Investigation into a high-p,T,c continuous flow synthesis of myristyl-γ-picolinium chloride (MGPC) – a preservative in pharmaceutical formulations

IF 2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Journal of Flow Chemistry Pub Date : 2024-01-26 DOI:10.1007/s41981-024-00309-0
Karuna Veeramani, Manish Shinde, Vishnuvardhana Vema Reddy Eda, Swamy Peraka, Saranya Mohan, Rakeshwar Bandichhor, Srinivas Oruganti
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Abstract

Myristyl-γ-picolinium chloride (MGPC) is an alkyl pyridine quaternary ammonium salt and a popular preservative in injectables such as Depo-Medrol (Methylprednisolone acetate). Herein we describe a successful high-p,T,c chemical intensification of MGPC synthesis from neat myristyl chloride and γ-picoline in continuous flow. The process is atom economical, scalable with low reactor footprint and under optimized conditions, consistently affords MGPC in 45 min (instead of 8–12 h reported in literature for a conventional batch process) with excellent yield (> 90%) and purity (> 99%).

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肉豆蔻基-γ-氯化吡啶(MGPC)的高p,T,c连续流合成研究--一种药物配方中的防腐剂
氯化肉豆蔻基-γ-甲基吡啶(MGPC)是一种烷基吡啶季铵盐,也是 Depo-Medrol(醋酸甲泼尼龙)等注射剂中常用的防腐剂。在此,我们介绍了一种成功的高p,T,c 化学强化方法,即在连续流条件下,从纯肉豆蔻酰氯和 γ-甲基吡啶合成 MGPC。该工艺具有原子经济性、可扩展性和反应器占地面积小的特点,在优化的条件下,只需 45 分钟(而不是文献报道的传统间歇工艺的 8-12 小时)即可稳定地合成出 MGPC,并具有极佳的收率(90%)和纯度(99%)。
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来源期刊
Journal of Flow Chemistry
Journal of Flow Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
6.40
自引率
3.70%
发文量
29
审稿时长
>12 weeks
期刊介绍: The main focus of the journal is flow chemistry in inorganic, organic, analytical and process chemistry in the academic research as well as in applied research and development in the pharmaceutical, agrochemical, fine-chemical, petro- chemical, fragrance industry.
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