up-scaling

Preparation of 2-(2H-Tetrazol-2-yl)benzoic Acids via Regioselective Cu(I) Catalyzed N2 Arylation of Tetrazole

[1]

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  • Z.J. Song, P. Maligres, C. Molinaro, G. Humphrey, J. Fritzen, J. Wilson, and Y. Chen, "Preparation of 2-(2H-Tetrazol-2-yl)benzoic Acids via Regioselective Cu(I) Catalyzed N2 Arylation of Tetrazole", Organic Process Research & Development, vol. 23, pp. 2354-2361, 2019. http://dx.doi.org/10.1021/acs.oprd.9b00243
  • Development and Scale-up of a Route to ATR Inhibitor AZD6738

    up-scaling of a sulfoximine-containing AI (Astra-Zeneca / AsymChem)

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  • W.R.F. Goundry, K. Dai, M. Gonzalez, D. Legg, A. O’Kearney-McMullan, J. Morrison, A. Stark, P. Siedlecki, P. Tomlin, and J. Yang, "Development and Scale-up of a Route to ATR Inhibitor AZD6738", Organic Process Research & Development, vol. 23, pp. 1333-1342, 2019. http://dx.doi.org/10.1021/acs.oprd.9b00075
  • Making the SF5 Group More Accessible: A Gas Reagent‐free Approach to Aryl Tetrafluoro‐λ6‐sulfanyl Chlorides


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  • C.R. Pitts, D. Bornemann, P. Liebing, N. Santschi, and A. Togni, "Making the SF5 Group More Accessible: A Gas-Reagent-Free Approach to Aryl Tetrafluoro-λ6 -sulfanyl Chlorides", Angewandte Chemie International Edition, vol. 58, pp. 1950-1954, 2019. http://dx.doi.org/10.1002/anie.201812356
  • Catalytic Deprotonative α-Formylation of Heteroarenes by an Amide Base Generated in Situ from Tetramethylammonium Fluoride and Tris(trimethylsilyl)amine


    [1]

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  • M. Shigeno, Y. Fujii, A. Kajima, K. Nozawa-Kumada, and Y. Kondo, "Catalytic Deprotonative α-Formylation of Heteroarenes by an Amide Base Generated in Situ from Tetramethylammonium Fluoride and Tris(trimethylsilyl)amine", Organic Process Research & Development, vol. 23, pp. 443-451, 2018. http://dx.doi.org/10.1021/acs.oprd.8b00247
  • Scalable Continuous Flow Process for the Synthesis of Eflornithine Using Fluoroform as Difluoromethyl Source


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  • M. Köckinger, C.A. Hone, B. Gutmann, P. Hanselmann, M. Bersier, A. Torvisco, and C.O. Kappe, "Scalable Continuous Flow Process for the Synthesis of Eflornithine Using Fluoroform as Difluoromethyl Source", Organic Process Research & Development, vol. 22, pp. 1553-1563, 2018. http://dx.doi.org/10.1021/acs.oprd.8b00318
  • Development of a Large-Scale Copper(I)/TEMPO-Catalyzed Aerobic Alcohol Oxidation for the Synthesis of LSD1 Inhibitor GSK2879552


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  • A. Ochen, R. Whitten, H.E. Aylott, K. Ruffell, G.D. Williams, F. Slater, A. Roberts, P. Evans, J.E. Steves, and M.J. Sanganee, "Development of a Large-Scale Copper(I)/TEMPO-Catalyzed Aerobic Alcohol Oxidation for the Synthesis of LSD1 Inhibitor GSK2879552", Organometallics, vol. 38, pp. 176-184, 2018. http://dx.doi.org/10.1021/acs.organomet.8b00546
  • Development and Demonstration of a Safer Protocol for the Synthesis of 5-Aryltetrazoles from Aryl Nitriles

    [tetrazoles, Bristol-Myers Squibb]

    [1]

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  • D.S. Treitler, S. Leung, and M. Lindrud, "Development and Demonstration of a Safer Protocol for the Synthesis of 5-Aryltetrazoles from Aryl Nitriles", Organic Process Research & Development, vol. 21, pp. 460-467, 2017. http://dx.doi.org/10.1021/acs.oprd.7b00016
  • Two Approaches to the Chemical Development and Large-Scale Preparation of a Pyrimidyl Tetrazole Intermediate

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  • P. Mullens, E. Cleator, M. McLaughlin, B. Bishop, J. Edwards, A. Goodyear, T. Andreani, Y. Jin, J. Kong, H. Li, M. Williams, and M. Zacuto, "Two Approaches to the Chemical Development and Large-Scale Preparation of a Pyrimidyl Tetrazole Intermediate", Organic Process Research & Development, vol. 20, pp. 1075-1087, 2016. http://dx.doi.org/10.1021/acs.oprd.6b00136