CAS: 127254-12-0; Sitafloxacin

上下游产品

-5-azaspiroheptane7-(S)-amino-5-1(R)-phenylethyl-5-azaspiro2.4heptane (7S)-5-azaspiro[2.4]heptan-7-ylcarbamic acid tert-butyl ester -4-oxo-5-azaspiroheptane7-(S)-amino-5-1(R)-phenylethyl-4-oxo-5-azaspiro2.4heptane -5--5-azaspiroheptane7(S)-(tert-butoxycarbonyl)amino-5-1(R)-phenylethyl-5-azaspiro2.4heptane

在 三氟乙酸体系中,用 氯仿 用作溶剂,以97.3%的收率获得西他沙星
参考文献:一种西他沙星制备方法
标题:一种西他沙星制备方法
摘要:本发明公开了一种西他沙星的制备方法,包括以下步骤:取原料4‑溴乙酰乙酸乙酯与1,2‑二溴乙烷充分反应,所得产物在羰基还原酶的作用下,制备得到化合物ⅱ;在碳酸铯存在下,取化合物ⅱ与苄胺在溶剂中进行环合反应,所得产物再与dppa反应,制备得到化合物ⅳ;将化合物ⅳ的叠氮基团还原,制备得到化合物ⅴ;将化合物ⅴ的伯胺基团连上boc保护基团,得到化合物ⅵ;将化合物ⅵ经pd/c还原,所得产物与8‑氯‑6,7‑二氟‑1‑[(1R,2S)‑2‑氟代环丙烷基]‑4‑氧代‑1,4‑二氢喹啉‑3‑羧酸乙酯反应制备得到化合物ⅷ;化合物ⅷ进行脱保护即得.本发明西他沙星的制备步骤少,后处理简单,收率相对较高.

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2010143980-A1
优先权日:2007-02-22
标题:Synthesis of novel xylosides and potential uses thereof
发明人：BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM
权利人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM
摘要:The present invention includes a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, the xyloside having a chemical structure of one of Formula (1), Formula (2), Formula (3), Formula (4), Formula (5), Formula (6), Formula (7), Formula (8), Formula (9), or Formula (10) as shown herein. Also, the present invention includes a method of making a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, wherein the method is performed with “Clickâ€? chemistry. Additionally, the present invention includes a method of administering a xyloside so as to induce synthesis of a glycosaminoglycan in a cell.

专利号:US-6350878-B1
优先权日:1998-05-18
标 题 :Intermediates for the synthesis of epothilones and methods for their preparation
发明人：ALTMANN KARL-HEINZ; BAUER ARMIN; SCHINZER DIETER
权利人:NOVARTIS AG
摘要:The invention relates to a method of synthesis for a compound of formula (I),wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.

专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-6846917-B2
优先权日:2001-01-23
标题:Solid- and solution-phase synthesis of heparin and other glycosaminoglycans
发明人：SEEBERGER PETER H; ORGUEIRA HERNAN; SCHELL PETER
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.

专利号:US-8536153-B2
优先权日:2008-11-04
标 题 :Chemical synthesis of phosphatidylinositol mannoside glycans from Mycobacterium tuberculosis
发明人：SEEBERGER PETER H; BOONYARATTANAKALIN SIWARUTT; LEPENIES BERND
权利人:SEEBERGER PETER H; BOONYARATTANAKALIN SIWARUTT; LEPENIES BERND; MAX PLANCK GESELLSCHAFT
摘要:The efficient synthesis of phosphatidylinositol mono- to hexa-mannoside (PIM 1 to PIM 6 ) is reported. The invention relates to these phosphatidylinositol mono- to hexa-mannosides carrying a linker and a reactive functional group, e.g. the sulfhydryl group, a protein, a fluorescent probe, or a solid phase. The invention further relates to vaccines comprising the PIMs linked to a carrier protein or an antigen.