- Synthetic method of high-purity dopamine hydrochloride
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The invention provides a synthetic method of dopamine hydrochloride, and belongs to the field of drug synthesis. The preparation method comprises the following steps: taking 3,4-dimethoxyphenylethylamine as an initial raw material, firstly reacting with an acid to form a salt, re-crystallizing and refining to obtain 3,4-dimethoxyphenylethylamine salt, reacting with hydrobromic acid to remove methyl to generate dopamine hydrobromide, and finally reacting with hydrochloric acid to form a salt so as to obtain dopamine hydrochloride. The preparation method provided by the invention has the advantages of cheap and easily available initial raw materials, simple process, no high-temperature and high-pressure hydrogenation step, low cost, high purity and high yield, and is suitable for industrialproduction.
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Paragraph 0007-0008; 0052
(2020/11/23)
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- Tetrahydropalmatine derivative and application thereof
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The invention relates to a tetrahydropalmatine derivative and application thereof, a compound as shown in a formula (VI) and a preparation method thereof, and an application of the compound in medicine. Specifically, the invention relates to a derivative of the compound as shown in the general formula (VI) and a preparation method thereof, and an application of the derivative as a therapeutic agent in prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, diabetes type II, hyperglycemia, adiposis, or insulin resistance and metabolic syndrome. The compound disclosed by the invention also can reduce total cholesterol, low density lipoprotein (LDL)-cholesterol and triglycerides, and increases the expression of a liver LDL receptor and inhibits the expression of proprotein convertase subtilisin/kexin type 9 (PCSK9).
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- Total Synthesis of (-)-Melanthioidine by Copper-Mediated Cyclodimerization
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An efficient asymmetric total synthesis of the dimeric macrocyclic diaryl ether phenethyltetrahydroisoquinoline alkaloid (-)-melanthiodine is reported. Key steps of the synthesis include an efficient Noyori asymmetric transfer hydrogenation to access the enantioenriched phenethyltetrahydroisoquinoline monomeric subunit and a copper-mediated cyclodimerization to form the two diaryl ether linkages with concomitant macrocyclization.
- Wang, Jianjun,Evano, Gwilherm
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p. 3542 - 3545
(2016/08/16)
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- TETRAHYDROPROTOBERBINE COMPOUNDS AND USES THEREOF IN THE TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND NEURODEGENERATIVE DISEASES
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Tetrahydroprotoberbine (THPB) compounds and their use in the treatment of neurological, psychiatric and neurodegenerative diseases is provided. The compounds include d-govadine, l-govadine and racemic govadine, as well as d-THPBs of general formula (I). Enantioselective processes for preparing compounds of formula (I), and d- and l-govadine are also provided.(I)
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Paragraph 0193
(2013/03/26)
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- Syntheses of NAMDA derivatives inhibiting NO production in BV-2 cells stimulated with lipopolysaccharide
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Sixteen derivatives of N-acetyl-3-O-methyldopamine (NAMDA), an inhibitor of BH4 synthesis, were designed and synthesized. The ability of these derivatives to inhibit NO and BH4 production by lipopolysaccharide- stimulated BV-2 microglial cells was determined. While NAMDA at 100 μM inhibited NO and BH4 production by only about 20%, its catecholamide 8, indole 23 derivative, 13, and N-acetyl tetrahydroisoquinoline 25 inhibited the NO production by >50% at the same concentration. In particular, 13 and 25 inhibited both NO and BH4 production to similar degrees, which suggested that these compounds might inhibit NO production by blocking BH 4-dependent dimerization of the newly synthesized iNOS monomer.
- Jai, Woong Seo,Srisook, Ekaruth,Hyo, Jin Son,Hwang, Onyou,Cha, Young-Nam,Dae, Yoon Chi
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p. 3369 - 3373
(2007/10/03)
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- SYNTHESIS OF 3-O-METHYLATED DERIVATIVES OF CATECHOLAMINES
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3-O-Methylated catecholamines, used in the radioenzyme method for the analysis of catecholamines in blood, were synthesized. The optimum conditions for the production of both the intermediate and the final products were determined. By the use of tetrabutylammonium bromide in the condensation of nitromethane with O-benzylvanilin it is possible to obtain a high yield of 1-(3-methoxy-4-benzyloxyphenyl)-2-nitroethanol. The latter is easily transformed at a palladium catalyst into methylnoradrenaline by reduction with ammonium formate. The reduction of 1-(3-methoxy-4-benzyloxyphenyl)-2-nitroethylene with hydrogen or its donors at a palladium catalyst takes place significantly more readily in the presence of ferric chloride.
- Kulikov, S. V.,Samartsev, M. A.
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p. 280 - 288
(2007/10/02)
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