Morpholine-mediated defluorinative cycloaddition of gem-difluoroalkenes and organic azides

• Tzu-Yu Huang,
• Mario Djugovski,
• Sweta Adhikari,
• Destinee L. Manning and
• Sudeshna Roy

Beilstein J. Org. Chem. 2023, 19, 1545–1554, doi:10.3762/bjoc.19.111

• product 3a was obtained. This shows the synthetic utility of this method; however, additional investigations into process chemistry may be necessary to accommodate a larger reaction scale. Conclusion In conclusion, we have shown for the first time a [3 + 2] cycloaddition of gem-difluoroalkenes with

Sulfate radical anion-induced benzylic oxidation of N-(arylsulfonyl)benzylamines to N-arylsulfonylimines

• Joydev K. Laha,
• Pankaj Gupta and
• Amitava Hazra

Beilstein J. Org. Chem. 2023, 19, 771–777, doi:10.3762/bjoc.19.57

• Joydev K. Laha Pankaj Gupta Amitava Hazra Department of Pharmaceutical Technology (Process Chemistry), National Institute of Pharmaceutical Education and Research, S. A. S. Nagar, Punjab 160062, India 10.3762/bjoc.19.57 Abstract A mild, operationally convenient, and practical method for the

Modern flow chemistry – prospect and advantage

• Philipp Heretsch

Beilstein J. Org. Chem. 2023, 19, 33–35, doi:10.3762/bjoc.19.3

• small dimensions of flow reactors enable explosive, toxic, or otherwise dangerous reactions and reagents to be accumulated only to a much lesser degree, especially when scaling up. This virtue has been exploited in process chemistry, where in the manufacturing of HIV protease inhibitor nelfinavir

Mechanochemical synthesis of unsymmetrical salens for the preparation of Co–salen complexes and their evaluation as catalysts for the synthesis of α-aryloxy alcohols via asymmetric phenolic kinetic resolution of terminal epoxides

• Shengli Zuo,
• Shuxiang Zheng,
• Jianjun Liu and
• Ang Zuo

Beilstein J. Org. Chem. 2022, 18, 1416–1423, doi:10.3762/bjoc.18.147

• key organic intermediates in the drug discovery and process chemistry [4][5][6]. Chiral metal–salen complexes were designed for catalyzing reaction processes that resulted in good yield, high regioselective and enantioselective control for the asymmetric ring opening of terminal epoxides. Various

Organocatalytic asymmetric nitroso aldol reaction of α-substituted malonamates

• Ekta Gupta,
• Narendra Kumar Vaishanv,
• Sandeep Kumar,
• Raja Krishnan Purshottam,
• Ruchir Kant and
• Kishor Mohanan

Beilstein J. Org. Chem. 2022, 18, 217–224, doi:10.3762/bjoc.18.25

• Ekta Gupta Narendra Kumar Vaishanv Sandeep Kumar Raja Krishnan Purshottam Ruchir Kant Kishor Mohanan Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, P.O. Box 173, Lucknow 226031, India Sophisticated Analytical

A comprehensive review of flow chemistry techniques tailored to the flavours and fragrances industries

• Guido Gambacorta,
• James S. Sharley and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2021, 17, 1181–1312, doi:10.3762/bjoc.17.90

• published in the chemical and engineering literature which would constitute a known solution or inspiration for commonly encountered procedures in the manufacture of fragrance and flavour chemicals. Keywords: flavours and fragrances; flow chemistry; process chemistry; synthesis; Introduction The fragrance

Design, synthesis and application of carbazole macrocycles in anion sensors

• Alo Rüütel,
• Ville Yrjänä,
• Sandip A. Kadam,
• Indrek Saar,
• Mihkel Ilisson,
• Astrid Darnell,
• Kristjan Haav,
• Tõiv Haljasorg,
• Lauri Toom,
• Johan Bobacka and
• Ivo Leito

Beilstein J. Org. Chem. 2020, 16, 1901–1914, doi:10.3762/bjoc.16.157

• Alo Ruutel Ville Yrjana Sandip A. Kadam Indrek Saar Mihkel Ilisson Astrid Darnell Kristjan Haav Toiv Haljasorg Lauri Toom Johan Bobacka Ivo Leito Institute of Chemistry, University of Tartu, Ravila 14a, 50411 Tartu, Estonia, https://analytical.chem.ut.ee Johan Gadolin Process Chemistry Centre

