Continuous synthesis of dolutegravir sodium crystals using liquid-gas heterogeneous microreactor

Luo, Wenbin; Liu, Fen; Guo, Yaohao; Qiu, Junjie; Yan, Jinrui; Zhao, Teng; Bao, Bo

doi:10.1016/j.cclet.2022.06.059

Cited by 5 publications

(3 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The parameter (D 90 − D 10 )/D 50 is used to quantify the width of the crystal size distribution (CSD) peak, with a narrower peak indicating a more uniform distribution of particle sizes. 65 At a supersaturation level of 2.60, the peak width of the crystals obtained through our method is significantly diminished by 60%, decreasing from 2.98 to 1.19, in direct comparison to the characteristics of the raw materials. The crystal morphology is successfully controlled from irregular rod-like agglomerates to quasi-spherical particles by microfluidic antisolvent crystallization.…”

Section: In Situ Monitoring Of Oiling-out Crystallizationmentioning

confidence: 78%

“…The optimized pyraclostrobin crystals and raw materials were characterized, as shown in Figure a,b, respectively. The parameter ( D 90 – D 10 )/ D 50 is used to quantify the width of the crystal size distribution (CSD) peak, with a narrower peak indicating a more uniform distribution of particle sizes . At a supersaturation level of 2.60, the peak width of the crystals obtained through our method is significantly diminished by 60%, decreasing from 2.98 to 1.19, in direct comparison to the characteristics of the raw materials.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Microfluidic Crystallization for Screening of Spherical Particles of Pyraclostrobin

Zhong,

Guo,

Bao

2024

Ind. Eng. Chem. Res.

Self Cite

View full text Add to dashboard Cite

The semicontinuous antisolvent crystallization process of pyraclostrobin was investigated utilizing an integrated microfluidic device that encompasses both microfluidic channels and an agitated crystallizer. We successfully regulated the crystal morphology as quasi-spherical particles and narrowed the particle size distribution compared with that of the raw materials. We explored the impact of ultrasound powers, initial concentration, antisolvent content, and stirring rate on crystal morphology. Our innovative approach involves precisely manipulating the stirring rate and solvent content, resulting in diverse crystal morphologies. Notably, we unveil two distinct mechanisms governing the formation of spherical particles, which can be attributed to the variability in the oil droplet sizes. Our apparatus and approach enable the efficient screening of spherical particles, advocating minimal reagent consumption. This achievement holds the potential to be scaled across a variety of fields ranging from pharmaceuticals to material science.

show abstract

Section: In Situ Monitoring Of Oiling-out Crystallizationmentioning

confidence: 78%

Section: Resultsmentioning

confidence: 99%

Microfluidic Crystallization for Screening of Spherical Particles of Pyraclostrobin

Zhong,

Guo,

Bao

2024

Ind. Eng. Chem. Res.

Self Cite

View full text Add to dashboard Cite

show abstract

“…Other benefits are a confined reaction system and strong pressure resistance . Hence, it has the advantages of intrinsic safety, , precise control, and rapid scale-up. , It is well–known that these benefits have been demonstrated with good effect on fast and strong exothermic reactions, such as nitration and hydrogenation, , toxic and harmful reactions, such as chlorination and fluorination, dangerous and explosive reactions, such as azide oxidation and some extreme conditions. , Therefore, microreactor technology has been widely used in the fine chemical industry, life science and preparation of nanoparticles, − and pharmaceutical continuous manufacturing, which are increasingly moving toward green and intelligent development …”

Section: Introductionmentioning

confidence: 99%

Fully Continuous Flow Synthesis of 2′-Deoxy-2′-fluoro-arabinoside: A Key Intermediate of Azvudine

Chen,

Sun,

et al. 2024

Org. Process Res. Dev.

View full text Add to dashboard Cite

Azvudine was approved for the treatment of adult HIV-1 infection in China in 2021, and it was approved for conditional marketing for the treatment of SARS-CoV-2 in China in 2022. In this work, we describe a fully continuous flow synthesis of 2′-deoxy-2′-fluoroarabinoside, a key intermediate for azvudine. The process was accomplished via six chemical transformations, including chlorination, hydrolysis, fluorination, bromination, condensation, and deprotection in six sequential continuous flow devices. Under the optimized process conditions, the total yield was 32.3% with a total residence time of 156 min. Compared with batch conditions, the total yield was doubled, the total reaction time was shortened 16 times, and the E factor was reduced 1.63 times.

show abstract

Continuous-flow synthesis and crystal modification of Pigment Red 53

Mao

Zhou

Wang

et al. 2023

Chinese Chemical Letters

View full text Add to dashboard Cite

Continuous synthesis of dolutegravir sodium crystals using liquid-gas heterogeneous microreactor

Cited by 5 publications

References 47 publications

Microfluidic Crystallization for Screening of Spherical Particles of Pyraclostrobin

Microfluidic Crystallization for Screening of Spherical Particles of Pyraclostrobin

Fully Continuous Flow Synthesis of 2′-Deoxy-2′-fluoro-arabinoside: A Key Intermediate of Azvudine

Continuous-flow synthesis and crystal modification of Pigment Red 53

Contact Info

Product

Resources

About