✍ Scribed by Shoichiro Uyeo; Hikaru Itani
No coin nor oath required. For personal study only.
Rcclction of acctoxy-xxctidinone 4, (Z)-crotylbromidc 5 xnd Zn sclcctively gave 6. which was eollvcrtcd to @-~Yl-2-chYdroXY-ttYl~ 11,8kcyiatcmlcdiateinayllW&30f xntibia6c2,inlQbovcrxllyield. 2-Functionalized-methyl-1 ~methylcarbapenem antibiotics 1 1.2, which can be clearly distinguished from conventional-type le-methylcarbapenems represented by meropenem (W-7338) 3 3, have recently at&a&d much attention because of their high therapeutic potential. In the course of OUT project to develop carbapenem antibiotics, we have found that 2-(N-methyl4pyridinio)thiomethyl derivative 2 showed excellent in viva as well as in vitro activity against both Gram-pitive and -negative bac&a 4. M 1 Y=Na X=OAcyl ONMe
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AbstractÐThe 2a-functionalized 1b-methylcarbapenems 3 were synthesized from the 2-formyl 1b-methylcarbapenem intermediate 5. The best compound in the series of 2a-(hydroxy)alkylcarbapenems, KR-21012, displayed well balanced in vitro and in vivo activity as a parent compound of oral carbapenem.