5-(3,4-Dimethoxybenzyl)-2,2-Dimethyl-1,3-Dioxane-4,6-Dione置于盐酸,甲酸,三乙胺体系中,用 氯仿,水 用作溶剂,化学反应生成3,4-二甲氧基苯丙酸 参考文献:Process For The Preparation Of Carboxylic Acids And Derivatives Of Them 标题:Process For The Preparation Of Carboxylic Acids And Derivatives Of Them 摘要:本发明的主题是一种用于制备通式为的羧酸及其衍生物的过程 其中 R表示氢,或c₁₋₄烷基或(C₁₋₅烷氧基)甲酰基,R₁如权利要求1中定义,R₇代表氢或c₁₋₇烷基团和 R₈表示氢或羧酸基,通过将通式为的1,3-二氧杂环己烷-4,6-二酮衍生物与醛或酮反应 其中 R₉代表c₁₋₄烷基或苯基,可选地由卤素单取代 R₁₀代表氢或c₁₋₅烷基或 R₉和r₁₀共同形成一个戊烷基,在甲酸和[a]胺的存在下,如果需要,还可以在上述定义的醇的存在下,R₇-Oh Vi,其中 R₇是c₁₋₇烷基,在20至140oc的温度下,和/或 将通式的不饱和1,3-二氧杂环己烷-4,6-二酮衍生物还原 和/或 通式为的1,3-二氧杂环己烷-4,6-二酮衍生物 与甲酸在[a]胺的存在下,如果需要,还可以在上述定义的醇的存在下.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-11746364-B2 优先权日:2018-01-17 标题 :Enzymatic synthesis of kavalactones and flavokavains 发明人:PLUSKAL TOMÃ?S; Weng jing-ke 权利人:WHITEHEAD INST BIOMEDICAL RES 摘要:Disclosed are methods, compositions, proteins, nucleic acids, cells, vectors, compounds, reagents, and systems for the preparation of kavalactones, flavokavains, and kavalactone and flavokavain biosynthetic intermediates using enzymes expressed in heterologous host cells, such as microorganisms or plants, or using in vitro enzymatic reactions. This invention also provides for the expression of the enzymes by recombinant cell lines and vectors. Furthermore, the enzymes can be components of constructs such as fusion proteins. The kavalactones produced can be utilized to treat anxiety disorder, insomnia, and other psychological and neurological disorders. The flavokavains produced can be utilized to treat various cancers including colon, bladder, and breast cancers.
专利号:US-7339065-B2 优先权日:2003-07-21 标题 :Design and synthesis of optimized ligands for PPAR 发明人:AVERY MITCHELL A; PERSHADSINGH HARRIHAR A 权利人:BETHESDA PHARMACEUTICALS INC; UNIV MISSISSIPPI 摘要:This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.
专利号:US-6664282-B2 优先权日:1999-09-17 标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
专利号:US-5856107-A 优先权日:1997-02-04 标 题 :Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein 发明人:OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.
专利号:WO-9834113-A1 优先权日:1997-02-04 标题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein 发明人:OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; HOUGHTEN RICHARD A; BLONDELLE SYLVIE E; SCHONER CHRISTA C 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
[参考文献]: Pace Bs, Et Al. Short-Chain Fatty Acid Derivatives Induce Fetal Globin Expression And Erythropoiesis In Vivo. Lood. 2002 Dec 15;100(13):4640-8. [参考文献]: Betty S Pace, Et Al. Short-Chain Fatty Acid Derivatives Induce Fetal Globin Expression And Erythropoiesis In Vivo. Blood. 2002 Dec 15;100(13):4640-8.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749