申请人:Rhone-Poulenc Industries
公开号:US04520193A1
公开(公告)日:1985-05-28
The invention provides new cephalosporin derivatives of the general formula, ##STR1## which are in the form of a bicyclooct-2-ene or bicyclooct-3-ene, in which formula R.sub.1 is a radical of the general formula ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an amino-protecting radical, R.sub.2 is an acid-protecting radical and R.degree. represents various organic radicals, or alternatively R.sub.1 is an amino-protecting radical or various acyl radicals, R.sub.2 is a protective radical and R.degree. represents various organic radicals, and R.sub.3 and R.sub.4 are alkyl radicals optionally substituted by alkoxy or dialkylamino, or phenyl radicals, or --NR.sub.3 R.sub.4 forms a heterocyclic ring. These products are intermediates for the synthesis of cephalosporins having antibacterial activity.
本发明提供了一种新的头孢菌素衍生物,其一般式为##STR1##,其形式为双环辛二烯或双环辛三烯,在该式中,R.sub.1是一般式##STR2##的基团[其中R.sub.5是氢,烷基,乙烯基,氰甲基,保护羧基烷基或保护基团,R.sub.6是保护基团]或氨基保护基团,R.sub.2是酸保护基团,R.degree.表示各种有机基团,或者R.sub.1是氨基保护基团或各种酰基基团,R.sub.2是保护基团,R.degree.表示各种有机基团,R.sub.3和R.sub.4是烷基,可以被烷氧基或二烷基氨基取代,或苯基,或--NR.sub.3 R.sub.4形成杂环环。这些产品是合成具有抗菌活性的头孢菌素的中间体。