867022-55-7

Upstream product

• 7364-44-5 N,O-bis(trimethylsilyl)-L-valine 
• 589-15-1 1-bromomethyl-4-bromobenzene 
• 867022-53-5 methyl N-(4-bromobenzyl)-L-valinate 
• 72-18-4 L-valine 
• 1122-91-4 4-bromo-benzaldehyde 

Downstream Products

• 867022-57-9 (S)-2-[(4-bromo-benzyl)-pentanoyl-amino]-3-methyl-butyric acid 

Relevant academic research and scientific papers

PROCESS FOR OBTAINING VALINE DERIVATIVES USEFUL FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND

The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an-OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a "one pot" reaction.

PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTIC COMPOUNDS

A process for the preparation of angiotensin II antagonists and novel intermediates useful for the synthesis thereof.

A process for the preparation of angiotensin II antagonistic compounds

A process for the preparation of angiotensin II antagonists and novel intermediates useful for the synthesis thereof.

PROCESS FOR THE PREPARATION OF VALSARTAN AND PRECURSORS THEREOF

This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation.