Construction of CF₂ moieties in FDA-approved drugs (2016–2025): industrial routes, mechanisms, and scale-up considerations

• Wenyan Yao,
• Huanhuan Zhang,
• Xiaolong Yang and
• Feng Liu

Beilstein J. Org. Chem. 2026, 22, 1122–1150, doi:10.3762/bjoc.22.91

• applicability in industrial production. The analysis shows that for alkyl-CF2 groups, the industry strongly favors preformed CF2 building blocks or indirect fluorination strategies to avoid hazardous reagents and harsh conditions. Continuous flow technology using SF4 has emerged as an important complement to

• structure [64]. However, these methods involve reagents that are either relatively expensive (TMSCF2X) or highly hazardous (BrF3), which may limit their practicality at production scale. Currently, the more commonly reported strategy in industry is the use of ClCF2COONa as a difluorocarbene precursor

• in the chemical industry and the risks are controllable. Routes b and c use the CSCl2/AgF method to construct the CF2 group in the difluorobenzodioxole ring, which is relatively mild. However, the special pretreatment required for silver fluoride needs comprehensive evaluation for industrial

Controlled supramolecular assemblies of luminescent tridentate cyclometalated alkynylgold(III) amphiphiles in aqueous media

• Kelvin Sze-Yim Cai,
• Brian Boyan Liu and
• Franco King-Chi Leung

Beilstein J. Org. Chem. 2026, 22, 1097–1106, doi:10.3762/bjoc.22.88

• commercial reagents were purchased from Acros Organics, Aladdin, Bidepharm, Dieckmann, Macklin and Tokyo Chemical Industry Co. Ltd, and were used as received unless otherwise specified. All reactions were performed under nitrogen unless otherwise specified. Analytical thin-layer chromatography (TLC) was

Amino acid-based surfactants: sustainable synthesis and antimicrobial mechanisms

• Rafaela Gomes Bezerra,
• Lourdes Pérez and
• Francisco Fábio Oliveira de Sousa

Beilstein J. Org. Chem. 2026, 22, 1067–1085, doi:10.3762/bjoc.22.85

Electrochemical reduction of unsaturated carbon–carbon bonds via 3d transition-metal catalysis

• Geon Kang,
• Minki Jeon,
• Pooja Kumari Jat,
• Cheoljae Kim and
• Isaac Choi

Beilstein J. Org. Chem. 2026, 22, 955–981, doi:10.3762/bjoc.22.75

• among chemistry and chemical industry community [1][2][3][4][5][6][7][8][9]. Given this longstanding significance, the development of controlled reduction strategies has diversified to accommodate the distinct reactivity and selectivity. Representatively, complete hydrogenation of alkynes or alkenes is

Rongalite addition to dienones: diastereoselectivity in cyclic sulfone synthesis; stereochemical rationalization and prospects as a general conjugate nucleophile

• Melina Goga,
• Hao Zong,
• James Franco,
• Jazmine Prana,
• Rudolph Michel,
• Antonia Muro,
• Elana Rubin,
• Janet Brenya,
• Henk Eshuis and
• Magnus W. P. Bebbington

Beilstein J. Org. Chem. 2026, 22, 742–752, doi:10.3762/bjoc.22.56

• used as a bleaching agent in the dyeing industry for more than a century [5][6]. Over the last 10 years particularly, it has begun to join the toolbox of reagents in organic synthesis, and shows diverse reactivity. It has been employed in reductions, radical processes and as a reagent for C1 transfer

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

• ]. Recently, continuous-flow organic synthesis has attracted much attention from both academia and industry, because it offers numerous advantages, such as not only a high productivity with limited space but also realizing green sustainable syntheses minimizing required energy and resources. When

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

• triazoles and aminocyclitols, which have numerous applications in industry, medicine, and pharmacy [1][2][3][4][5]. They are found in many biologically active compounds. For example, 3’-azido-3’-deoxythymidine (zidovudine, 1) is used in treatment of AIDS, while azapride (2), azidamphenicol (3), and

