- Preparation method of 5 -aminolevulinic acid hydrochloride intermediate (by machine translation)
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The invention relates to a preparation method of 5 -aminolevulinic acid hydrochloride intermediate, which belongs to the field of pharmaceutical compound synthesis and provides a 5 -aminolevulinic acid hydrochloride intermediate preparation method which comprises the following technical points: (a), (1) or (2) compound in reaction solvent a, oxidizing agent a, compound of formula (5); or process b) wherein the compound of formula (6) or formula (3 4) is obtained under the action of a reaction solvent b and an oxidizing agent b 6. The compound of formula (6) is then purified to give 5 -aminolevulinic acid hydrochloride by an acidic hydrolysis deprotecting group, or a direct acidic hydrolysis deprotecting group. The environment-friendly oxidation reagent is adopted, the quality requirement of high-quality medicine raw materials can be met at the same time, the production efficiency can be improved, and the requirement of industrial large-scale production can be met. (by machine translation)
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Paragraph 0060; 0125
(2020/09/08)
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- Carbonylation Access to Phthalimides Using Self-Sufficient Directing Group and Nucleophile
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Herein we report a novel palladium-catalyzed oxidative carbonylation reaction for the synthesis of phthalimides with high atom- and step-economy. In our strategy, the imine and H2O, which are generated in situ from the condensation of aldehyde and amine, serve as self-sufficient directing group and nucleophile, respectively. This method provides rapid access to phthalimides starting from readily available materials in a one-pot manner. Various phthalimide derivatives are constructed efficiently, including medicinally and biologically active phthalimide-containing compounds.
- Ji, Fanghua,Li, Jianxiao,Li, Xianwei,Guo, Wei,Wu, Wanqing,Jiang, Huanfeng
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p. 104 - 112
(2018/02/19)
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- Preparation method of 5-aminolevulinic acid and Use of the same
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The present invention refers to 5-aminolevulinic acid or 5-aminolevulinic acid novel manufacturing method and 5-aminolevulinic acid or a pharmaceutically acceptable salts, for the treatment of skin diseases relates to the use. Synthesis of 5-aminolevulinic acid salt the present invention according to 5-aminolevulinic acid or features a previously known method being much high yield than synthetic method, heavy metals nor chlorine, boron intermediates halogen such as single plate, do not is not synchronized residual product, organic solvent as a solvent in addition a solvent soluble instead, more wound on a clean roll and a.. And the present invention according to 5-aminolevulinic acid or a pharmaceutically acceptable salt by comprising, as an active ingredient for treatment or treatment skin disease gel system or the like, and number lotion composition is topically applied to the skin disease site more excellent the active mode, and for conserving having electrode and the ground of the diode, skin diseases in particular psoriasis alarm healing therapeutic agent for a disease is constructed based on the character data useful for the development can be used..
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Paragraph 0054-0057
(2016/12/12)
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- Method of preparing an acid additional salt of delta-aminolevulinic acid
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An acid addition salt of δ-aminolevulinic acid is prepared in such a way that tetrahydrofurfurylamine (VI) is reacted with phthalic anhydride under an anhydrous condition to introduce a phthal group which protects amino group of tetrahydrofurfurylamine to give N-tetrahydrofurfuryl phthalimide (III), carbon atoms of the first- and fourth-positions of thus obtained N-tetrahydrofurfurylphthalimide (III) are oxidized at 80° C. using sodium periodate as a oxidizing agent and ruthenium chloride hydrate as a catalyst to yield 5-phthalimidolevulinic acid (II), then the protecting group of 5-phthalimidolevulinic acid (II) is deprotected using an acid to prepare an acid additional salt of δ-aminolevulinic acid. The acid additional salt of δ-aminolevulinic acid is readily converted by neutralization by an alkali to δ-aminolevulinic acid, which is very useful as a precursor of Vitamin B12, heme and chlorophyll.
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