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Use of High-Throughput Tools for Telescoped Continuous Flow Synthesis of an Alkynylnaphthyridine Anticancer Agent, HSN608
Contributor(s):: Biyani, Shruti A., Qi, Qingqing, Wu, Jingze, Moriuchi, Yuta, Larocque, Elizabeth A., Sintim, Herman O., Thompson, David H.
Developing continuous syntheses of lead compounds to support in vivo studies and preclinical evaluation remains an underdeveloped area. We report a telescoped continuous flow synthesis of an alkynylnaphthyridine lead compound for the treatment of FLT3 mutations in acute myeloid leukemia....
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Process Intensive Synthesis of Propofol Enabled by Continuous Flow Chemistry
Contributor(s):: Vinet, Laurent, Di Marco, Lorenzo, Kairouz, Vanessa, Charette, André B.
A multi-step process using continuous flow chemistry to produce propofol is described. A scale-up of a 5-stage process (two continuous flow chemical steps, two extractions using a semi-batch approach, and one purification) provided propofol in high purity. This process minimizes the number of...
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Multiple Organolithium Generation in the Continuous Flow Synthesis of Amitriptyline
Contributor(s):: Kupracz, Lukas, Kirschning, Andreas
A continuous flow protocol for the preparation of the tricyclic antidepressant (TCA) amitriptyline is reported. The advantages of flow chemistry when handling organometallic agents as well as when performing reaction with gases are demonstrated. Continuous multilithiation combined with...
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Continuous flow production in the final step of vortioxetine synthesis. Piperazine ring formation on a flow platform with a focus on productivity and scalability
| Contributor(s):: Boros, Zoltán, Nagy-Győr, László, Kátai-Fadgyas, Katalin, Kőhegyi, Imre, Ling, István, Nagy, Tamás, Iványi, Zoltán, Oláh, Márk, Ruzsics, György, Temesi, Ottó, Volk, Balázs
In this study, the piperazine formation step of vortioxetine synthesis was investigated under continuous flow conditions. The batch variant of this step could be carried out at laboratory scale at 130–135 °C with a long reaction time (27 h) followed by a laborious optimization...
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A Continuous Flow Process for the Synthesis of Hymexazol
| Contributor(s):: Ma, Xin-peng, Chen, Jin-sha, Du, Xiao-hua
Hymexazol is an efficient and low-toxicity soil fungicide. In this work, a fully continuous flow process for the synthesis of hymexazol has been developed. This process begins with combining ethyl acetoacetate and hydroxylamine hydrochloride to form a hydroxamic acid intermediate. The reaction...
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A Practical and Convenient Synthesis of the Essential Antibiotic Drug Cefazolin under Sequential One-Flow Conditions
| Contributor(s):: Sugita, Shoichi, Ishitani, Haruro, Kobayashi, Shū
A sequential continuous-flow synthesis of cefazolin, which isavital first-choice drug used for the prevention of primary infection in most surgeries, was investigated. Rapid flow and efficient mixing of substrates in suitable flow reactors enabled the target compound to be obtained in a short...
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The Continuous-Flow Synthesis of Ibuprofen
| Contributor(s):: Bogdan, Andrew R., Poe, Sarah L, Kubis, Daniel C., Broadwater, Steven J., McQuade, D. Tyler
Let relief flow forth! A three-step, continuous-flow synthesis of ibuprofen was accomplished using a simplified microreactor. By designing a synthesis in which excess reagents and byproducts are compatible with downstream reactions, no intermediate purification or isolation steps are required.
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Continuous-flow synthesis of the anti-malaria drug artemisinin
| Contributor(s):: Lévesque, François, Seeberger, Peter H
Malaria is a serious global health issue. Artemisinin combination treatments are the first-line drugs, but supplies are limited because artemisinin is obtained solely by extraction from Artemisia annua. A continuous-flow process that converts dihydroartemisinic acid into artemisinin (see scheme)...