📜6-氨基青霉烷酸,苯基丙二酸单苯酯 反应生成羧苄青霉素苯酯 参考文献:Preparation,Hydrolysis,And Oral Absorption Of .Alpha.-Carboxy Esters Of Carbenicillin 标题:Preparation,Hydrolysis,And Oral Absorption Of .Alpha.-Carboxy Esters Of Carbenicillin 摘要:Twelve Alpha-Carboxy Esters Of Carbenicillin,A Parenteral Broad Spectrum Semisynthetic Penicillin,Were Synthesized And Examined As Potential Oral Carbenicillin Derivatives. The Rates At Which The Esters Were Hydrolyzed In Vitro To Carbenicillin By Animal And Human Tissues Were Compared And The Carbenicillin Serum Levels Arising After Oral Administration Of The Esters Were Measured In Squirrel Monkeys And Human Volunteer Subjects. The Alpha-Carboxyphenyl Ester Of Carbenicillin [carfecillin (British Pharmacopoeia Approved Name),Brl 3475] Was Selected For Further Study And Is Presently Undergoing Clinical Trial. Doi:10.1021/jm00236A013
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-2005239725-A1 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
专利号:US-4452796-A 优先权日:1982-06-14 标题:6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors 发明人:BARTH WAYNE E 权利人:PFIZER 摘要:Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, used in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.
专利号:US-2005070715-A1 优先权日:2003-07-15 标 题:Methods for synthesis of acyloxyalkyl compounds
1: Humphrey MJ, Filer CW, Jeffery DJ, Langley PF, Wadds GA. The availability of carfecillin and its phenol moiety in rat and dog. Xenobiotica. 1980 Oct;10(10):771-8. Russian. Russian. Russian. Japanese. Italian. 15: Jedlicková Z, Rýc M, Libánská A. Combination effect with some aminoglycoside antibiotics. J Hyg Epidemiol Microbiol Immunol. 1981;25(2):204-6.