2380-94-1Relevant articles and documents
A PHOTOCHEMICAL SYNTHESIS OF 4-HYDROXYINDOLE
Kaneko, Chikara,Okuda, Wakako,Karasawa, Yoshio,Somei, Masanori
, p. 547 - 550 (1980)
1-Alkoxycarbonyl-4-hydroxyindoles were prepared in ca. 25percent yields from 5-(alkoxycarbonylamino)isoquinoline 2-oxides by irradiation in an aprotic solvent, followed by an acid treatment under solvolytic conditions. 1-benzyloxycarbonyl-4-hydroxyindole was then converted to the title compound by catalytic hydrogenation.
A facile synthesis of 4-hydroxy- and 4-aminoindoles through corresponding indolines
Tanaka,Murakami,Aizawa,Torii
, p. 3742 - 3744 (1989)
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Method for synthesizing 4 -hydroxyindole
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Paragraph 0025; 0028-0029; 0030; 0033-0034, (2021/09/01)
The invention discloses a novel method for synthesizing 4 -hydroxyindole, and belongs to the field of medical intermediate synthesis. With 1, 3 - Cyclohexanedione reacts with 2 - aminoethanol to produce a corresponding enamine compound which is then converted to 4 - hydroxyindole in the presence of a supported or framework-type metal catalyst. The synthesis route is short in step, high-temperature reaction of the pressure vessel is avoided, 4 - hydroxyl indole synthesis efficiency and safety are improved. 2 - Aminoethanol is adopted as the synthetic raw material, the use of higher 2 - chloroacetaldehyde is avoided, the reaction by-product with 1 and 3 - cyclohexanedione is water, and the reaction by-product of the generated enamine under the action of the catalyst is H. 2 , 4 - Hydroxyl indole production cost is reduced.
4-hydroxyindole preparation method suitable for industrial production
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Paragraph 0071; 0072, (2019/11/19)
The invention relates to the technical field of organic synthesis, in particular to a preparation method of a medical intermediate 4-hydroxyindole. The method includes: taking 1, 5, 6, 7-tetrahydro-4H-indole-4-one as the raw material, carrying out nucleophilic substitution reaction under the action of alkali to obtain an amino protection product (I), reacting the compound (I) with a halogenation reagent to obtain alpha-halogenated ketone (II), subjecting the compound (II) to elimination reaction under the action of alkali to remove HX so as to obtain a 4-hydroxyindole derivative (III), and finally conducting hydrolysis deprotection on the compound (III) to obtain 4-hydroxyindole (IV). The invention provides a simple industrial production route for 4-hydroxyindole, and the method has the advantages of simple reaction operation, avoidance of high temperature, high pressure and catalytic reaction, and low cost.