Microwave-assisted synthesis of azetidines in aqueous media
摘要:
Simple azetidines are synthesized in good to excellent yields and high purity via cyclization of 3-(ammonio nio)propyl sulfates derived from primary amines and the cyclic sulfate of 1,3-propanediol. A feature of this methodology includes the accelerated synthesis of azetidines in water under the influence of microwave-assisted heating. (C) 2009 Elsevier Ltd. All rights reserved
2-ARYLMETHYLAZETIDINE-CARBAPENEM-3-CARBOXYLIC ACID ESTER DERIVATIVE OR ITS SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
申请人:Choi Young-Ro
公开号:US20110118229A1
公开(公告)日:2011-05-19
The present invention provides a 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives or their pharmaceutically acceptable salts show high oral absorption rate, and thus can be orally administered. The active metabolites thereof have a broad spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial activities against methicillin-resistant
Staphylococcus aurus
(MRSA) and quinolone-resistant strains (QRS). In particular, the acid addition salts of the 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives are obtained in crystalline forms having excellent stability.
NOVEL CYCLOSPORIN DERIVATIVES FOR THE TREATMENT AND PREVENTION OF A VIRAL INFECTION
申请人:Su Zhuang
公开号:US20130303438A1
公开(公告)日:2013-11-14
The present invention relates to a compound of the formula (I): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection using the same.
Process for the preparation of an azetidine and intermediates therefor
申请人:A.H. ROBINS COMPANY, INCORPORATED
(a Delaware corporation)
公开号:EP0279543A1
公开(公告)日:1988-08-24
A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.