📜Alkaline Earth Salt Of/the/ Methylsulfuric Acid 反应生成 溴美喷酯 参考文献:Antispasmodics. Ii. Derivatives Of N-Substituted-3-Piperidols 标题:Antispasmodics. Ii. Derivatives Of N-Substituted-3-Piperidols 摘要: DOI:10.1021/ja01613A068
专利号:US-2004077674-A1 优先权日:2002-03-01 标题:Mappicine analogs, intermediates in the synthesis of mappicine analogs and methods of synthesis of mappicine analogs 发明人:CURRAN DENNIS P; PARNIAK MICHAEL A; GABARDA ANA; ZHANG WEI; LUO ZHIYONG; CHEN CHRISTINE HIU-TUNG 摘要:A compound having the following structure: n n n wherein Z is —CHOR 1 R 2 or —C(O)R 2 ; R 1 is H, an alkyl group, an aryl group, —OC(O)OR a , wherein R a is an alkyl group, —C(O)R b wherein R b is an alkyl group, an aryl group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, an aryl amino group, a diarylamino group, an arylalkyl amino group, a protecting group or a fluorous tag; R 2 is an alkyl group, an aryl group or an arylalkyl group; R 3 is H, an alkyl group, hydroxyalkyl group or an aryl group; R 4 —R 8 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, an alkoxy group, an aryloxy group, an acyloxy group, a haloalkyl group, a perfluoroalkyl group, fluorine, chlorine, bromine, a haloalkyloxy group, a carbamoyloxy group, a hydroxy group, a nitro group, a cyano group, a cyanoalkyl group, an azido group, an azidoalkyl group, a formyl group, a hydrazino group, a hydrazinoalkyl group, a hydroxyalkyl group, an alkoxyalkyl group, —NR 1 R m , wherein R 1 and R m are independently hydrogen, an alkyl group, an aryl group, an arylalkyl group, or —C(O)R b , an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an aryl aminoalkyl group, a diarylaminoalkyl group, an arylalkyl aminoalkyl group, —OC(O)OR a , wherein R a is an alkyl group, —C(O)R b , —SR c , S(O)R c or S(O 2 )R c wherein R c is hydrogen, —C(O)R b , an alkyl group, or an aryl group, (CH 2 ) n SiR d R e R f wherein n is an integer within the range of 0 through 10 and R d , R e and R f are independently a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group, an aryl group, a haloalkyl group, a cyanoalkyl group, an azidoalkyl group, a hydrazinoalkyl group, a hydroxyalkyl group, an alkoxyalkyl group, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an aryl aminoalkyl group, a diarylaminoalkyl group, an arylalkyl aminoalkyl group. Alternatively R 4 and R 5 , R 5 and R 6 ; R 6 and R 7 ; or R 7 and R 8 can form together a chain of 3 or four groups selected from CH, CH 2 , O, S, N, NH, N-alkyl or N-aryl. Provided that, at least one of R 5 —R 7 is not H, a lower alkyl group, fluorine, a cyano group, a hydroxyl group, hydroxyalkyl group, an alkoxy group, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an amino group, an alkylamino group, a dialkylamino group, a carbamoyloxy group, a formyl group or —C(O)R x wherein R x is an alkyl group.
专利号:US-4353989-A 优先权日:1981-01-19 标 题:Chemical synthesis apparatus for preparation of polynucleotides 发明人:BENDER ROBERT; DUCK PETER D 权利人:ENS BIO LOGICALS INC 摘要:An apparatus for the stepwise synthesis of polynucleotides in which the polynucleotide chains are extended in stepwise fashion from a modified form of polymer support to which the first unit is linked comprises a reaction column containing the polymer supported product and acting as the reaction vessel, and a series of reaction bottles all connected to the reaction column by means of a fluid flow conduit to which the vessels make connection via two-way valves arranged in series. The farthest upstream vessel of the series contains reaction solvent, used for washing purposes and the like. The most downstream of the reaction vessels contain nucleotide reagents. Each of the valves has two separate and discreet fluid flow passageways, the first of which is used exclusively for flow of reagent from its associated vessel into the fluid flow conduit, and the second of which is used exclusively for flow of solvent or reagents from an upstream vessel therethrough, thereby eliminating the possibilities of cross-contamination as a result of reagent residuals left in the dead space of the valve. The valves are biased towards their solvent flow condition. Materials are drawn through the fluid flow conduit and valves by suction, e.g. by means of a downstream pump.
专利号:US-2017198027-A1 优先权日:2012-01-31 标 题:Process of afod and afcc and manufacturing and purification processes of proteins 发明人:HOANG KIEU 权利人:HOANG KIEU 摘要:Manufacturing and purification processes of proteins, KH 1-through KH-52, and more KH proteins are being discovered in good healthy cells—named KH CELLS. KH CELLS are good healthy cells in which the RNA synthesizes good proteins that: 1) Send signal to the damaged, sick, and bad cells that triggers that synthesis of good proteins that transform these cells to become GOOD healthy cells; 2) Send signal to the other currently undamaged cells to synthesis of good proteins to protect them from being damaged, infected and prone to DNA and other cellular alterations; and 3) Send signal to the body to produce new cells that are healthy and forbid them from being affected by intra- and extracellular damaging signals. The mechanism that governs these processes is that the KH good healthy cells provide innate good signals that make good proteins to boost the immune system.
专利号:EP-1104414-B1 优先权日:1998-08-14 标题 :Enantioselective synthesis 发明人:DRAPER RICHARD W; IYER RADHA V; LU YUELIE; VATER EUGENE J 权利人:SCHERING CORP 摘要:A short practical commercial process for the efficient enantioselective synthesis of the non-steroidal antiestrogen of formula (I) or (XIV) or a pharmaceutically acceptable salt thereof.
专利号:US-6262270-B1 优先权日:1998-08-14 标题:Enantioselective synthesis 发明人:DRAPER RICHARD W; IYER RADHA V; LU YUELIE; VATER EUGENE J 权利人:SCHERING CORP 摘要:A short practical commercial process for the efficient enantioselective synthesis of the non-steroidal antiestrogen of formula I or XIVor a pharmaceutically acceptable salt thereof.
专利号:WO-2023086801-A1 优先权日:2021-11-09 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
1: Yamashita Y, Tanaka K, Asano T, Yamakawa N, Kobayashi D, Ishihara T, Hanaya K, Shoji M, Sugai T, Wada M, Mashimo T, Fukunishi Y, Mizushima T. Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities. Bioorg Med Chem. 2014 Jul 1;22(13):3488-97. doi: 10.1016/j.bmc.2014.04.029. Epub 2014 Apr 30. doi: 10.1124/jpet.114.213009. Epub 2014 Apr 25. doi: 10.1038/srep04510. 4: Tanaka K, Ishihara T, Sugizaki T, Kobayashi D, Yamashita Y, Tahara K, Yamakawa N, Iijima K, Mogushi K, Tanaka H, Sato K, Suzuki H, Mizushima T. Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease. Nat Commun. 2013;4:2686. doi: 10.1038/ncomms3686.
合成参考文献
摘要:Drug Dosages in Laboratory Animals - A Handbook, Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973, -(148), 1973