To obtain the subject new compound useful as a cysteine protease inhibitor excellent in oral absorbability, tissue migration properties, cell wall permeability, etc.
This compound is represented by formula I [R1 is a (substituted) 6-14C aryl or a (substituted) heterocyclic residue; R2 is H or an (aryl-substituted) 1-10C alkyl; R3 is H or a group represented by the formula; R4-CO (R4 is a 1-10C alkyl); A is an (alkyl-substituted) 1-3C alkylene], e.g. (3S)-3-{(S)-2-(4,6- dimethoxy-2-pyrimidinyl)amino-4-methylvalerylamino}-2-tetrahydrofuranol. The compound represented by formula I in which R3 is H is obtained by reacting a compound represented by the formula R1X with an amino acid salt represented by formula II, providing an amino acid derivative represented by formula III, then reacting the resultant compound with an aminolactone derivative represented by formula IV and treating the resultant lactone derivative represented by formula V with a reducing agent such as diisopropylaluminum hydride.
MASUDA HIROKAZU
ANDO NAOKO
NAKAO AKIRA
ANDO RYOICHI
YOSHII SHIGEHIKO
SAITO KENICHI
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