| 摘要 |
PURPOSE:To provide a new peptide compound having a specific amino acid sequence, exhibiting pharmacological actions such as endothelin antagonistic action and useful for the treatment and prevention of hypertension, stenocardia, myocardial infarction, cerebral infarction, asthma, chronic renal insufficiency, etc. CONSTITUTION:This peptide compound expressed by formula III and exhibiting pharmacological action such as endothelin antagonistic action can be produced by reacting an ethyl acetate solution of (S)-alpha-benzyloxycarbonyl-gamma-methylbutyl isocyanate with an L-valine dimethylamide hydrochloride in the presence of triethylamine, reacting the reactional product with hydrogen in methanol in the presence of 10% palladium-carbon to obtain N-[N-{(1S)-1- dimethylcarbamoyl-2--methylpropyl}carbamoyl]-L-leucine of formula I and reacting the product with a compound of formula II [R<1> is H or lower alkyl; D-Pya is D-(2-pyridyl)alanine]. |
