摘要 |
<p>PURPOSE:To obtain a new intermediate useful for the practical synthesis of a 1beta-substituted carbapenem derivative having strong antibacterial activity and chemical stability and stable even to dihydropeptidase existing in vivo. CONSTITUTION:The compound of formula I {R<1> is H or OH-protecting group; R<2> is 1-6C alkyl, 1-6C alkoxy, halogen, phenyl or phenoxy; R<3> is CYR<5>R<6> [Y is O or S; R<5> and R<6> are 1-6C alkyl phenyl or together form (CH2)m(X)L(CH2)n ((m) and (n) are 0-5; m+n>=2; L is 0 or 1; X is O0]; R<3>' is H, 1-6C alkyl, 1-6C alkoxy, OH, halogen, CN, NO2 or NH2; R<4> is H or carboxy-protecting group; (k) is 0-2}, e.g. (1R,5S,6S)-2-(2-diethylcarbamoyphenylthio)-1-methyl-6-[(R)-1- trimwethylsililoxyethyl]-1-carbapen-2-em-3-carboxylic acid 4-nitrobenzyl ester.</p> |