摘要 |
<p>PURPOSE:To obtain the title compound which is an anticarcinogenic immunizing agent, etc., in high yield, by the diazotization of 3-amino-2-hydroxy-4-p- aminophenylbutanoylleucine derivative obtained from easily available bestatin, followed by the decomposition. CONSTITUTION:3-Amino-2-hydroxy-4-p-aminophenylbutanoylleucine derivative of formula I(R1 is H; R2 is amino-protecting group; R1 and R2 may form a phthalyl group; R3 is H or protecting group of COOH) is converted into diazonium salt by acting diazotizing agent on it. The title compound of formula II(R4 is H or amino- protecting group; R1 and R4 may form a phthalyl group; R5 is H or protecting group of COOH) is obtained by the decomposition of the diazonium salt. The compound I is produced from bestatin obtained by synthesis or fermentation.</p> |