99149-83-4

Upstream product

• 80875-98-5 (2S,3aS,7aS)-perhydroindole-2-carboxylic acid 
• 827622-31-1 N-[1(S)-ethoxycarbonylbutyl]-(S)-alanine-2'-benzothiazolylthio ester 
• 110592-39-7 (S)-N-acetyl-2,3-dihydroindoline-2-carboxylic acid methyl ester 
• 748154-69-0 N-[1-(S)-ethoxycarbonyl-1-butyl]-(S)-alanyl chloride 
• 82864-25-3 ethyl (2S,3aS,7aS)-octahydro-1H-indole-2-carboxylate hydrochloride 
• 79854-42-5 Ethyl (S)-indoline-2-carboxylate hydrochloride 
• 23358-62-5 (S) norvaline ethyl ester hydrochloride 
• 107045-53-4 (2S,3aS,7aS)-1-(benzyloxycarbonyl)octahydro-1H-indole-2-carboxylic acid 
• 488097-90-1 Ethyl (2S)-2-[(4S)-4-methyl-2,5-dioxo-1,3-oxazolidin-3-yl]pentanoate 
• 107133-36-8 perindopril tert-butylamine 
• 866430-96-8 (2S,3aS,7aS)-1-{2-[1-ethoxycarbonyl-(S)-butylamino]-(S)-propionyl}-octahydroindole-2-carboxylic acid p-nitrobenzylic ester 
• 1477-50-5 Indole-2-carboxylic acid 
• 3770-50-1 2-carbethoxyindole 
• 4792-54-5 ethyl pyruvate phenylhydrazone 

Relevant academic research and scientific papers

Method for preparing perindopril despinner and intermediate thereof

The invention discloses a method for preparing perindopril despinner and an intermediate thereof. The method comprises the following steps: halogenating N-propionyl indole-2-carboxylic acid under theaction of a halogenation reagent so as to obtain a halogenation product, and further carrying out amine substitution and catalytic hydrogenation reduction on the obtained halogenation product, therebyobtaining the perindopril despinner. Compared with the prior art, the method is cheap and easy in reaction raw material, has a total yield as high as 64%, is high in product purity and is applicableto industrial production.

Of enantiomerically enriched indoline - 2 - formic acid

The invention discloses a synthesis method of enantiomer-enriched indoline-2-formic acid shown in a formula (I). The synthesis method of the enantiomer-enriched indoline-2-formic acid comprises the following steps: by adopting low-cost and available ortho-position halogen substituted benzaldehyde and N-benzoyl substituted glycine as starting materials, carrying out Erlenmeyer-Plochl cyclization, alkaline hydrolysis and asymmetric catalytic hydrogen for constructing a chiral center, and then carrying out acid catalysis, deprotection and cyclization sequentially or cyclization, acid catalysis and deprotection sequentially, so that the enantiomer-enriched indoline-2-formic acid is obtained. The synthesis method of the enantiomer-enriched indoline-2-formic acid has the advantages that raw materials used in the whole process route are low-cost and easily available, harmful substances or multiple danger special processes are not used, reaction conditions are mild, technological operation is simple, production is safe and stable, the product yield is high, the purity is high, less three wastes are produced, and the energy consumption is low, so that the synthesis method of the enantiomer-enriched indoline-2-formic acid is a process route especially applicable to industrial production. The formula (1) is described in the specification.

PROCESS FOR THE PREPARATION OF THE L-ARGININE SALT OF PERINDOPRIL

Process for the preparation of the compound of formula (I):

PERINDOPRIL TOSYLATE

The present invention relates to a novel salt of perindopril, namely the paratoluene sulfonic acid salt. The present invention also relates to an amorphous form of the perindopril paratoluene sulfonic acid salt. The invention further relates to processes for the preparation of the novel salt and the amorphous form thereof. The invention also relates to pharmaceutical compositions comprising the perindopril tosylate for the treatment of hypertension and heart failure.

SALTS OF PERINDOPRIL

The present invention relates to new salts of perindopril, particularly to a new calcium salt and new amine salts of perindopril, to a process for their preparation and to a pharmaceutical formulations containing the new salts.

PROCESS FOR THE PREPARATION OF PERINDOPRIL ERBUMINE SALT AND NOVEL POLYMORPH (S) THEREOF

A single pot process for the preparation of perindopril erbumine salt according to which condensation of (2S, 3aS, 7aS)-octahydroindole-2-carboxylic acid benzyl ester para toluene sulfonate with N-((S-)-ethoxy carbonyl -1-ethyl-(S)-alanine, catalytic hydrogenation of benzyl ester of (2S, 3aS, 7aS)-1-{2-[1-(ethoxycarbonyl)-(S)-butylamino]-(S)propionyl}- octahydro-indole-2-carboxylate and conversion of (2S,3aS, 7aS)-1-{2-[1-ethoxycarbonyl)_(S)-butylamino]-(S)-propionyl}octahydroindole-2-carboxylic acid to its perindopril erbumine salt are carried out in a single pot using a single solvent such as isopropyl acetate to obtain perindopril erbumine salt of very high purity. Also a novel polymorph S of perindopril erbumine having X-ray diffraction peaks of 9.10, 14.64, 15.37, 16.58, 17.39, 19.99, 20.62, 21.50, 22.15, 22.60, 24.20, 27.55 ± 0.2 at 2Θ values. Also processes for preparing the novel polymorph S.

NEW PHARMACEUTICAL INTERMEDIATES IN THE SYNTHESIS OF ACE- INHIBITORS AND THE USE THEREOF

The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the gen

PROCESS FOR SYNTHESIS OF PERINDOPRIL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF.

Process for the synthesis of perindopril of formula (I): and pharmaceutically acceptable salts thereof.

PROCESS FOR THE PREPARATION OF CRYSTALLINE PERINDOPRIL

The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof.

PROCESS FOR THE PREPARATION OF PERINDOPRIL

The present invention relates to an improved process for the preparation of silylated (2S, 3aS, 7aS)-2-carboxyperhydroindole. Also provided is an improved process for the preparation of perindopril and its pharmaceutically acceptable salts.