摘要:
The present invention provides a process for preparing a penicillanic acid derivative of the formula which comprises reacting lead with a halogenated penicillanic acid derivative of the formula wherein X, Y, Z and R¹ are defined in the specification. The reaction is conducted more advantageously in the presence of a metal having higher ionization tendency than lead.
wherein R 1 means hydrogen, halogen, amino or protected amino; R 2 means hydrogen, halogen, lower alkoxy, lower acyl, lower alkyl, hydroxy- or protected hydroxy-substituted lower alkyl, hydroxy or protected hydroxy, or R 1 and R 2 may jointly represent oxo; R 3 means hydrogen or a carboxy-protecting group; R 4 means hydrogen; R 5 means a group of the formula -CH 2 Y where Y means halogen, -N 3 , - ON0 2 , -OR 6 , -OCOR 6 , -SCSOR 6 , -SCSN(R 6 ) 2 , -SR 6 , -S0 2 R 6 , - NHR 6 , -N(R 6 ) 2 or a substituted or unsubstituted nitrogen-containing heterocyclic group having a free valence on nitrogen; R 6 means a lower alkyl, aryl or heterocyclic group which is substituted or unsubstituted; or R 4 and R 5 may jointly represent =CH 2 ; n means 0, 1 or 2; provided, however, that where R 4 and R 5 jointly represent =CH 2 , n is not equal to 0.
wherein R 1 means hydrogen, halogen, amino or protected amino; R 2 means hydrogen, halogen, lower alkoxy, lower acyl, lower alkyl, hydroxy- or protected hydroxy-substituted lower alkyl, hydroxy or protected hydroxy, or R 1 and R 2 may jointly represent oxo; R 3 means hydrogen or a carboxy-protecting group; R 4 means hydrogen; R 5 means a group of the formula -CH 2 Y where Y means halogen, -N 3 , - ON0 2 , -OR 6 , -OCOR 6 , -SCSOR 6 , -SCSN(R 6 ) 2 , -SR 6 , -S0 2 R 6 , - NHR 6 , -N(R 6 ) 2 or a substituted or unsubstituted nitrogen-containing heterocyclic group having a free valence on nitrogen; R 6 means a lower alkyl, aryl or heterocyclic group which is substituted or unsubstituted; or R 4 and R 5 may jointly represent =CH 2 ; n means 0, 1 or 2; provided, however, that where R 4 and R 5 jointly represent =CH 2 , n is not equal to 0.
摘要翻译:通式的penam衍生物,其中R 1表示氢,卤素,氨基或被保护的氨基; R 2表示氢,卤素,低级烷氧基,低级酰基,低级烷基,羟基或保护的羟基取代的低级烷基,羟基或保护的羟基,或R 1和R 2可以共同表示氧代; R 3表示氢或羧基保护基; R 4表示氢; R 5表示式-CH 2 Y的基团,其中Y表示卤素,-N 3,-ONO 2,-OR 6,-OCOR 6,-SCSOR 6,-SCSN(R 6)2 ,-SR 6,-SO 2 R 6,-NHR 6,-N(R 6)2或取代或未取代的在氮上具有游离价的含氮杂环基; R 6表示取代或未取代的低级烷基,芳基或杂环基; 或R 4和R 5可以共同表示= CH 2; n表示0,1或2; 但是,当R 4和R 5共同表示= CH 2时,n不等于0。
摘要:
The present invention provides a process for preparing a 1,1-disubstituted ethylene derivative of the formula which comprises reacting lead with a carbinol derivative of the formula wherein R¹, R², R³, X, Y, m and n are defined in the specification. The reaction is conducted more advantageously in the presence of a metal having higher ionization tendency than lead.