专利号:US-8163903-B2 优先权日:2009-01-13 标 题 :Process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-acetamide 发明人:SALLARES ROSELL JUAN; MARQUILLAS FRANCISCO 权利人:SALLARES ROSELL JUAN; MARQUILLAS FRANCISCO; INTERQUIM SA 摘要:The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABA A receptor. In this process, N-(5-acetyl-2-fluorophenyl)-N-methyl-acetamide (VI) is reacted with an excess of N,N-dimethylformamide dimethyl acetal (NNDMF-DMA). The present invention also provides a new process for the preparation of a compound with affinity for GABA A receptor, N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methyl-acetamide (II), which comprises the following steps: a) methylation of N-(5-acetyl-2-fluorophenyl)-N-acetamide (IV) with a methyl sulfonate, b) reaction of the resulting compound (VI) with NNDMF-DMA, and c) reaction of the resulting compound (I) with (5-amino-1H-pirazol-4-yl)thiophen-2-yl-methanone (III) in glacial acetic acid. The present invention also relates to new intermediate (VI).
专利号:US-2024059678-A1 优先权日:2021-01-18 标 题 :Synthesis Method for Aminopyrimidine FAK Inhibitor Compound 发明人:DU WU; LV HAIBIN; LI YU; KUANG TONGTAO; GENG XI 权利人:HINOVA PHARMACEUTICALS INC 摘要:A synthesis method for an aminopyrimidine FAK inhibitor compound, relating to the field of pharmaceutical synthesis. In the synthesis method, R1 is hydrogen or a carboxylic acid protecting group, R2 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl, R3 and R4 are each independently selected from hydrogen or deuterium, and R5 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl. The synthesis method is simple to operate, and has low costs. The product prepared can obtain a high total yield (≥66%) and a high purity (≥99%), and the product yield and purity are superior to those in the prior art (in the prior art, the total yield is about 11%, and the purity is 99%). The synthesis method achieves excellent effects, can also successfully prepare a final product on kilogram scale, and is suitable for industrial production, having a good application prospect.
专利号:US-2006275768-A1 优先权日:2002-12-30 标 题 :Multiplex polymer ligation 发明人:KOCHENDOERFER GERD G; SHAO HAIYAN; CRESSMAN SONYA 权利人:KOCHENDOERFER GERD G; SHAO HAIYAN; CRESSMAN SONYA 摘要:The invention concerns a multiplex polymer ligation method involving water-soluble polymeric protecting groups, compositions and methods of use. The method involves synthesis of a first compound bearing one or more water-soluble polymeric protecting groups followed by replacing one or more of the water-soluble protecting groups with a chemical adduct of interest. Multiple different compounds derived from the first compound can be readily prepared by splitting the first compound into first and second reaction systems, followed by replacing one or more of the water-soluble polymeric protecting groups of the first reaction system with a first chemical adduct, and replacing one or more of the water-soluble polymeric protecting groups of the second reaction system with a second chemical adduct of interest, where the first and second chemical adducts are different. Also provided are kits useful for carrying out the multiplex polymer ligation methods of the invention.
专利号:US-5859191-A 优先权日:1996-12-05 标 题:Method for the site-specific modification of peptide alpha amines 发明人:MILLER STEPHEN; SCANLAN THOMAS S 权利人:UNIV CALIFORNIA 摘要:A peptide comprising a free terminal alpha amine is treated with an aryl sulfonamide activating agent, resulting in an activated amide. The resulting activated amide is deprotonated with a base and modified by the addition of a substituent group. The aryl sulfonamide activating group is cleaved using a nucleophilic substitution reaction. The method is particularly useful for the modification of peptides at specific N-alpha positions, and is compatible with conventional solid phase peptide synthesis, including those that utilize Fmoc protecting groups.
专利号:US-9695116-B2 优先权日:2011-12-30 标题:Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives 发明人:BHAT LAXMINARAYAN; ADIEY KOUACOU; BHAT SEEMA RANI 权利人:REVIVA PHARMACEUTICALS INC 摘要:The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
专利号:US-7030218-B2 优先权日:2000-09-08 标 题 :Pseudo native chemical ligation 发明人:HUNTER CHRISTIE L; BOTTI PAOLO; BRADBURNE JAMES A; CHEN SHIAH-YUN; CRESSMAN SONYA; KENT STEPHEN B H; KOCHENDOERFER GERD G; LOW DONALD W 权利人:GRYPHON THERAPEUTICS 摘要:The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1 ). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
参考标题:Evolution Of The Total Syntheses Of Ustiloxin Natural Products And Their Analogues 作者:Pixu Li,Cory D. Evans,Yongzhong Wu,Bin Cao,Ernest Hamel,Madeleine M. Joullié |发布日期:2008.2.1 摘要:Synthetically Challenging Chiral Tertiary Alkyl-Aryl Ether Linkage. The First Total Synthesis Of Ustiloxin D Was Achieved In 31 Linear Steps Using An S(N)Ar Reaction. An Noe Study Of This Synthetic Product Showed That Ustiloxin D Existed As A Single Atropisomer. Subsequently, Highly Concise And Convergent Syntheses Of Ustiloxins D And F Were Developed By Utilizing A Newly Discovered Ethynyl Aziridine Ring-Opening
合成参考文献
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