A FACILE SYNTHESIS OF BESTATIN
RINZO NISHIZAWA, TETSUSHI SAINO, MASAO SUZUKI, TADASHI FUJII, TADASHI SHIRAI, TAKAAKI AOYAGI, HAMAO UMEZAWA
著者情報
1983 年 36 巻 6 号 p. 695-699
詳細
1983 年 36 巻 6 号 p. 695-699
Bestatin, an immunomodulator useful in cancer treatment with the structure: N-[(2S, 3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, has been synthesized from N-acyl-α-aminoacetophenone. This novel method using readily available reagents and mild conditions can be applied to a large scale production of this useful agent. The overall yield of bestatin was 10.5% from N-acetyl-α-aminoacetophenone and 7.8%. from N-benzoyl-α-aminoacetophenone. Bestatin(1) is an aminopeptidase B inhibitor discovered in a culture filtrate of Streptomyces1-3 ).