Stereoselective total synthesis and structural revision of the diacetylenic diol natural products strongylodiols H and I

• Pamarthi Gangadhar,
• Sayini Ramakrishna,
• Ponneri Venkateswarlu and
• Pabbaraja Srihari

Beilstein J. Org. Chem. 2018, 14, 2313–2320, doi:10.3762/bjoc.14.206

• Pamarthi Gangadhar Sayini Ramakrishna Ponneri Venkateswarlu Pabbaraja Srihari Department of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad-500007, Telangana, India Department of Chemistry, S. V. U. College of Sciences, Tirupati-517502, India

Automating multistep flow synthesis: approach and challenges in integrating chemistry, machines and logic

• Chinmay A. Shukla and
• Amol A. Kulkarni

Beilstein J. Org. Chem. 2017, 13, 960–987, doi:10.3762/bjoc.13.97

• literature) which can be understood by process chemists as well as engineers from other disciplines. Figure 2 shows the list of symbols used in the current review. For each case, initially we have described the process chemistry and transformations followed by the approach that needs to be followed to make

A new paradigm for designing ring construction strategies for green organic synthesis: implications for the discovery of multicomponent reactions to build molecules containing a single ring

• John Andraos

Beilstein J. Org. Chem. 2016, 12, 2420–2442, doi:10.3762/bjoc.12.236

• carrying out a reaction. Reduction of waste originating from the former group of solvents, however, can present challenges in process chemistry with respect to thermal control, solubility, mixing, and product separation issues when reactions are carried out in very large scale. The idea of “intrinsic

Opportunities and challenges for direct C–H functionalization of piperazines

• Zhishi Ye,
• Kristen E. Gettys and
• Mingji Dai

Beilstein J. Org. Chem. 2016, 12, 702–715, doi:10.3762/bjoc.12.70

• ]. This simple and effective diamine-free procedure allowed the reaction to take place at −30 °C, which is more desirable than −78 °C in process chemistry. Under the new reaction conditions, electrophiles such as TMSCl, MeO2CCl, DMF, Ph2CO, and PhBr (via a Negishi coupling process) can be used to install

Synthesis of the pentasaccharide repeating unit of the O-antigen of E. coli O117:K98:H4

• Pintu Kumar Mandal

Beilstein J. Org. Chem. 2014, 10, 2724–2728, doi:10.3762/bjoc.10.287

• Pintu Kumar Mandal Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, Lucknow, 226 031, India 10.3762/bjoc.10.287 Abstract The pentasaccharide repeating unit of the O-antigen of E. coli O117:K98:H4 strain has

Tandem Cu-catalyzed ketenimine formation and intramolecular nucleophile capture: Synthesis of 1,2-dihydro-2-iminoquinolines from 1-(o-acetamidophenyl)propargyl alcohols

• Gadi Ranjith Kumar,
• Yalla Kiran Kumar,
• Ruchir Kant and
• Maddi Sridhar Reddy

Beilstein J. Org. Chem. 2014, 10, 1255–1260, doi:10.3762/bjoc.10.125

• Gadi Ranjith Kumar Yalla Kiran Kumar Ruchir Kant Maddi Sridhar Reddy Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, P.O. Box 173, Lucknow 226031, India Academy of Scientific and Innovative Research, New Delhi

Convergent synthesis of a tetrasaccharide repeating unit of the O-specific polysaccharide from the cell wall lipopolysaccharide of Azospirillum brasilense strain Sp7

• Pintu Kumar Mandal,
• Debashis Dhara and
• Anup Kumar Misra

Beilstein J. Org. Chem. 2014, 10, 293–299, doi:10.3762/bjoc.10.26

• Pintu Kumar Mandal Debashis Dhara Anup Kumar Misra Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, Lucknow, 226 031, India Bose Institute, Division of Molecular Medicine, P-1/12, C.I.T. Scheme VII-M, Kolkata

Investigating the continuous synthesis of a nicotinonitrile precursor to nevirapine

• Ashley R. Longstreet,
• Suzanne M. Opalka,
• Brian S. Campbell,
• B. Frank Gupton and
• D. Tyler McQuade

Beilstein J. Org. Chem. 2013, 9, 2570–2578, doi:10.3762/bjoc.9.292

• a completely continuous process provides the opportunity to advance process chemistry/technology, a new process can often require significant investment for regulatory validation. We wish to implement our technology as quickly as feasible and to do so we want to avoid potential regulatory problems

