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  1. Article ; Online: Process Intensification of a Napabucasin Manufacturing Method Utilizing Microflow Chemistry.

    Usutani, Hirotsugu / Yamamoto, Kenji / Hashimoto, Kazuki

    ACS omega

    2023  Volume 8, Issue 11, Page(s) 10373–10382

    Abstract: Microflow chemistry is one of the newest and most efficient technologies used today for the safe and effective production of medicines. In this paper, we show the use of this technology in the development of a manufacturing method for napabucasin, which ... ...

    Abstract Microflow chemistry is one of the newest and most efficient technologies used today for the safe and effective production of medicines. In this paper, we show the use of this technology in the development of a manufacturing method for napabucasin, which has potential in the treatment of colorectal and pancreatic cancers. In conventional "batch-type" reactor systems, the generation of side products can be controlled with traditional techniques such as reagent reverse-addition and temperature control. However, there is a limitation to which the yield and purity can be improved by these methods, as both are constrained by the efficiency of heat/mass transfer. Applying microflow chemistry technology alters the parameters of the constraint through the use of precise mixing in a microchannel, which offers increased possibility for improving yields and process intensification of the napabucasin process. Reported herein is a proof-of-concept study for the scale-up production of napabucasin using microflow chemistry techniques for manufacturing at the kilogram scale.
    Language English
    Publishing date 2023-03-09
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.2c07997
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Rapid and efficient synthesis of a novel cholinergic muscarinic M

    Miura, Shotaro / Fukuda, Koichiro / Masada, Shinichi / Usutani, Hirotsugu / Kanematsu, Makoto / Cork, David G / Kawamoto, Tetsuji

    Organic & biomolecular chemistry

    2019  Volume 17, Issue 35, Page(s) 8166–8174

    Abstract: Continuous flow-flash synthesis of a 2-bromobenzaldehyde derivative 18 as a key intermediate of a novel cholinergic muscarinic ... ...

    Abstract Continuous flow-flash synthesis of a 2-bromobenzaldehyde derivative 18 as a key intermediate of a novel cholinergic muscarinic M
    MeSH term(s) Allosteric Regulation/drug effects ; Benzaldehydes/chemical synthesis ; Benzaldehydes/chemistry ; Benzaldehydes/pharmacology ; Cholinergic Agents/chemical synthesis ; Cholinergic Agents/chemistry ; Cholinergic Agents/pharmacology ; Humans ; Molecular Structure ; Receptor, Muscarinic M1/metabolism
    Chemical Substances 2-bromobenzaldehyde ; Benzaldehydes ; CHRM1 protein, human ; Cholinergic Agents ; Receptor, Muscarinic M1
    Language English
    Publishing date 2019-08-29
    Publishing country England
    Document type Journal Article
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/c9ob01718f
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Generation and reaction of cyano-substituted aryllithium compounds using microreactors.

    Nagaki, Aiichiro / Kim, Heejin / Usutani, Hirotsugu / Matsuo, Chika / Yoshida, Jun-ichi

    Organic & biomolecular chemistry

    2010  Volume 8, Issue 5, Page(s) 1212–1217

    Abstract: We developed a microflow method for the generation and reactions of aryllithiums bearing a cyano group, including o-lithiobenzonitrile, m-lithiobenzonitrile and p-lithiobenzonitrile. The method was effective at much higher temperatures than are required ... ...

    Abstract We developed a microflow method for the generation and reactions of aryllithiums bearing a cyano group, including o-lithiobenzonitrile, m-lithiobenzonitrile and p-lithiobenzonitrile. The method was effective at much higher temperatures than are required for conventional macrobatch reactions, by virtue of rapid mixing, short residence time, and efficient temperature control. In addition, reactions of o-lithiobenzonitrile with carbonyl compounds followed by trapping of the resulting lithium alkoxides with electrophiles were achieved in an integrated microflow system.
    MeSH term(s) Cyanides/chemical synthesis ; Cyanides/chemistry ; Equipment Design ; Hydrocarbons, Aromatic/chemical synthesis ; Hydrocarbons, Aromatic/chemistry ; Lithium Compounds/chemical synthesis ; Lithium Compounds/chemistry ; Microfluidics/instrumentation ; Microfluidics/methods
    Chemical Substances Cyanides ; Hydrocarbons, Aromatic ; Lithium Compounds
    Language English
    Publishing date 2010-03-07
    Publishing country England
    Document type Journal Article
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/b919325c
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article: Generation and reactions of o-bromophenyllithium without benzyne formation using a microreactor.

    Usutani, Hirotsugu / Tomida, Yutaka / Nagaki, Aiichiro / Okamoto, Hideho / Nokami, Toshiki / Yoshida, Jun-ichi

    Journal of the American Chemical Society

    2007  Volume 129, Issue 11, Page(s) 3046–3047

    Language English
    Publishing date 2007-03-21
    Publishing country United States
    Document type Journal Article
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja068330s
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Bonn / Germany

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  5. Article ; Online: Integrated micro flow synthesis based on sequential Br-Li exchange reactions of p-, m-, and o-dibromobenzenes.

    Nagaki, Aiichiro / Tomida, Yutaka / Usutani, Hirotsugu / Kim, Heejin / Takabayashi, Naofumi / Nokami, Toshiki / Okamoto, Hideho / Yoshida, Jun-ichi

    Chemistry, an Asian journal

    2007  Volume 2, Issue 12, Page(s) 1513–1523

    Abstract: A micro flow system consisting of micromixers and microtube reactors provides an effective method for the introduction of two electrophiles onto p-, m-, and o-dibromobenzenes. The Br-Li exchange reaction of p-dibromobenzene with nBuLi can be conducted by ...

    Abstract A micro flow system consisting of micromixers and microtube reactors provides an effective method for the introduction of two electrophiles onto p-, m-, and o-dibromobenzenes. The Br-Li exchange reaction of p-dibromobenzene with nBuLi can be conducted by using the micro flow system at 20 degrees C, although much lower temperatures (< -48 degrees C) are needed for a batch reaction. The resulting p-bromophenyllithium was allowed to react with an electrophile in the micro flow system at 20 degrees C. The p-substituted bromobenzene thus obtained was subjected to a second Br-Li exchange reaction followed by reaction with a second electrophile at 20 degrees C in one flow. A similar transformation can be carried out with m-dibromobenzene by using the micro flow system. However, the Br-Li exchange reaction of o-dibromobenzene followed by reaction with an electrophile should be conducted at -78 degrees C to avoid benzyne formation. The second Br-Li exchange reaction followed by reaction with an electrophile can be carried out at 0 degrees C. By using the present method, a variety of p-, m-, and o-disubstituted benzenes were synthesized in one flow at much higher temperatures than are required for conventional batch reactions.
    Language English
    Publishing date 2007-12-03
    Publishing country Germany
    Document type Journal Article
    ISSN 1861-471X
    ISSN (online) 1861-471X
    DOI 10.1002/asia.200700231
    Database MEDical Literature Analysis and Retrieval System OnLINE

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