- Preparation method for benflumetol and matched system thereof
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The invention belongs to the field of benflumetol, and relates to preparation and a system for the benflumetol, in particular to a preparation method for the benflumetol and a matched system thereof.The preparation method for the benflumetol is completed by sequentially through bulk drugs, a plurality of intermediates and the benflumetol. The matched system for the preparation method sequentiallycomprises an intermediate I matched system, an intermediate II matched system, an intermediate IV matched system, an intermediate V matched system and a benflumetol matched system. According to the invention, overall preparation is simple, reasonable and highly-efficient; the required time is greatly shortened; and exploration of industrial production conditions of the benflumetol is completed.
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- Asymmetric Deoxygenative Cyanation of Benzyl Alcohols Enabled by Synergistic Photoredox and Copper Catalysis?
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Summary of main observation and conclusion. An enantioselective deoxygenative cyanation of benzyl alcohols was accomplished for the first time through the synergistic photoredox and copper catalysis. This reaction features the use of organic photosensitizer and low-cost 3d metal catalyst, simple and safe operations, and extremely mild conditions. A variety of chiral benzyl nitriles were produced in generally good yields and high level of enantiocontrols from readily available feedstocks (22 examples, up to 93% yield and 92% ee).
- Chen, Hong-Wei,Lu, Fu-Dong,Cheng, Ying,Jia, Yue,Lu, Liang-Qiu,Xiao, Wen-Jing
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supporting information
p. 1671 - 1675
(2020/11/03)
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- An improved manufacturing process for the antimalaria drug coartem. Part II
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The manufacturing process for lumefantrine, 2, one of the two active principles in the fixed-dose combination of the anti-malarial drug Coartem, was reworked. For the conversion of 2-chloro-1-(2,7-dichloro-9H-fluoren-4-yl) ethanone, 5, to 2-dibutylamino-1-(2,7-dichloro-9H-fluoren-4-yl)ethanol, 8, a onepot process was developed that eliminated isolation of the epoxide 2-(2,7-dichloro-9H-fluoren-4-yl)oxirane, 7. Significant increase in throughput was achieved by applying new reaction and crystallization conditions for the Knoevenagel condensation of 2-dibutylamino-1-(2,7-dichloro-9H-fluoren-4-yl) ethanol, 8, to 2-dibutylamino-1-{2,7-dichloro-9-[1-(4-chlorophenyl)meth-(Z)- ylidene]-9H-fluoren-4-yl}ethanol, 2.
- Beutler, Ulrich,Fuenfschilling, Peter C.,Steinkemper, Andreas
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p. 341 - 345
(2012/12/31)
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- POLYMORPHIC FORM I OF LUMEFANTRINE AND PROCESSES FOR ITS PREPARATION
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The invention relates to a novel polymorphic form of lumefantrine and processes for its preparation. More particularly, it relates to the preparation of polymorphic form of lumefantrine designated as Form I. The invention also relates to pharmaceutical compositions that include the polymorphic Form I and use of said compositions for treatment of malaria.
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Page/Page column 7
(2010/11/24)
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