867022-53-5

Upstream product

• 4070-48-8 L-Valine methyl ester 
• 589-15-1 1-bromomethyl-4-bromobenzene 
• 6306-52-1 L-valine methylester hydrochloride 
• 1122-91-4 4-bromo-benzaldehyde 

Downstream Products

• 867022-55-7 (S)-2-(4-bromo-benzyl)-amino-3-methyl-butyric acid 

Relevant academic research and scientific papers

Convenient synthesis of Valsartan via a Suzuki reaction

An efficient synthesis of the angiotensin II inhibitor Valsartan (Diovan) is presented. The formation of the aryl-aryl bond represents the key step of its synthesis, which has been done by a Suzuki coupling of aryl boronate with 2-bromophenyl oxazoline with good yield and purity. This method overcomes many of the drawbacks associated with the previously reported syntheses.

PROCESS FOR PREPARING VALSARTAN

Provided is a process for preparing valsartan and precursors 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.

One-pot three-step solution phase syntheses of thiohydantoins using microwave heating

An efficient one-pot three-step solution phase protocol suitable for library syntheses of thiohydantoins was developed. The reactions included are in the following order, Negishi or Suzuki C-C coupling reactions, reductive amination and finally a cyclisation reaction. Protocols using a solid supported reagent and protocols suitable for combinatorial chemistry were developed, all including microwave heating.