CAS: 290297-26-6; 2-(3,5-Bis(Trifluoromethyl)Phenyl)-N,2-Dimethyl-N-(6-(4-Methylpiperazin-1-yl)-4-(O-Tolyl)Pyridin-3-yl)Propanamide

上下游产品

CAS号290297-25-5 N-甲基-4-(2-甲基苯基)... | CAS号289686-69-7 α,α-dimethyl-3,... | CAS号342417-01-0 6-(4-甲基哌嗪-1-基)-... | CAS号342417-02-1 [6-(4-甲基-哌嗪-1-基... | CAS号109-01-3 N-甲基哌嗪 | CAS号4548-45-2 2-氯-5-硝基吡啶 | CAS号55403-34-4 5-硝基-2-(4-甲基-1-... | CAS号342417-00-9 6-chloro-4-o-to... | CAS号342416-99-3 6-氯-4-邻甲苯基烟酸 | CAS号342417-04-3 N-叔丁基-6-氯-4-邻甲苯基烟酰胺

奈妥吡坦中间体2置于n,N-二异丙基乙胺,红铝体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 4.0H,反应生成奈妥吡坦
参考文献:新型nk 1受体拮抗剂的高效合成:格氏试剂到6-氯烟酸衍生物的选择性1,4-加成.
标题:新型nk 1受体拮抗剂的高效合成:格氏试剂到6-氯烟酸衍生物的选择性1,4-加成.
摘要:描述了从6-氯烟酸开始的两类新型nk 1受体拮抗剂的新有效合成方法,其中包括befetupitant和netupitant.O的介绍吡啶环c(4)上的甲苯基取代基是通过对6-氯烟酸或其衍生物的一锅选择性1,4-格里雅加成/氧化序列实现的.检查了该添加/氧化顺序的范围.还表明,可以通过霍夫曼重排然后还原将羧基官能团转化为甲基氨基.此外,建立了一种新的高产率合成2-(3,5-双三氟甲基苯基)-2-甲基丙酸的方法,该方法是通过将3,5-双(三氟甲基)溴苯加到丙酮中而获得的叔醇羰基化而合成的. .
Doi:10.1021/jo0523666

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.

专利号:US-12084407-B2
优先权日:2019-11-26
标 题 :Cannabigerol derivatives and use thereof as cannabinoid receptor modulators
发明人：AHMAR SIAWASH; GNANASEKARAN KRISHNA KUMAR; OMEARA JEFFREY ALAN
权利人:CANOPY GROWTH CORP
摘要:The synthesis of a range of pentylbezene-1,3-diol compounds of formula I is disclosed. These compounds bind to cannabinoid 1 and 2 receptors (CB1 and CB2), and are thus presumed to be useful in modulating the activity of such receptors. Accordingly, the use of such synthetic cannabinoids in the treatment of various disorders mediated by CB1 and CB2 is contemplated.