1003567-15-4

Upstream product

• 1003567-14-3 4-(1-tert-butoxycarbonyl-1-methylethoxy)-5-chloro-2-hydroxybenzoic acid methyl ester 
• 74-89-5 methylamine 

Downstream Products

• 1003567-16-5 2-(2-chloro-4-methylcarbamoyl-5-((S)-oxiran-2-ylmethoxy)phenoxy)-2-methylpropionic acid tert-butyl ester 

Relevant academic research and scientific papers

INTERMEDIATES 2-(2-CHLORO-5-HYDROXY-4-METHYLCARBAMOYLPHENOXY)-2-METHYLPROPIONIC ACID TERT-BUTYL ESTER AND GLYCIDYL BENZENE SULFONATES OR SALTS THEREOF AND THE PROCESS FOR PREPARATION OF SAID INTERMEDIATES

The present invention relates to novel processes for the preparation of intermediate compounds which can be used to prepare therapeutic drugs. The invention relates to the intermediates 2-(2-Chloro-5-hydroxy-4-5 methylcarbamoylphenoxy)-2-methylpropionic acid tert-butyl ester and glycidyl benzene sulfonates or salts thereof. More specifically, the present invention relates to the intermediates 2-(2-Chloro-5-hydroxy-4-methylcarbamoylphenoxy)-2-methylpropionic acid tert-butyl ester and novel glycidyl benzene sulfonates of formula IV as defined below, useful in the preparation of 2-10 {2-Chloro-5-{[(2S)-3-(5-chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-[(methylamino)carbonyl]phenoxy}-2-methylpropanoic acid.

PROCESS FOR THE PREPARATION OF CYCLIC SPIROPIPERIDINES

The present invention relates to new processes for the preparation of compounds of formula I, especially the compound 2-{2-Chloro-5-{[(2S)-3-(5-chloro-1'H,3H-spiro[1- benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-5 [(methylamino)carbonyl]phenoxy}-2-methylpropanoic acid and to new intermediates useful in the preparation thereof.

SPLROPIPERIDINE COMPOUNDS, A PROCESS OF THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THE TREATMENT OF AIRWAY DISEASES, INFLAMMATORY DISEASES, COPD OR ASTHMA

The present invention relates to new polymorphs of compounds 2-{2-Chloro-5-{[(2S)-3-(5-chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4- [(methylamino)carbonyl]phenoxy}-2-methylpropanoic acid, and the hydrochloride and sodium hydroxide salts thereof,and compound 2-{2-Chloro-5-{[(2R)-3-(5-chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4- [(methylamino)carbonyl]phenoxy}-2-methylpropanoic acid. The invention further relates to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention also relates to processes for the preparation of said compounds.

NOVEL TRICYCLIC SPIROPIPERIDINE COMPOUNDS, THEIR SYNTHESIS AND THEIR USES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

Compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, and R10 are as defined in the specification, are described. The present invention also relates to pharmaceutical composition comprising said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. Beside, the invention relates to salts and polymorphic forms of the new compounds as well as the preparation thereof.