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

• has explored a broader space for the pharmaceutical industry, enabling the highly efficient synthesis of structurally complex compounds. In 2019, Yan and co-workers achieved the efficient asymmetric synthesis of chiral helicenes 59 with biaxial chirality via a vinylidene ortho-quinone methide (VQM

Synthesis of diaryl phosphates using phytic acid as a phosphorus source

• Kazuya Asao,
• Seika Matsumoto,
• Haruka Mori,
• Riku Yoshimura,
• Takeshi Sasaki,
• Naoya Hirata,
• Yasuyuki Hayakawa and
• Shin-ichi Kawaguchi

Beilstein J. Org. Chem. 2026, 22, 213–223, doi:10.3762/bjoc.22.15

• raw materials. Experimental Chemicals and reagents All reagents and solvents were purchased from Nacalai Tesque (Kyoto, Japan), Tokyo Chemical Industry (Tokyo, Japan), FUJIFILM Wako Pure Chemical Industries (Osaka, Japan), and Sigma-Aldrich (St. Louis, MO, USA). Phytic acid was obtained from Tokyo

• Chemical Industry. The rice bran used for phytic acid extraction was purchased from a rice-cleaning mill in Saga, Japan. Phytic acid extraction Phytic acid was extracted as described by Ida et al. [1]. n-Hexane (300 mL) was poured into rice bran (30 g) and the mixture was stirred with a magnetic stirrer

Base-promoted deacylation of 2-acetyl-2,5-dihydrothiophenes and their oxygen-mediated hydroxylation

• Vladimir G. Ilkin,
• Margarita Likhacheva,
• Igor V. Trushkov,
• Tetyana V. Beryozkina,
• Vera S. Berseneva,
• Vladimir T. Abaev,
• Wim Dehaen and
• Vasiliy A. Bakulev

Beilstein J. Org. Chem. 2026, 22, 192–204, doi:10.3762/bjoc.22.13

• Oxidative transformations are an important area of modern organic synthesis [1], producing a broad range of valuable synthetic products for the industry. A variety of catalytic reactions were developed for the oxidative conversions of unsaturated compounds [2][3][4][5], alcohols [6][7], alkanes [8][9][10

Highly electrophilic, gem- and spiro-activated trichloromethylnitrocyclopropanes: synthesis and structure

• Ilia A. Pilipenko,
• Mikhail V. Grigoriev,
• Olga Yu. Ozerova,
• Igor A. Litvinov,
• Darya V. Spiridonova,
• Aleksander V. Vasilyev and
• Sergey V. Makarenko

Beilstein J. Org. Chem. 2026, 22, 123–130, doi:10.3762/bjoc.22.5

• Resource Center for collective use "Modern physicochemical methods for the formation and study of materials for the needs of industry, science and education" Herzen State Pedagogical University of Russia. Some spectral studies were performed at the Center for Magnetic Resonance, the Center for Chemical

Silica gel with covalently attached bambusuril macrocycle for dicyanoaurate sorption from water

• Michaela Šusterová and
• Vladimír Šindelář

Beilstein J. Org. Chem. 2025, 21, 2604–2611, doi:10.3762/bjoc.21.201

• central role in gold mining industry [18]. In addition, it allows comparison with the previously prepared SG-BnBU material with noncovalently bound BnBU, which was also tested using the same anion. When either SG-NHCO-BU1 or SG-BU1 was treated with a 1 mM solution of K[Au(CN)2] in water, the anion

• industry, whereas dicyanoargentate is considered a contaminant in this context. To assess selectivity, we measured the sorption of dicyanoaurate from a 1 mM aqueous solution both in the absence and in the presence of an equimolar amount of dicyanoargentate. The measurements revealed that dicyanoaurate

