- Synthesis method of (S)-amino compound
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The invention relates to a synthesis method of a benazepril hydrochloride intermediate (S)-amino compound. According to the technical scheme, the preparation method of the (S)-amino compound comprises the following steps of by taking 2-aminobenzaldehyde 15 as an initial raw material, carrying out Aldol condensation under the action of alkali to prepare a compound 16, carrying out Pd/C catalytic hydrogenation on the compound 16 to prepare a compound 17, and carrying out DCC condensation on the compound 17 to generate a main structure compound 18 of the benazepril intermediate (S)-amino compound, carrying out substitution reaction on the compound 18 and tert-butyl chloroacetate to prepare a compound 19, and carrying out transamination reaction on the compound 19 under the catalytic action of a quinine-derived catalyst to generate the benazepril intermediate (S)-amino compound 1. The benazepril intermediate (S)-amino compound is synthesized by a method for directly constructing a chiral center through asymmetric catalysis, so that the reaction yield is increased.
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Paragraph 0012; 0047; 0051; 0052; 0056; 0057; 0061; ...
(2021/08/25)
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- PROCESS FOR PREPARATION OF BENAZEPRIL
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The present invention relates to an improved process for preparation of highly pure benazepril of Formula I, wherein R is hydrogen or pharmacologically acceptable salt thereof by completely eliminating the impurity of 7-bromo analogue of benazepril of Formula Ia, wherein R is bromo group.
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Page/Page column 16
(2008/06/13)
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- Phosphonic acid-substituted benzazepinone-n-acetic acid derivatives process for their preparation and pharmaceutical compositions comprising them
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Compounds having NEP-inhibitory activity, corresponding to the formula I in whichR 1 is hydrogen or a group forming a biolabile phosphonic acid ester,R 2 is hydrogen or a group forming a biolabile phosphonic acid ester and R. sup.3 is hydrogen or a group forming a biolabile carboxylic acid esterand physiologically acceptable salts of acids of formula I, and pharmaceutical compositions comprising these compounds.
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- Pharmaceuticals which promote gastrointestinal blood circulation
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The use is described of compounds of the general formula I STR1 wherein R1 represents a phenyl-lower alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or represents a naphthyl-lower alkyl group, R2 denotes hydrogen or a biolabile ester-forming group, and R3 denotes hydrogen or a biolabile ester-forming group, and physiologically acceptable salts of the acids of formula I for preparing pharmaceutical compositions for the treatment and/or prophylaxis of gastrointestinal blood circulation disturbances.
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- Piperidine compounds and pharmaceutical uses thereof
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Piperidine compounds of the formula: STR1 or isomers thereof as well as pharmaceutically acceptable salts and/or hydrate forms thereof, and piperidine compounds of the formula: STR2 or isomers thereof as well as salt and/or hydrate forms thereof. In the above formulae, A represents a methylene group, an oxygen atom or a sulfur atom; B represents an oxygen atom or a sulfur atom; R 1 and R 2 independently represent a hydrogen atom, a lower alkyl group or an aralkyl group; R 3 represents a hydrogen atom or an amino protecting group; Z represents an amino group or a protected amino group, a hydroxy group, or a reactive atom or group; m represents 1 or 2; and n represents the integer of 0 to 3.Piperidine compounds (I) possess an inhibitory activity against angiotensin-converting enzyme, and exhibit a long lasting hypotensive activity and are useful as antihypertensive agents. Piperidine compounds (II) are useful as intermediates for said piperidine compounds (I).
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