78273-80-0Relevant articles and documents
Novel preparation method of intermediate namely 3-(1-piperidine methyl)phenol of roxatidine acetate hydrochloride
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Paragraph 0074-0077, (2018/04/02)
The invention relates to a preparation method of an intermediate namely 3-(1-piperidine methyl)phenol of roxatidine acetate hydrochloride. M-nitrobenzaldehyde is taken as the primary raw material; under the effect of a phase transfer catalyst, m- nitrobenzaldehyde is reduced by metal borohydride to obtain corresponding benzyl alcohol; in the presence of an alkali, benzyl alcohol reacts with organic sulfonyl chloride to generate active organic sulfonate; then in the presence of an alkali, organic sulfonate carries out N-alkylation reactions with piperidine to generate N-substituted piperidine derivatives; reducing the nitro groups of N-substituted piperidine derivatives to obtain corresponding amino compounds; and subjecting the amino compounds to diazotization, hydrolysis, and alkalizationin a sulfuric acid water solution to obtain 3-(1-piperidine methyl)phenol. The problem that the supply of the conventional raw material (m-hydroxyl benzaldehyde) is not enough and the cost is greatlyincreased is solved. The method is simple and safe, the raw materials are cheap and easily available, the reaction yield is high, and the method is very suitable for industrial production of 3-(1-piperidine methyl)phenol.
The use of 2-hydroxymethyl benzoic acid as an effective water surrogate in the Passerini reaction: A straightforward access to α-hydroxyamides
Serafini, Marta,Griglio, Alessia,Oberto, Elena,Pirali, Tracey,Tron, Gian Cesare
, p. 4786 - 4789 (2017/11/29)
Dozens of strategies have been described for the synthesis of α-hydroxyamides over the years, but they share common drawbacks in terms of generality and tolerability, especially to acid labile functionalities. Here we report a truncated Passerini reaction suitable for the easy and mild preparation of functionalized α-hydroxyamides. In particular, this procedure is tolerant to acid sensitive protecting groups, which remain intact during the multicomponent reaction.
Acetamide derivative and application thereof
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, (2008/06/13)
2-Substituted-N-{3-[3-(1-piperidinomethyl)phenoxy]propyl}acetamide, derivatives thereof, and pharmaceutically acceptable salts thereof. The substitution group may be aminomethylcyclohexane carbonyl group or N-carbobenzoxy-p-aminomethylhexane carbonyl group. The compounds having the first-mentioned group can be an effective component of an antiulcer drug composition, and the compounds of the last-mentioned group are intermediates for producing the compounds having the first-mentioned group. Disclosed also is an antiulcer drug composition comprising the above compound as an effective component. The antiulcer drug composition exhibits both the gastric acid secretion inhibitive activity and the gastric mucosa protective activity, and is effective as suppression and cure of ulcers.
Antiulcer phenoxypropylamine derivatives
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, (2008/06/13)
Phenoxypropylamine derivatives of the general formula STR1 wherein R1 represents a hydrogen atom or a methyl or ethyl group, R2 and R3, independently from each other, represent a lower alkyl group, or together form a linear alkylene group having 4 to 7 carbon atoms which may be optionally substituted by a hydroxyl or hydroxymethyl group, and R4 represents a hydrogen atom or a group of the formula --R5 --Z in which R5 represents a lower alkylene group, and Z represents a hydrogen atom or an amino, mono- or di-(lower alkyl)-amino, hydrdoxy lower alkylamino, lower alkanoylamino, hydroxyl, lower alkoxy, lower alkanoyloxy, phenoxy, halophenoxy, benzoyloxy or halobenzoyloxy group, and the salts thereof; to a process for production thereof; and to their medicinal use, particularly to antiulcer agents comprising these phenoxypropylamine derivatives or their salts.
