Novel carbapenem derivatives of quarternary salt type
申请人:——
公开号:US20030022881A1
公开(公告)日:2003-01-30
An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof:
1
wherein R
1
represents H or methyl; R
2
and R
3
each independently represent H, halogen, lower alkyl or the like; R
4
represents optionally substituted lower alkylthio or the like; and R
5
represents optionally substituted lower alkyl or the like.
Iron(III)-Catalyzed Radical Cross-Coupling of Thiols with Sodium Sulfinates: A Facile Access to Thiosulfonates
作者:Lal Yadav、Twinkle Keshari、Ritu Kapoorr
DOI:10.1055/s-0035-1562101
日期:——
A convenient and efficient synthesis of symmetrical and asymmetric thiosulfonates from thiols and sodiumsulfinates is reported. The protocol involves iron(III)-catalyzed formation of sulfenyl and sulfonyl radicals in situ under aerobic conditions and their subsequent cross-coupling to afford thiosulfonates in 83–96% yield. The utilization of readily available, nontoxic, and inexpensive iron(III) as
Generation and fate of nondecarboxylating acyloxy radicals derived from the photolysis of acyl derivatives of N-hydroxy-2-thiopyridone
作者:Derek H.R. Barton、Manlan Ramesh
DOI:10.1016/s0040-4039(00)94400-9
日期:1990.1
The acyl derivatives of 1 with the acyl group linked to aryl, vinyl etc. give on photolysis carboxy radicals. These radicals, by attack on the thiopyridone function, afford thio-peresters which are the real precursors of the anhydrides observed before. The benzoyloxy radical from 2 can be trapped by ethylvinyl ether to give adduct 14 in promising yield.
An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof:
wherein R1 represents H or methyl; R2 and R3 represent H, a halogen atom, alkyl or the like; and R4 represents substituted lower alkylthio or the like.
An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and β-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof:
wherein R1 represents H or methyl; R2 and R3 represent H, a halogen atom, alkyl or the like; and R4 represents substituted lower alkylthio or the like.