CAS: 104451-70-9; 2,3,6-Trifluorobenzaldehyde

相似化合物

136514-17-5 2358-29-4 773134-90-0

N,N,N'-Trimethyl-(2,3,6-Trifluorophenyl)-N'-Trimethylsilanylmethanediamine置于盐酸,水体系中,用80 %的收率获得2,3,6-三氟苯甲醛
参考文献:苯二氨基甲基化中的潜在卡宾:机理和实际应用
标题:苯二氨基甲基化中的潜在卡宾:机理和实际应用
摘要:由于甲硅烷基团容易迁移,甲硅烷基甲脒1与其碳烯形式1'处于平衡状态.1与各种取代的氟苯的反应随着亲核卡宾1'的插入而进行在混合试剂后进入最酸性的 C-H 键,不需要任何催化剂.根据 Dft 计算,通过三元过渡态结构进行的插入反应的经典解释需要高活化能.相反,预计将芳香底物中酸性最强的质子转移到卡宾碳上的活化势垒较低.下一步,形成的离子对向产物的无障碍重排完成了该过程.取代苯在与甲硅烷基甲脒反应中的反应性可以通过计算的c-H 氢的p K A (Dmso) 值粗略评估.具有 P K A的苯衍生物约 少于 31 个可以进行 C-H 插入.该反应提供缩醛胺作为第一批产物,它可以很容易地通过酸水解转化为相应的醛.由于甲硅烷基甲脒1对许多官能团具有耐受性,该反应可应用于多种苯衍生物,使其成为有机合成应用的可靠策略.
Doi:10.1021/acs.Joc.3C00470

专利信息

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-2022267331-A1
优先权日:2019-06-05
标题 :Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO; BELIAEV ALEXANDER; ROSSI TINO; PALMA NUNO; SOARES DA SILVA PATRÃ?CIO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & CA SA
摘要:This invention relates to: (a) compounds of formula I (with R1 to R5 and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:US-6822092-B2
优先权日:2000-06-12
标 题:Expanded porphyrins and a method for synthesis thereof
发明人：OSUKA ATSUHIRO
权利人:JAPAN SCIENCE & TECH AGENCY
摘要:Novel meso-aryl substituted expanded porphyrins comprising of alternate arrangement of more than six of pyrrole units bridged by a methine group whose hydrogen is substituted with Ar-group; and their synthetic method. Ar-group is either a 2,6-substituted phenyl group which can possess a substituent at the other 3, 4, and 5 positions, or 9-anthryl group which can possess a substituent at the other positions of the anthracence, or a cyclohexyl group which can possess a substituent at the other positions of the cyclohexyl group. The substituents at the 2 and 6 positions mentioned above can be selected independently from halogen atom or lower alkyl group of carbon number 1 to 4, substituents at 3-5 positions, 9-anthryl group and cyclohexyl group can be selected independently from the group consisting of substituted or non-substituted alkyl of carbon number 5 or 6, substituted or non-substituted aryl group, besides above mentioned substituents at 2 and 6 positions. Each Ar-group can be different.

专利号:US-11034695-B2
优先权日:2016-09-23
标 题:Dopamine-β-hydroxylase inhibitors
发明人：SOARES DA SILVA PATRÃ?CIO; ROSSI TINO; KISS LASZLO ERNO; BELIAEV ALEXANDER; LEAL PALMA PEDRO NUNO
权利人:BIAL—PORTELA & CA S A; BIAL—PORTELA & Cᵃ S A
摘要:This invention relates to: (a) compounds of Formula Ia (with R1, R4, R5, R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:US-5574146-A
优先权日:1994-08-30
标题:Oligonucleotide synthesis with substituted aryl carboxylic acids as activators
发明人：REDDY M PARAMESWARA; FAROOQUI FIRDOUS
权利人:BECKMAN INSTRUMENTS INC
摘要:A process for synthesizing oligonucleotides by phosphoramidite chemistry wherein the improvement is the use of substituted aryl carboxylic acids as the activators. These activators produce in situ nucleotide intermediates in which the substituted arylcarbonyl group has displaced the amidite moiety.

专利号:US-6245773-B1
优先权日:1996-05-16
标题:5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
发明人：WONG WAI C; LAGU BHARAT; NAGARATHNAM DHANAPALAN; MARZABADI MOHAMMAD R; GLUCHOWSKI CHARLES
权利人:SYNAPTIC PHARMA CORP
摘要:This invention is directed to dihydropyrimidine compounds of the following formula: n which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.