摘要:
Process for preparing carbapenem derivative of the formula [I], which comprises subjecting azetidinone compound of the formula [II] to intramolecular cyclization reaction together with elimination reaction of the group of -SR⁴, followed by re-adding said group of -SR⁴ to the 2-position of the carbapenem skeleton of the intramolecularly cyclized compound, which is industrially useful as process for preparing carbapenem antimicrobials or synthetic intermediate therefor.
wherein R¹ is protected or unprotected hydroxy-substituted lower alkyl group, R² is hydrogen atom or ester residue, R³ is hydrogen atom or lower alkyl group, and the group of -SR⁴ is group which can be used as substituent at 2-position of the carbapenem antimicrobials.
wherein R¹ and R² are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R³ is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: -OR⁴ and -OR⁵ are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.
摘要:
A method for removing tri-substituted silyl group from β-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.