| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new compound, having nitrogen atom at the 10-position and useful as an antimicrobial agent for treating microbism or a synthetic intermediate therefor. SOLUTION: This compound is represented by formula I [R<0> is H or a protecting group of OH; R<1> is H or a protecting group of carboxy group; R<2> is H or a protecting group of secondary amino group, a (substitute) lower alkyl, etc.], e.g. 10-(2-aminoethyl)-5-(1-hydroxyethyl)-4-oxo-3,10- diazatricyclo[5.4.0.0<3.6> ]undec-1-ene-2-carboxylic acid. The compound represented by formula I is obtained by reacting a compound represented by formula II with an oxalyl chloride derivative, then reacting the resultant compound with a phosphorus compound (e.g. triethyl phosphite), thermally cyclizing the resultant phosphonium ylide compound represented by formula III (R<6> and R<7> are each a lower alkyl, alkoxy, etc.), and then, as necessary, deptotecting the otained compound. The compound is capable of manifesting excellent stability to a β-lactamase or a dehydropeptidase I. |