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

• many applications in industry, but also plays an important role in many fields, such as electronics [3], agriculture [4], environmental protection [5] and cosmetics [6]. Chiral organic selenium-containing compounds also have important applications in organic synthesis and biomedicine [7][8]. These

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

• : aldehydes; biobased chemistry; biomass; carbonyl; fine chemicals; ketones; multicomponent; platforms; sustainability; Introduction Shifting towards sustainable practices in the chemical industry relies on continued advancement of green chemistry sciences which aim to minimize the global environmental

• valuable chemical used in the feed and food industry, is produced by petrochemical processes. Its synthesis from biobased lactic acid (LA) offers an access from renewable resources. However, this conversion is difficult due to the high activation energy required for the hydrogenation reaction removing the

• benzo[a]carbazole (a very important scaffold in the pharmaceutical industry) from the commercially available 2-phenylindole and bio-renewable 1-hydroxypropan-2-one (acetol) using a sulfone-containing Brønsted acidic medium as catalyst. The process was applied to a number of substituted 2-phenylindoles

Research progress on calixarene/pillararene-based controlled drug release systems

• Liu-Huan Yi,
• Jian Qin,
• Si-Ran Lu,
• Liu-Pan Yang,
• Li-Li Wang and
• Huan Yao

Beilstein J. Org. Chem. 2025, 21, 1757–1785, doi:10.3762/bjoc.21.139

• , for example, classic macrocycles like cyclodextrins [38] and cucurbiturils [39]. In recent years, aromatic macrocycles such as calixarenes (CAs) [40] and pillararenes (PAs) [41] have attracted widespread attention from the industry and scientists due to their simple synthesis which only require a one

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

• potential in advancing the green transformation of the chemical industry while enhancing inherent process safety. Safety, cost-effectiveness, and operational efficiency serve as pivotal drivers for advancing flow chemistry in nitration processes. This review provides a comprehensive analysis of the

• development, and (ii) refining existing synthetic processes through process intensification strategies. Nitric acid (HNO3) and its binary systems with sulfuric acid (HNO3/H2SO4) remain the industry-standard nitrating systems, particularly for the nitration of aromatic substrates. Motivated by environmental

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

Synthesis of optically active folded cyclic dimers and trimers

• Ena Kumamoto,
• Kana Ogawa,
• Kazunori Okamoto and
• Yasuhiro Morisaki

Beilstein J. Org. Chem. 2025, 21, 1603–1612, doi:10.3762/bjoc.21.124

• standard. Analytical thin-layer chromatography (TLC) was performed with silica gel 60 Merck F254 plates. Column chromatography was performed with silica gel 60N (spherical neutral). Recyclable preparative high-performance liquid chromatography (HPLC) was carried out on a Japan Analytical Industry Model

Azide–alkyne cycloaddition (click) reaction in biomass-derived solvent Cyrene^TM under one-pot conditions

• Zoltán Medgyesi and
• László T. Mika

Beilstein J. Org. Chem. 2025, 21, 1544–1551, doi:10.3762/bjoc.21.117

• should be strictly limited, particularly in the pharmaceutical industry. To develop an environmentally benign alternative to this useful method, the identification of an alternative reaction medium is highly desired. Among the recently characterized biomass-based potential solvents dihydrolevoglucosenone

General method for the synthesis of enaminones via photocatalysis

• Paula Pérez-Ramos,
• Raquel G. Soengas and
• Humberto Rodríguez-Solla

Beilstein J. Org. Chem. 2025, 21, 1535–1543, doi:10.3762/bjoc.21.116

• ; enaminones; nickel; photocatalysis; Introduction Enaminones are relevant intermediates in organic chemistry and the pharmaceutical industry [1][2][3][4][5][6]. These enamines have a carbonyl group conjugated to a carbon–carbon double bond, owing its great versatility in organic synthesis to its ability to

Calcium waste as a catalyst in the transesterification for demanding esters: scalability perspective

