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氧青霉烷类抗生素是近年来新发现的一类新抗生素,它具有抗细菌、抗真菌、抗肿瘤及抑制β-内酰胺酶的作用,引起人们很大的关注。 由1,2,4-丁三醇出发,用异丙叉基将相邻的二羟基保护,使4-羟基苯甲酰化,水解去掉异丙叉基后,将1-羟基选择性地对甲苯磺酰化,每经叠氮基转变成氨基,生成的化合物与醋酸缩合,得二氧唑的化合物,最后与氯乙酰氯缩合,形成β-内酰胺环,制得目的化合物,产物和中间体的结构经IR、~1H-NMR、C~(13)-NMR及MS等确证无疑。
Oxapenem antibiotics is a newly discovered class of new antibiotics in recent years. It has anti-bacterial, anti-fungal, anti-tumor and inhibit the role of β-lactamase, aroused great concern. Starting from 1,2,4-butanetriol, the adjacent dihydroxy group is protected with an isopropylidene group to effect the 4-hydroxybenzoylation. After the isopropylidene group is hydrolyzed to remove the 1-hydroxy group selectively Tosylate, each azido group into amino, the resulting compound condensation with acetic acid to give a compound of oxadiazole, and finally chloroacetyl chloride condensation, the formation of β-lactam ring, the desired compound, the product and the middle Structure of the body by IR, ~ 1H-NMR, C ~ (13) -NMR and MS confirmed no doubt.