6609-56-9 = 611-20-1 + 90921-35-0 反应条件:1.1 Reagents: Potassium Tert-Butoxide,18-Crown-6 Solvents: 1,4-Dioxane; Rt -> 80 °C; 16 H,80 °C 标题:Metal-Free Etherification Of Aryl Methyl Ether Derivatives By C-Ome Bond Cleavage 作者:Wang,Xueqiang; Li,Chenchen; Wang,Xia; Wang,Qingli; Dong,Xiu-Qin; Et Al 参考文献:Organic Letters 日期:2018 卷标:20(14) 页码:4267-4272]
403705-99-7 = 611-20-1 + 90-02-8 + 74405-18-8 + 90921-35-0 [标题:Reaction Conditions 标题:Reactions Of 1-(2-Alkoxyphenyl)Alkaniminyl Radicals 作者:Leardini,Rino; Mcnab,Hamish; Minozzi,Matteo; Nanni,Daniele; Reed,David; Et Al 参考文献:Journal Of The Chemical Society 日期:2001 卷标:(20) 页码:2704-2710
专利号:US-8138330-B2 优先权日:2006-09-11 标 题 :Process for the synthesis of oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED 权利人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED; SIGMA ALDRICH CO LLC 摘要:The present invention discloses novel methods for the synthesis of oligonucleotides with nucleoside phosphoramidites on solid supports. The methods comprise the stepwise chain assembly of oligonucleotides on supports with 5′-acyl phosphoramidites. The synthesis cycles consist of a front end deprotection step which is conducted with a solution of a primary amine or a phenolate, a phosphoramidite coupling step with a 5′-acyl nucleoside phosphoramidite in the presence of an activator, a phosphite oxidation step and an optional capping step. The novel methods improve the quality of synthetic oligonucleotides due to the irreversibility of the front end deprotection step, which prevents the formation of deletion sequences, and due to the avoidance of acidic reagents in the synthesis cycles, which prevent the formation of depurination side products. The invention further discloses novel nucleoside phosphoramidite compositions wherein the phosphoramidites carry acyl front end protective groups which are cleavable with primary amines or phenolates. The invention is applicable to the synthesis of oligodeoxyribonucleotides, oligoribonucleotides and oligonucleotides with modifications in their sugar or phosphate groups.
专利号:US-7576234-B2 优先权日:2002-05-15 标题 :Synthesis of 2-alkyl amino acids 发明人:CHORGHADE MUKUND S; GURJAR MUKUND K; MOHAPATRA DEBENDRA K 权利人:GENZYME CORP 摘要:Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
专利号:US-10927135-B2 优先权日:2017-08-03 标 题:Metal-free direct arylation of dialkyl phosphonates for the synthesis of mixed alkyl aryl phosphonates 发明人:KANG JUN YONG; HUANG HAI 权利人:THE BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIV OF NEVADA LAS VE 摘要:Provided herein are phosphates, thiophosphates, phosphonates, and phosphinates, methods of making same, and methods of using these compounds and methods for the generation of pharmaceutically relevant phosphate, phosphonate, and phosphinate analogs. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:WO-9845231-A1 优先权日:1997-04-09 标题:Supports for solid phase synthesis 发明人:SHAO HUI; CASTELHANO ARLINDO L 权利人:CADUS PHARMACEUTICAL CORP 摘要:Supports for solid-phase synthesis are disclosed. The supports include a phenol or thiophenol linker moiety. A substrate compound can be immobilized to the support through the linker moiety. The supports are suitable for combinatorial synthesis, including synthesis of combinatorial libraries.
专利号:US-2002042514-A1 优先权日:2000-06-26 标 题 :Synthesis of chlorinated pyrimidines 发明人:DOYLE TIMOTHY JOHN; WEHRENBERG PETER KARL; STANDEN MICHAEL CHARLES HENRY 摘要:A facile process for the preparation of 4,6-dichloropyrimidine is provided, which utilizes quaternary ammonium salts or quaternary phosphonium salts as catalysts for the reaction of, for example, 4,6-dihydroxypyrimidine or 4-chloro-6-methoxypyrimidine with phosgene.
专利号:WO-2025078335-A1 优先权日:2023-10-09 标 题 :Processes for the preparation of deucravacitinib 发明人:ETAYO PÉREZ PABLO; PUJOL OLLÉ XAVIER; MOLINA NIETO JUAN 权利人:FARMHISPANIA GROUP S L 摘要:The invention relates to processes for the preparation of deucravacitinib of formula (XI), or a pharmaceutically acceptable salt thereof. It also relates to intermediates of formula (V') and (V'') as defined herein useful in the synthesis of this molecule.
[参考文献]: Giulia Caron, Et Al. Calculating Virtual Log P In The Alkane/water System (Log P(N)(Alk)) And Its Derived Parameters Deltalog P(N)(Oct-Alk) And Log D(Ph)(Alk). J Med Chem. 2005 May 5;48(9):3269-79.
合成参考文献
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