Meesschaert B, Adriaens P, Eyssen H
J Antibiot (Tokyo). 1976 Apr;29(4):433-7. doi: 10.7164/antibiotics.29.433.
The synthesis of benzylpenicillin and 6-aminopenicillanic acid, labeled with tritium in the beta-methyl group, is described. Benzylpenicillin S-sulfoxide benzyl ester is refluxed in benzene and tritiated water and is successively debenzylated and deoxygenated to (beta-methyl-3H)-benzylpenicillin. Removal of the side chain with a bacterial acylase gives (beta-methyl-3H)-6-aminopenicillanic acid.
本文描述了在β-甲基上用氚标记的苄青霉素和6-氨基青霉烷酸的合成。苄青霉素S-亚砜苄酯在苯和氚化水中回流,依次进行脱苄基和脱氧反应,得到(β-甲基-³H)-苄青霉素。用细菌酰基转移酶去除侧链,得到(β-甲基-³H)-6-氨基青霉烷酸。