CAS: 143383-65-7; 1-Cyclopropyl-6-Fluoro-8-Methoxy-7-((R)-3-((S)-1-(Methylamino)Ethyl)Pyrrolidin-1-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

上下游产品

3R,1S-1-cyclopropyl-6-fluoro-7-[3-(1-N-tertbutoxycarbonyl-N-methylaminoethyl)-1-pyrrolidinyl]-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 26H33BF3N3O6C26H33BF3N3O6 -methylcarbamate1,1-dimethylethyl -methyl1-(3-pyrrolidinyl)ethylcarbamate 1-cyclopropyl-1,4-dihydro-6,7-difluoro-8-methoxy-4-oxo-quinoline-3-carboxylic acid difluoroborate ester

📜1,1-Dimethylethyl-Methyl<1-(3-Pyrrolidinyl)Ethyl>Carbamate置于盐酸,乙醇,三乙胺体系中,用 1,4-二氧六环,二氯甲烷,乙腈 用作溶剂,化学反应生成沛马沙星
参考文献:新型含腈氟喹诺酮类抗菌剂的合成及生物学评价.
标题:新型含腈氟喹诺酮类抗菌剂的合成及生物学评价.
摘要:据报道,几种新的含弱碱性胺类的含腈氟喹诺酮类药物具有减少的herg(人醚-Go-Go-Go基因)通道抑制作用的潜力,如多芬替利试验所测.新的氟喹诺酮类药物对革兰氏阳性和革兰氏阴性菌株均有效,包括耐甲氧西林的金黄色葡萄球菌和耐氟喹诺酮的肺炎链球菌.通过克隆形成性测试,几种类似物还显示出较低的人类遗传毒性潜力.具有非常好的体外活性和体外安全性的化合物22和37(分别命名为pf-00951966和pf-02298732)在大鼠中也显示出非常好的药代动力学特性.
Doi:10.1016/j.Bmcl.2007.01.090

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-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:US-2005222431-A1
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-7227028-B2
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-2007244331-A1
优先权日:2003-12-30
标 题 :Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof