodesmic reactions revealed that the

• prevents ring interconversion, unlike its larger analogs. It is widely used in pharmaceuticals and has attracted significant interest in medicinal chemistry, particularly when fluorinated [1][2][3][4][5][6]. The highly polar C–F bond in fluorinated cyclopropanes destabilizes the ring and alters its overall

• intramolecular forces in fluorinated systems but also provide a molecular framework for the design of advanced applications. Fluorinated cyclopropanes exhibit considerable potential in pharmaceuticals, where polarity influences drug solubility and activity, and in material sciences, particularly for the

Continuous-flow-enabled intensification in nitration processes: a review of technological developments and practical applications over the past decade

• Feng Zhou,
• Chuansong Duanmu,
• Yanxing Li,
• Jin Li,
• Haiqing Xu,
• Pan Wang and
• Kai Zhu

Beilstein J. Org. Chem. 2025, 21, 1678–1699, doi:10.3762/bjoc.21.132

• closely tied to the application fields of the resulting nitration compounds, with significant variations in production demands across industries. For high-value, low-volume sectors such as flavors and fragrances and pharmaceuticals, typical production scales fall within tens to hundreds of tons per year

Influence of the cation in hypophosphite-mediated catalyst-free reductive amination

• Natalia Lebedeva,
• Fedor Kliuev,
• Olesya Zvereva,
• Klim Biriukov,
• Evgeniya Podyacheva,
• Maria Godovikova,
• Oleg I. Afanasyev and
• Denis Chusov

Beilstein J. Org. Chem. 2025, 21, 1661–1670, doi:10.3762/bjoc.21.130

• of the most actively applied reductants with phosphorus-hydrogen bond in industry, for example, in production of polymers [1], pharmaceuticals [2], electroless plating [3], metal corrosion prevention [4] and even food preservation [5]. NaH2PO2 is a non-toxic (LD50 7640 mg/kg – rat) (SDS Thermo Fisher

High-pressure activation for the solvent- and catalyst-free syntheses of heterocycles, pharmaceuticals and esters

• Kelsey Plasse,
• Valerie Wright,
• Guoshu Xie,
• R. Bernadett Vlocskó,
• Alexander Lazarev and
• Béla Török

Beilstein J. Org. Chem. 2025, 21, 1374–1387, doi:10.3762/bjoc.21.102