366016-77-5

Upstream product

• 2930-05-4 Benzyloxymethyl-oxiran 
• 137618-52-1 4-(benzyloxy)-3-hydroxybutanenitrile 
• 100-51-6 benzyl alcohol 
• 7677-24-9 trimethylsilyl cyanide 
• 2930-05-4 (S)-benzyl glycidyl ether 

Downstream Products

• 366016-78-6 (S)-4-(benzyloxy)-3-hydroxybutanenitrile 
• 147849-64-7 tert-butyl (S)-6-(benzyloxy)-5-hydroxy-3-oxohexanoate 

Relevant academic research and scientific papers

Efficient lipase-catalyzed kinetic resolution of 4-arylmethoxy-3-hydroxybutanenitriles: application to an expedient synthesis of a statin intermediate

The kinetic resolution of 4-arylmethoxy-3-hydroxybutanenitriles was investigated by lipase-catalyzed transesterification in organic solvents. A high enantioselectivity was obtained via reaction with vinyl acetate in a mixed solvent (n-heptane/acetonitrile 1:1), which was catalyzed by the lipase from Artgribacter sp. A better selectivity was demonstrated when the number of substituents on the aryl ring increased. (S)-4-Arylmethoxy-3-hydroxybutanenitriles can be obtained with enantiomeric excesses of up to 98.0% by this method. Furthermore we have developed a novel route to synthesize tert-butyl (S)-6-benzyloxy-5-hydroxy-3-oxohexanoate, a key intermediate for the preparation of HMG-CoA reductase inhibitors (statins).

Preventive/therapeutic method for cancer

This invention provides a prophylactic or therapeutic method for cancer. A prophylactic or therapeutic method for cancer, which is characterized by selectively inhibiting ErbB-2 (HER2) to block information signals of multimers of the epithelial growth factor receptor family.

MEDICINAL COMPOSITIONS IMPROVED IN SOLUBLITY IN WATER

Solid dispersions are provided comprising an HER2 inhibitor which is hardly or not soluble in water and a hydrophilic polymer. These solid dispersions have been improved in the solubility of the HER2 inhibitor, oral absorption and bioavailability in blood

MEDICINAL COMPOSITIONS HAVING IMPROVED ABSORBABILITY

An HER2 inhibitor having an average particle size of about 3 μm or less or a composition containing the same which has improved HER2 inhibitor-absorbability.

Heterocyclic compounds their production and use

A compound represented by the formula: wherein m is 1 or 2, R1 is a halogen or an optionally halogenated C1-2 alkyl; one of R2 and R3 is a hydrogen atom and the other is a group represented by the formula: wherein n is 3 or 4; R4 is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.