检索结果-内蒙古大学图书馆

Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry 2025年第1期83卷 15-24页

作者： Tsuritani, Takayuki Kijima, Akihito Fukui, Nobuaki Yanagisawa, Shuichi Agura, Kazushi Kasamatsu, Koji API R&D Laboratory Pharmaceutical Technology Research Division Shionogi & Co. Ltd. 1–3 Kuise Terajima 2–chome Amagasaki660–0813 Japan

Ensitrelvir, SArS–CoV–2 3CL protease inhibitor, has been discovered for the treatment of the coronavirus disease 2019 (COVId–19). Ensitrelvir is structurally composed from three main units, which are indazole unit, triazole unit and triazinone unit. Synthetic strategies where these three units are employed at latter steps in the synthesis made it possible to construct a highly productive convergent route. In addition, the lean manufacturing process was also established through process optimization based on SELECT perspectives. These achievements contributed for the rapid commercial manufacturing of Ensitrelvir with less than one year. In this report, we describe r&d activities for route scouting and process optimization. In addition, a few trouble shootings which occurred during the manufacturing are also introduced. Lastly, additional study for further investigations to improve productivity and flexibility are briefly explained. © 2025 Society of Synthetic Organic Chemistry. All rights reserved.

关键词： Coronavirus

来源：评论

学校读者我要写书评

暂无评论

development of Continuous Flow Technology Handling Various reaction Systems toward Manufacturing drug Substances

Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Che...

引用

Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry 2024年第8期82卷 768-779页

作者： Hosoya, Masahiro API R&D Laboratory Research Division Shionogi & Co. Ltd. 3-1-1 Futaba-cho Toyonaka561-0825 Japan

Toward manufacturing drug substances under continuous flow conditions, homogeneous reaction systems are generally preferred to enable the process control. However, this approach toward the homogeneous reaction systems limits the implementation scope of continuous flow technology and may deviate from the ideal process because various reaction systems including heterogeneous reaction systems have to be handled in the recent pharmaceutical development. The author tried to establish the technological platform to enable the control of the various reaction systems under continuous flow conditions, which will truly contribute to the dissemination of continuous flow technology in the pharmaceutical development. © 2024 Society of Synthetic Organic Chemistry. All rights reserved.

关键词： Process control

来源：评论

学校读者我要写书评

暂无评论

development of practical synthetic method for the preparation ofdolutegravir sodium, a potent HIV-1 integrase inhibitor for the treatment of HIV infectious disease

Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Che...

引用

Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry 2020年第1期78卷 2-10页

作者： Yasukata, Tatsuro Aoyama, Yasunori API R&D Laboratory CMC R&D Division Shionogi and Co. Ltd. 2-1-3 Kuise Terajima Amagasaki660-0813 Japan

dolutegravir sodium, a potent inhibitor of Human Immunodeficiency Virus type-1 (HIV-1) integrase, is a promising drug for the treatment of HIV infectious disease. dolutegravir sodium has a highly-functionalized tricyclic core structure, thus it has been a challenge to establish practical synthetic methods. The synthetic route at the medicinal chemistry stage required numerous synthetic steps along with chromatographic purification operations, leading to a low total yield and difficult application to practical scale production. To solve these problems, we have developed two practical synthetic methods for the preparation of dolutegravir sodium;(i) a practical method starting from readily accessible material maltol and (ii) a more efficient method through the key intermediate pyrone diester. The first method includes scalable oxidation process of methyl moiety of maltol and palladium-catalyzed carbonylation for introduction of amide moiety, leading to a practical manufacturing method in less synthetic steps and enabling multikilogram scale manufacturing. The second method includes an efficient and practical synthetic method of the pyrone diester intermediate from readily accessible starting materials, and the obtained pyrone diester can easily be transformed to dolutegravir sodium, leading to a more efficient and atom-economical method for preparation of the potent anti-HIV agent. © 2020 Society of Synthetic Organic Chemistry. All rights reserved.

关键词： Sodium

来源：评论

学校读者我要写书评

暂无评论

Control of ship fouling in U.S. Navy

引用

Naval Engineers Journal 1967年第N 1期v 79卷 p77-85页

作者： Birnbaum, L.S. Bukzin, E.A. Saroyan, J.r. Leon S. Birnbaum holds a B.S. degree in Chemistry from City College of New York. He has completed graduate work in Chemistry at the University of Maryland and Temple University and in Technology and Management at American University. He has been with the Navy Department Washington since 1949 and is currently Head of the Coatings and Chemistry Branch of the Materials Development and Application Office of the Naval Ship Engineering Center. Responsibilities of this Branch include such items as coatings corrosion control techniques insulation chemical cleaning water treatment toxicology and detection and decontamination of biological and chemical warfare agents. Prior to this Mr. Birnbaum was employed in the Industrial Test Laboratory Philadelphia Naval Shipyard from 1938 to 1949. Work during this period included supervision of a section which inspected paints and allied materials and petroleum products to determine their suitability for Naval use and direction of research in fire retardant treatments. He is a member of the American Chemical Society Washington Paint Technical Group. National Association of Corrosion Engineers and the American Society of Naval Engineers. Mr. Bukzin is a research and development program manager in the Naval Ship Systems Command of the Department of the Navy in the fields of non-metallic materials fuels lubricants cold weather operations and several other areas. He is a graduate chemical engineer from New York University with additional training in naval architecture and management which culminated in his participation in the Senior Development Program at Cornell University during the summer of 1960. He has been employed by the Command and its predecessor for the past 2b years and has been in his present position of R&D planning and programming for the past six years. Prior to that his major technical responsibilities were in the field of elastomers and their applications. He received several awards and published a number of papers during those years. Mr. Bukzin is a me

report on paints used on surface ships and submarines for protection against corrosion and prevention of fouling, and on work connected with development and evaluation of such coatings;experiences with "hot plastic", "cold plastic" and vinyl paints;hazards in use of vinyl paints and safety precautions;test techniques;new toxics (which are only kind so far satisfactory antifouling formulations) under test.

关键词： Ships

来源：评论

学校读者我要写书评

暂无评论

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

请选择保存的检索档案：

请选择收藏分类：

通借通还

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：