138320-26-0Relevant articles and documents
Preparation method of amiodarone hydrochloride intermittent
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Paragraph 0019; 0055-0056; 0064-0065; 0072-0073; 0083-0084, (2019/01/13)
The invention belongs to the field of medicine synthesis, and relates to a preparation method of an amiodarone hydrochloride intermittent. The method is characterized by including the following stepsthat 1, under an alkaline condition, in the presence of a phase transfer catalyst, a compound 1 and a compound 2 are subjected to nucleophilic substitution reaction to obtain a compound 3; 2, under analkaline condition, the compound 3 is hydrolyzed to generate a compound 4; 3, the compound 4 is subjected to intramolecular aldol condensation, decarboxylation and dehydration to obtain a compound 5;4, a compound 6 and thionyl chloride are subjected to heating reaction to obtain a compound 7; 5, under the presence of lewis acid, the compound 5 and the compound 7 are subjected to friede-crafts acylation reaction to obtain a compound 8; 6, under the presence of lewis acid, the compound 8 is subjected to demethylation to generate a compound 9, namely the amiodarone hydrochloride intermittent 2-butyl-3-(4-hydroxybenzoyl)benzofuran. The preparation method of the amiodarone hydrochloride intermittent has the advantages of being short in reaction time, high in product purity and high in yield,and the amiodarone hydrochloride intermittent is suitable for large-scale industrial production.
Preparation method of amiodarone hydrochloride intermediate 2-butylbenzofuran
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Paragraph 0058; 0059, (2018/11/03)
The invention relates to a preparation method of an amiodarone hydrochloride intermediate 2-butylbenzofuran. The preparation method comprises the following steps: A, with methyl 2-(2-aldehydephenoxy)hexanoate as a reaction substrate, under the action of potassium carbonate and potassium iodide, reacting in an organic solvent until a raw material disappears; B, adding water and an organic solvent into a reaction solution obtained in the step A, thoroughly stirring for extracting, separating out an organic phase, drying and then concentrating under reduced pressure to obtain yellow transparent liquid 2-butylbenzofuran. The 2-butylbenzofuran prepared by the preparation method is high in purity; the operation is simple; use of cumbersome column chromatography is avoided; the preparation methodis suitable for large-scale industrial production.
Amiodarone hydrochloride preparation method
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Paragraph 0110-0112, (2018/03/13)
The invention belongs to the field of medicine, and especially relates to an amiodarone hydrochloride preparation method. The method takes 2-hydroxybenzaldehyde and 2-alkyl halohexoic acid ester as the raw materials to prepare 2-butylbenzofuran, 2-butylbenzofuran is taken as the raw material, and is subjected to the steps of friedel-crafts acylation, demethylation, iodination, etherification and salt forming to obtain the amiodarone hydrochloride. By employing the method, the raw materials have the advantages of low cost and easy acquisition, the process is simple, and 2-butylbenzofuran and amiodarone hydrochloride with high purity and high yield can be obtained, the cost is low, the waste water is little, and the method is suitable for industrial production.
Intermediates for making a bezofuran or benzothiophene derivative nitrated in position 5 and uses thereof
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Page/Page column 17, (2008/06/13)
The invention concerns novel nitroaromatic compounds of general formula (I′) wherein: R, R′1, R2, Z and n are as defined in claim 1. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further c
Method of preparing a benzofuran or benzothiophene compound
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, (2008/06/13)
The invention concerns a novel method for preparing a benzofuran or benzothiophene compound by cyclizing an aromatic compound bearing a side-chain comprising at least two carbon atoms, one of the carbon atoms being bound to the benzene cycle by an oxygen or sulphur atom, the other carbon atom is in carboxylic form and a formyl radical in ortho position relative to said chain. The inventive method is characterised in that it consists in cyclizing the latter in the presence of an efficient amount of a carbonate base in a medium comprising a carboxylic acid anhydride and optionally an organic solvent.
Synthesis and properties of new 2-alkyl-1,4-benzoxazepine derivatives. Part I. Synthesis and cyclization of 2-phenoxyalkanoic acid derivatives
Kwiecien
, p. 733 - 741 (2007/10/03)
2-Alkyl-1,4-benzoxazepin-3,5-diones (8) were readily prepared by cyclodehydration of 2-(o-carbamoilphenoxy)alkanoic acids (7) in acetic anhydride, and with low yields by the same reaction of 2-(o-carboxyphenoxy)alkanoic acid amides (4). The novel acid amides 4 were synthesized from salicylaldehyde and 2-bromo esters 1, via formyl amides 3. The acid amides 7 were formed directly by condensation of salicylamides with 2-bromo esters 1 in dimethyl formamide or by hydrolysis of esters 6 obtained by the same reaction in methyl-ethyl ketone solution.
Synthesis of 2-Phenoxyhexanal and 2-(o-Formylphenoxy)Hexanoic Acid and Its Derivatives
Kwiecien, H.
, p. 661 - 666 (2007/10/02)
The paper describes the synthesis of 2-phenoxyhexanal and 2-(o-formylphenoxy)hexanoic acid and its derivatives which are intermediate compounds in the synthesis of new heterocyclic compounds.Key words: 2-phenoxyhexanal, 2-phenoxyhexanoic acid derivatives, 2-butylbenzofurane