Spry D O, Snyder N J, Kasher J S
Lilly Research Laboratory, Eli Lilly & Company, Indianapolis, Indiana 46285.
J Antibiot (Tokyo). 1989 Nov;42(11):1653-60. doi: 10.7164/antibiotics.42.1653.
A series of C(3)-cyclopropyl cephems and carbacephems has been prepared by palladium catalyzed addition of diazomethane to the corresponding C(3)-vinyl derivatives. The phenylglycyl cyclopropyl cephem derivatives exhibit better Gram-positive activity than cephalexin or cefaclor, while the aminothiazole oxime cyclopropyl cephem derivatives were not as active as the corresponding C(3)-vinyl cephems.
通过钯催化重氮甲烷与相应的C(3)-乙烯基衍生物加成反应，制备了一系列C(3)-环丙基头孢烯和碳头孢烯。苯基甘氨酰环丙基头孢烯衍生物显示出比头孢氨苄或头孢克洛更好的革兰氏阳性菌活性，而氨基噻唑肟环丙基头孢烯衍生物的活性不如相应的C(3)-乙烯基头孢菌素。
