81165-23-3Relevant academic research and scientific papers
Synthesis and biological evaluation of tetrahydroisoquinoline-derived antibacterial compounds
Asmara, Anjar P.,Bottomley, Amy L.,Harry, Elizabeth J.,Hiscocks, Hugh G.,Och, Anthony,Payne, Matthew,Ung, Alison T.
, (2022/02/07)
Antibiotic resistance is one of the greatest threats to modern medicine. Drugs that were once routinely used to treat infections are being rendered ineffective, increasing the demand for novel antibiotics with low potential for resistance. Here we report
Half-quantity resolution method of racemic mixture of tetrahydroisoquinoline type compound
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Paragraph 0060-0063, (2017/10/13)
The invention discloses a half-quantity resolution method of a racemic mixture of a tetrahydroisoquinoline type compound. The half-quantity resolution method comprises the following steps: dissolving hydrochloride of the tetrahydroisoquinoline type compound into water and alkalifying under an alkaline condition to obtain the racemic mixture; dissolving the racemic mixture into a polar solvent; under a heating condition, enabling the racemic mixture to react with a single half-quantity resolution agent N-acyl-D-amino acid or D-diphenylacyl tartaric acid, so as to form salt; or after enabling the racemic mixture to react with the resolution agent N-acyl-D-amino acid for a period of time, adding the other resolution agent D-diphenylacyl tartaric acid and reacting to form the salt; after reacting, slowly cooling and crystalizing and carrying out a post-treatment process, so as to directly obtain R configuration tetrahydroisoquinoline type compound salt with high optical purity. According to the half-quantity resolution method, the half quantity of the mixed resolution agent or the half quantity of the single resolution agent is utilized, so that the dosage of the resolution agent is saved; recrystallization is not needed and a design is reasonable; the preparation method is simple and convenient and has high practicability; the total yield of an R configuration product can reach 83.25 percent at maximum and the purity can reach 97 percent or more at maximum.
