专利号:US-5326885-A 优先权日:1992-05-01 标 题 :Process of preparing enriched enantiomers of glycerol carbonate and derivatives thereof for synthesis of β-blockers 发明人:OLIVERO ALAN G; CASSEL JONATHAN M; POULSEN JAMES R 权利人:COGNIS INC 摘要:Enriched enantiomers of glycerol Carbonate are produced under the influence of a hydrolytic enzyme, either by selective esterification of racemic glycerol carbonate or by selective hydrolysis of an ester of the racemate. The enriched enantiomeric product is readily converted to starting materials and intermediates useful in the synthesis of enantiomerically pure therapeutic agents, such as beta -adrenergic blockers.
专利号:US-6087512-A 优先权日:1996-09-18 标题:Process for preparation of glycidyl ether 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; YANAGIMOTO TETSUYA; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of a glycidyl ether which is characrelized in reacting an epoxy compound of the formula ##STR1## wherein X is halogen or sulfonyloxy in the presence of a fluoride salt, with an alcohol. According to the above method, glycigyl ethers or their optically active compounds important as intermediates for synthesis of medicines are easily obtained in good yield and especially the optically active compounds are obtained with highly optical purity.
专利号:US-6057476-A 优先权日:1996-09-18 标题:Process for the preparation of 3-amino-2-hydroxy-1-propyl ethers 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of 3-amino-2-hydroxy-1-propyl ether of the formula ##STR1## wherein R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic ring, R 2 and R 3 are the same or different hydrogen atom, a substituted or unsubstituted alkyl, or may form a ring together with an adjacent nitrogen atom, which ring may be interrupted with nitrogen atom, oxygen atom or sulfur atom, n which is characterized in reacting an epoxy compound of the formula ##STR2## wherein X is halogen, in the presence of a fluoride salt, with an alcohol and then reacting an amine. n According to the above method, an intermediates for synthesis of medicines is obtained in good yield and highly optical purity.
专利号:US-4171439-A 优先权日:1975-04-11 标 题 :Antibacterial analogs of isocephalosporins 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo or hydroxyl and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.
专利号:US-3957811-A 优先权日:1974-10-09 标题 :Process for 3-(1-[arylmethyl]tetrazol-5-yl)penams 发明人:NAKANISHI SUSUMU 权利人:PFIZER 摘要:A process for the synthesis of 6-(triphenylmethylamino)-2,2-dimethyl-3-(1-[arylmethyl]tetrazol-5-yl)penams, intermediates useful in the preparation of antibiotic penams, which comprises contacting in a reaction-inert solvent a 6-(triphenylmethylamino)-2,2-dimethyl-3-(alkyl- or arylsulfonyloxy[N-(arylmethyl)imino]methyl)penam with one to three equivalents of hydrazoic acid or with an ammonium, sodium or lithium azide at a reaction temperature of 20°-60° C., in the presence of more than one equivalent of pyridine.
专利号:US-4171438-A 优先权日:1975-07-23 标 题:0-2-Isocephem-4-carboxylic acid derivatives as antibacterial agents 发明人:DOUGLAS JAMES L; HORNING DONALD E; MORRIS LEESON R 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein X is acylamino and Z represents optionally substituted C1-C6 alkyl, aryl or aralkyl. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.
[参考文献]: Gerd Sigmund, Et Al. Monitoring 2-Phenylethanamine And 2-(3-Hydroxyphenyl)Acetamide Sulfate In Doping Controls. Drug Test Anal. 2015 Nov-Dec;7(11-12):1057-62.