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青霉素(1a)自四十年代应用于临床以来,它在治疗上的卓越疗效及其脆奇的化学结构,促使人们对青霉素化学进行了广泛的研究,1949年已有较详尽的专著进行了综述。由于青霉素的化学不稳定性所带来的困难,直到1957年才成功地全合成了青霉素V(1b)(总收率约4％)。1959年,Batchlor等和Sheehan等又分别用不加前体的发酵和全合成的方法,制取了“无侧链青霉素”——6-氨基青霉烷酸(1c)(简称6-APA),使药物化学家能任意改变侧链结构,为此后半合成青霉素的发展开拓了广阔的道路,在短短几年中即已取得很大成就。至于头孢菌素C(2a)早在1955年即由Newton和Abraham发现,并在1961年确定了结
Penicillin (1a) Since its introduction into the clinic in the 1940s, its excellent therapeutic efficacy and its fragile chemical structure have led to extensive research on penicillin chemistry, with a more detailed monograph reviewed in 1949 . Penicillin V (1b) was not fully synthesized until 1957 (total yield of about 4%) due to the difficulties posed by the chemical instability of penicillin. In 1959, Batchlor et al. And Sheehan et al. Respectively used "unprotected fermentations and total synthesis methods to prepare 6-aminopenicillanic acid (1c) , So that drug chemists can arbitrarily change the structure of the side chain for the development of semi-synthetic penicillin has opened up a vast road, in a few short years has made great achievements. As for cephalosporin C (2a), which was discovered by Newton and Abraham as early as 1955 and established in 1961