Chemistry in flow systems III

• Andreas Kirschning

Beilstein J. Org. Chem. 2013, 9, 1696–1697, doi:10.3762/bjoc.9.193

• Ehrfeld Mikrosystem BTS and by CPC (Cellular Process Chemistry Systems) are marvelous examples of these engineered driven achievements. In the late nineties, organic chemists from both industry and academia, which included our group, became involved in the use of microreactors and provided a myriad of

Intramolecular carbolithiation cascades as a route to a highly strained carbocyclic framework: competition between 5-exo-trig ring closure and proton transfer

• William F. Bailey and
• Justin D. Fair

Beilstein J. Org. Chem. 2013, 9, 537–543, doi:10.3762/bjoc.9.59

• previously unreported compounds. Acknowledgements We are grateful to Dr. Terry L. Rathman of Optima Chemical, Douglas, GA, for generous gifts of t-BuLi and n-BuLi. This work was supported by a grant from the Process Chemistry Division, H. Lundbeck A/S, Copenhagen, Denmark.

Microwave-assisted three-component domino reaction: Synthesis of indolodiazepinotriazoles

• Rajesh K. Arigela,
• Sudhir K. Sharma,
• Brijesh Kumar and
• Bijoy Kundu

Beilstein J. Org. Chem. 2013, 9, 401–405, doi:10.3762/bjoc.9.41

• Rajesh K. Arigela Sudhir K. Sharma Brijesh Kumar Bijoy Kundu Medicinal & Process Chemistry Division CSIR-Central Drug Research Institute, Lucknow-226001, India Sophisticated Analytical and Instrumental Facility, CSIR-Central Drug Research Institute, Lucknow-226001, India 10.3762/bjoc.9.41

Tandem aldehyde–alkyne–amine coupling/cycloisomerization: A new synthesis of coumarins

• Maddi Sridhar Reddy,
• Nuligonda Thirupathi and
• Madala Haribabu

Beilstein J. Org. Chem. 2013, 9, 180–184, doi:10.3762/bjoc.9.21

• Maddi Sridhar Reddy Nuligonda Thirupathi Madala Haribabu Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow-226 001, India, Fax: +91-(522)-2623405, Tel: +91–(522)–2612 411, Extn: 4379 10.3762/bjoc.9.21 Abstract Cu-catalyzed A3 coupling of ethoxyacetylene

Engineering of indole-based tethered biheterocyclic alkaloid meridianin into β-carboline-derived tetracyclic polyheterocycles via amino functionalization/6-endo cationic π-cyclization

• Piyush K. Agarwal,
• Meena D. Dathi,
• Mohammad Saifuddin and
• Bijoy Kundu

Beilstein J. Org. Chem. 2012, 8, 1901–1908, doi:10.3762/bjoc.8.220

• Piyush K. Agarwal Meena D. Dathi Mohammad Saifuddin Bijoy Kundu Division of Medicinal and Process Chemistry, Central Drug Research Institute, CSIR, Lucknow, 226001, India, Phone: +91 522 2612411-18; Fax: +91 522 2623405 10.3762/bjoc.8.220 Abstract A mild, efficient and versatile method has been

New acylides: synthesis of 3-O-[γ-(4-oxo-2-aryl- thiazolidin- 3-yl)butyryl]erythromycin A derivatives

• Deepa Pandey,
• Wahajul Haq and
• Seturam B. Katti

Beilstein J. Org. Chem. 2008, 4, No. 14, doi:10.3762/bjoc.4.14

• Deepa Pandey Wahajul Haq Seturam B. Katti Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow, 226 001 India. Telephone: +91 0522 2612411-18 ext. 4364; fax: +91 0522 2623405 10.3762/bjoc.4.14 Abstract In search of new erythromycin derivatives 3-O-[γ-(4-oxo-2-aryl

An efficient synthesis of tetramic acid derivatives with extended conjugation from L-Ascorbic Acid

• Biswajit K. Singh,
• Surendra S. Bisht and
• Rama P. Tripathi

Beilstein J. Org. Chem. 2006, 2, No. 24, doi:10.1186/1860-5397-2-24

• Biswajit K. Singh Surendra S. Bisht Rama P. Tripathi Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow-226001, India 10.1186/1860-5397-2-24 Abstract Background Tetramic acids with polyenyl substituents are an important class of compounds in medicinal chemistry