| 摘要 |
<p>PURPOSE: To efficiently obtain the subject derivative useful as an intermediate for the carbapenem derivatives of antibiotics in a large amount by using a compound having a R(S) configuration and represented by a specific formula as a starting raw material. CONSTITUTION: (A) A compound of formula I (X is halogen; R<1> is H, an OH- protecting group; R<2> is a carboxyl-protecting group) having a R(S) configuration is reacted with (B) an alkali metal azide (e.g. lithium azide) in dimethylformamide, etc., at 80-110 deg.C for 4-7hrs, and the produced compound of formula II is reduced. The produced compound of formula III is subjected to a ring-closing reaction to obtain the objective compound of formula IV. For example, the reduction reaction is preferably a hydrogenation reaction performed in the presence of a catalyst such as 5-10% palladium-carbon catalyst in an organic solvent such as methanol at 10-30 deg.C under a hydrogen gas pressure of 1-4 atmospheric pressure for 0.5-2hrs.</p> |
