4-Acetoxymethyl-Piperidine-1-Carboxylic Acid Benzyl Ester置于乙酰氯体系中,用 甲醇 用作溶剂,化学反应 4.5H,以89%的收率获得1-Cbz-4-羟甲基哌啶 参考文献:Mild And Chemoselective Deacetylation Method Using A Catalytic Amount Of Acetyl Chloride In Methanol 标题:Mild And Chemoselective Deacetylation Method Using A Catalytic Amount Of Acetyl Chloride In Methanol 摘要:在中等酸性条件下,使用催化量的乙酰氯在甲醇中实现了乙酸酯的高效脱乙酰化,成功地对各种伯醇,仲醇,芳香醇和糖醇的乙酸酯进行了脱保护.在其他常用酯存在的情况下,乙酰基的高选择性去除也以优异的收率实现.研究发现,这种通过酯交换介导的脱乙酰化反应的活性直接取决于乙酸酯的电子和立体性质. Doi:10.1055/s-2005-869838
专利号:US-2003203915-A1 优先权日:2002-04-05 标题 :Nitric oxide donors, compositions and methods of use related applications 发明人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI 权利人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI 摘要:The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO 2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.
专利号:US-9708336-B2 优先权日:2014-01-22 标题 :Metallo-beta-lactamase inhibitors 发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-2008280933-A1 优先权日:2006-07-25 标 题:Benzimidazolyl compounds 发明人:EFREMOV IVAN; ROGERS BRUCE N; DUPLANTIER ALLEN J; ZHANG LEI; ZHANG QIAN; MAKLAD NOHA S; EVRARD EDELWEISS; BRODNEY MICHAEL A 权利人:EFREMOV IVAN; ROGERS BRUCE N; DUPLANTIER ALLEN J; ZHANG LEI; ZHANG QIAN; MAKLAD NOHA S; EVRARD EDELWEISS; BRODNEY MICHAEL A 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n n n n n n n n n n as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2008312271-A1 优先权日:2006-07-25 标 题 :Azabenzimidazolyl compounds 发明人:EFREMOV IVAN; ROGERS BRUCE N; DUPLANTIER ALLEN J; ZHANG LEI; ZHANG QIAN; MAKLAD NOHA S 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n n n n n n n n n n as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.