39989-43-0Relevant academic research and scientific papers
Synthesis method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride
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Paragraph 0057-0062, (2021/03/18)
The invention relates to a synthesis method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride, and belongs to the technical field of synthesis of medical intermediates. The method comprises the steps that 3, 5-dichlorobenzaldehyde serves as a raw material, 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride is obtained through Schiff base preparation, reduction, ring closing and reductive acidification reaction, and the total yield is 60% or above. The method avoids using expensive raw materials, and is simple in process route, mild in condition, low in production costand suitable for industrial production.
Versatile Dynamic Covalent Assemblies for Probing π-Stacking and Chirality Induction from Homotopic Faces
Ye, Hebo,Hai, Yu,Ren, Yulong,You, Lei
supporting information, p. 3804 - 3809 (2017/03/27)
Herein we report for the first time the use of dynamic covalent reactions (DCRs) for building a π-stacking model system and further quantifying its substituent effects (SEs), which remain a topic of debate despite the rich history of stacking. A general DCR between 10-methylacridinium ion and primary amines was discovered, in which π-stacking played a stabilizing role. Facile quantification of SEs with in situ competing π-stacking systems was next achieved in the form of amine exchange exhibiting structural diversity by simply varying components. The linear correlation with σm in Hammett plots indicates the dominance of purely electrostatic SEs, and the additivity of SEs is in line with the direct interaction model. With α-chiral amines π-stacking within the adduct enabled chirality transfer from homotopic faces. The strategy of dynamic covalent assembly should be appealing to future research of probing weak interactions and manipulating chirality.
Benzylamines: Synthesis and evaluation of antimycobacterial properties
Meindl,Von Angerer,Schonenberger,Ruckdeschel
, p. 1111 - 1118 (2007/10/02)
The synthesis of benzylamines with various N-alkyl chains and substituents in the aromatic system as well as their evaluation on Mycobacterium tuberculosis H 37 Ra are described. The most active compounds in this test, N-methyl-3-chlorobenzylamine (MIC 10.2 μg/mL), N-methyl-3,5-dichlorobenzylamine (93, MIC 10.2 μg/mL), and N-butyl-3,5-difluorobenzylamine (MIC 6.4 μg/mL), also exhibited a marked inhibitory effect on Mycobacterium marinum and Mycobacterium lufu used for the determination of antileprotic properties. The combination of 93 with aminosalicylic acid, streptomycin, or dapsone exert marked supra-additive effects on M. tuberculosis H 37 Ra.