• Anton N. Potorochenko and
• Konstantin S. Rodygin

Beilstein J. Org. Chem. 2025, 21, 1520–1527, doi:10.3762/bjoc.21.114

• Anton N. Potorochenko Konstantin S. Rodygin Institute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya nab., St. Petersburg, 199034, Russia 10.3762/bjoc.21.114 Abstract Esters are valuable compounds in fine organic synthesis and industry. The significant growth in the demand

• ][4][5][6][7]. Nowadays, esters have found indispensable applications as solvents [8][9][10][11], biolubricants [12][13][14][15], food additives [16][17][18][19], polyester plastics and materials [20][21][22][23][24][25], in the pharmaceutical industry [26][27][28][29][30], in perfumes and flavoring

• applied as a transesterification catalyst for biodiesel production [50][51][52][53][54][55][56][57]. The amount of carbide slag generated is significant because of the many applications in chemistry [58][59][60][61] and industry as a large-tonnage product. Carbide slag was successfully utilized in various

Ambident reactivity of enolizable 5-mercapto-1H-tetrazoles in trapping reactions with in situ-generated thiocarbonyl S-methanides derived from sterically crowded cycloaliphatic thioketones

• Grzegorz Mlostoń,
• Małgorzata Celeda,
• Marcin Palusiak,
• Heinz Heimgartner,
• Marta Denel-Bobrowska and
• Agnieszka B. Olejniczak

Beilstein J. Org. Chem. 2025, 21, 1508–1519, doi:10.3762/bjoc.21.113

• polymer chemistry [36] and the crop protection industry [37] as well. Therefore, in extension of a typically synthetic work, a preliminary study on biological activity of the hitherto unreported 1H-tetrazole derivatives such as thioaminals 9 and dithioacetals 10 was carried out and it demonstrated that

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

• with pressurized gases (0.01–0.1 kbar). The first reports of using HHP were related to food industry applications [3][4], and later in chemical synthesis [5][6]. While the technique had been known since the late 1800s, and it had become popular in materials science and inorganic synthesis, it has

• investigate the scale-up potential of the HHP-assisted method. Although the HHP-assisted organic syntheses are relatively rare, the large (often ton) scale-capable equipment is readily available in the food industry. Accordingly, industrial level organic syntheses are attainable in a large scale. In an

Oxetanes: formation, reactivity and total syntheses of natural products

• Peter Gabko,
• Martin Kalník and
• Maroš Bella

Beilstein J. Org. Chem. 2025, 21, 1324–1373, doi:10.3762/bjoc.21.101

• electrophilicity of the carbonyl [74]. The oxetane products were obtained in good to high yields and further transformed into useful sulphone, butenolide and tetrahydrofuran derivatives. Besides laboratory-scale reactions, this ring expansion has also found applications in industry, specifically for a multi

• challenging amines. The combination of simple reaction conditions and excellent chemoselectivity makes this protocol very robust and suitable for both the academia and industry. Kinetic and computational experiments support an SN1 mechanism via loss of sulphur dioxide and oxetane carbocation formation. Two

Gold extraction at the molecular level using α- and β-cyclodextrins

• Susana Santos Braga

Beilstein J. Org. Chem. 2025, 21, 1116–1125, doi:10.3762/bjoc.21.89

• ][10] and a variety of implants, from hearing aids to prosthetic coatings and endovascular stents [11]. Traces of gold are found in a few electronic components of the automotive industry, such as airbag sensors, circuit boards, and audio systems [12]. Last but not least, gold coatings have gained a

• , heat, oxidation, and hydrolysis. Owing to their properties, cyclodextrins are frequently applied in pharmaceutical formulations with low-soluble or unstable drugs [28][29][30], in cosmetic formulations [31][32], and in the food industry [33][34]. The vast majority of guests in these applications are

• , thus confirming a strong interaction affinity lying within the 104 molar range. Gold extraction with β-CD and derivatives The possibility of using β-CD instead of α-CD in gold recovery and extraction is highly sought after by both researchers and industry because of the readiness of availability of β