Crystallization of Cyclic Amine Derivatives and Its Medical Application
A technology of crystallization and medicine, applied in the field of crystallization of cyclic amine derivatives, can solve the problem of low therapeutic effect
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[0107] Preparations of the above-mentioned dosage forms can be carried out according to known production methods generally used in the field of pharmaceutical preparations. At this time, if necessary, for example, excipients, binders, lubricants, disintegrants, sweeteners, surfactants, suspending agents or emulsifiers generally used in the field of formulations can be contained and produced.
[0108] Tablets can be prepared with, for example, excipients, binders, disintegrants or lubricants, and pills and granules can be prepared with, for example, excipients, binders or disintegrants. In addition, powders and capsules can be prepared containing, for example, excipients, syrups can be prepared containing, for example, sweeteners, and emulsions or suspensions can be prepared containing, for example, surfactants, suspending agents or emulsifying agents. And proceed.
[0109] Examples of excipients include lactose, glucose, starch, sucrose, microcrystalline cellulose, licorice pow...
Embodiment
[0121] The following examples are given to describe the present invention in detail, but the present invention is not limited to these examples.
[0122] Compound (I) and the raw materials and intermediates of compound (I) were synthesized by the methods described in the following Reference Examples. In addition, the commercially available compound was used for the compound used for the synthesis|combination of the reference example compound whose synthesis method is not described.
[0123] In the following description, the name of the solvent shown in the NMR data is the solvent used for the measurement. Also, the 400 MHz NMR spectrum was measured using a JNM-AL400 nuclear magnetic resonance apparatus (manufactured by JEOL Ltd.). The chemical shifts are based on tetramethylsilane, expressed in δ (unit: ppm), and the signals are expressed in s (singlet), d (doublet), t (triplet), q (quartet), quint (quintuplet) doublet), sept (septet), m (multiplet), br (broad), dd (double d...
reference example 1
[0124] (Reference Example 1) Preparation of the amorphous body of compound (I):
[0125] To 1-(4-(dimethylamino)piperidin-1-yl)-3-(1-methyl-1H-imidazol-2-yl)propane-1,3-dione (3.0g, 10.8mmol ) in isopropanol (90mL) solution in nitrogen atmosphere, add chloro[(S,S)-N-[2-[2-(4methylbenzyloxy)ethyl]amino-1,2-diphenyl Ethyl]-p-toluenesulfonamide]ruthenium(II) catalyst (175mg, 0.263mmol), and stirred at an internal temperature of 80°C for 18 hours. The reaction solution was concentrated, and 42.8 g of distilled water was transferred to a separatory funnel. After extraction with ethyl acetate, the ethyl acetate layer was extracted with distilled water, and all aqueous layers were combined and concentrated. After concentration, ethyl acetate was added, and azeotropic dehydration was performed with an evaporator. The residue was substituted with chloroform, and the concentrate was purified by silica gel column chromatography (NH silica gel, chloroform). Drying under reduced pressu...
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Abstract
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