CAS: 56187-47-4; (6R,7R)-7-(2-(3,5-Dichloro-4-Oxopyridin-1(4H)-yl)Acetamido)-3-(((5-Methyl-1,3,4-Thiadiazol-2-yl)Thio)Methyl)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid

上下游产品

2-(3,5-dichloro-4-oxopyridine-1(4H)-yl)acetic acid (6R,7R)-7-amino-3-(5-methyl-1,3,4-thiadiazol-2-ylthiomethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]°Ct-2-ene-2-carboxylic acid 3-deacetyloxy-7-amin°Cephalosporanic acid 2-mercapto-5-methyl-1,3,4-thiadiazole(6R,7R)-3-[[(5-methyl-1,3,4-thiadiazolyl-2-yl)thio]methyl]-7-[2-(3,5-dichloro-4-pyridone-1-acetylamido)]-8-oxo-5-thia-1-azabicyclo[4.2.0]°Ct-2-ene-2-carboxylic acid sodium salt

7-氨基头孢烷酸置于三氟化硼乙醚,溶剂黄146,三乙胺体系中,用 乙腈 作为反应溶剂,化学反应 0.5H,反应生成 头孢西酮
参考文献:一种头孢西酮的合成工艺
标题:一种头孢西酮的合成工艺
摘要:本发明公开了一种头孢西酮的合成工艺,本发明将化合物ⅱ与7‑aca反应制备化合物ⅲ,化合物ⅲ与化合物ⅳ反应制得终产品头孢西酮(ⅰ).本发明合成路线简单,反应条件温和,缩短了反应周期,降低了生产成本低,提高了产品总收率及纯度,适合工业化生产.

专利信息

专利号:US-5945414-A
优先权日:1996-12-03
标 题:Process for the preparation of new intermediates useful in the synthesis of cephalosporins
发明人：SOGLI LORIS; TERRASSAN DANIELE; BERNASCONI ERMANNO; SALTO FRANCISCO
权利人:ANTIBIOTICOS SPA
摘要:Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: with a compound of formula (II): R-SH(II) wherein R is 5-methyl-1,3,4-thiadiazol-2-yl, 1H-1,2,3-triazol-4-yl, 1-methyl-tetrazol-5-yl or 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl group, and R1 and R2 are both hydrogen and the other is an acyl group, in an aqueous solution in an amount of 3-5 mols per mol of glutaryl 7-ACA to about 90 DEG C. and for a time from about 2 to about 10 hours; optionally recovering the excess of the compound of formula (II), thereby preparing a compound of formula (III) in an aqueous solution: wherein R is as above defined and optionally deacylating said compound of formula (III); and converting the resulting compound of formula (I) wherein R, R1 and R2 are as defined above in the presence of a non-chlorinated solvent into one of said cephalosporins.

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:US-5387679-A
优先权日:1991-07-15
标题 :Process for the preparation of cephalosporins intermediates
发明人：SOGLI LORIS; TERRASSAN DANIELE; RIBALDONE GIUSEPPE
权利人:ANTIBIOTICOS SPA
摘要:PCT No. PCT/EP92/01595 Sec. 371 Date Mar. 15, 1993 Sec. 102(e) Date Mar. 15, 1993 PCT Filed Jul. 14, 1992 PCT Pub. No. WO93/02085 PCT Pub. Date Feb. 4, 1993.The present invention relates to a process for preparing a compound of formula (I) ntains at least one nitrogen atom with or without oxygen or sulphur and R1 and R2 are both hydrogen atoms or one of them is an hydrogen atom and the other is an acyl group; the process comprising reacting a compound of formula (II) (II) wherein R1 and R2 are each as defined above, and wherein, if necessary, any reactive group is protected by a suitable protective group, or a salt thereof, with a compound of formula (III) R-SH(III) wherein R is as defined above, or a salt thereof, in the presence of an acid and of a compound of formula (IV) (IV) wherein each of R3 and R4 is a C1-C4 alkyl group or R3 and R4 taken together are a C2 or C3 alkylene chain and, if necessary, removing the protective groups possibly present. The compounds of formula (I) are useful intermediates in the synthesis of Cefazolin and Cefazedone.

专利号:WO-0032619-A1
优先权日:1998-11-30
标题:Methods and compositions for identification of inhibitors of ribosome assembly
发明人：DAMMEL CAROL S; WATSON JULIE C
权利人:RIBOGENE INC
摘要:The invention provides a means for identifying novel antibiotics by screening for compounds that inhibit bacterial ribosome assembly and ribosomal protein synthesis, which comprises the screening of test compounds to identify those that inhibit the activity of a bacterial ribosomal protein. The in vitro and in vivo assays detect (a) increased translation of a reporter mRNA that is normally repressed in the presence of a ribosomal protein, (b) increased growth in cells that over-express ribosomal protein, and (c) decreased binding of the ribosomal protein to its target RNA. The invention encompasses the (a) methods of screening and testing compounds by the above methods, (b) compounds that are identified in the assay which inhibit ribosome assembly and protein synthesis and (c) methods for treatment using said compounds.

专利号:US-2025002508-A1
优先权日:2020-05-05
标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
发明人：HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
权利人:QPEX BIOPHARMA INC
摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).