专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-4267070-A 优先权日:1979-10-30 标题:Catalyst for the synthesis of aromatic monoisocyanates 发明人:NEFEDOV BORIS K; MANOV-JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L 权利人:NEFEDOV BORIS K; MANOV JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L 摘要:A catalyst for the synthesis of aromatic monoisocyanates comprising 1.64 to 16.6% by weight of palladium chloride, 0.16 to 47.6% by weight of an oxide of a metal of Group VB of the periodic system, 1.5 to 81.8% by weight of an oxide of a metal of Group VI B of the periodic system, 1.64 to 89.8% by weight of pyridine or an alkylsubstituted pyridine. n The use of the catalyst according to the invention in the synthesis of aromatic monoisocyanates makes it possible to obtain a high degree of conversion of the starting compound of up to 100%, a high yield of the desired product of up to 97%, and increased productivity of the catalyst of up to 40 g of the desired product per g of PdCl 2 per hour.
专利号:US-12338202-B2 优先权日:2021-09-10 标 题 :One pot synthesis of urea (meth)acrylates 发明人:BESTGEN SEBASTIAN; BEYER SILVIA 权利人:EVONIK OPERATIONS GMBH 摘要:A one-pot synthesis of polymerizable and acyclic urea (meth)acrylates, preferably mono(meth)acrylates, can be performed via in-situ synthesis of urea alcohols or amines followed by direct reaction with a (meth)acrylate reactive diluent. The urea alcohol/amine is obtained from isocyanates and alcohols, amines, or hydroxyamines. Subsequently, the reaction with the (meth)acrylate reactive diluent takes place and the urea (meth)acrylate is directly obtained either in solution with the reactive diluent, or as a pure material after removal of the reactive diluent.
专利号:US-4460501-A 优先权日:1983-08-30 标题 :Process for the synthesis of peptides utilizing thioxanthylmethyloxycarbonyl dioxides 发明人:CARPINO LOUIS A; SEGEV DAVID 权利人:RESEARCH CORP 摘要:A composition of the formula: ##STR1## wherein X is lower alkyl, and Z is an amino acid a peptide residue or a good leaving group, the composition is adaptable as a blocking or protecting group for an amine composition useful in peptide synthesis and a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.
专利号:US-2023348657-A1 优先权日:2020-07-23 标题 :Synthesis of linear polyoxazolidinones using uretdiones as diisocyanate component 发明人:QUELL AGGELIKI; THOMAS HANS-JOSEF; ELING BEREND 权利人:BASF SE 摘要:A process for preparing a thermoplastic polymer involves reacting at least components (a) to (b), in the presence of a catalyst composition (c). Component (a) is an isocyanate composition containing at least one uretdione diisocyanate (a-i), and component (b) is an epoxide composition containing at least one diepoxide (b-i). The catalyst composition (c) contains at least one ionic liquid (c-i), preferably selected from 1-ethyl-3-methyl imidazolium bromide, 1-benzyl-3-methyl imidazolium chloride. 1-butyl-1-methylpiperidinium chloride, 1-ethyl-2,3-dimethylimidazolium bromide, 1-(2-hydroxyethyl)-3-methyl imidazolium chloride, butyl-1-methylpiperidinium acetate, or mixtures of two or more thereof. A thermoplastic polymer obtained or obtainable from the process is useful for the preparation of a fibre or a molded article or as a modifier for another thermoplastic material.
专利号:US-2009156465-A1 优先权日:2005-12-30 标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors 发明人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
参考标题:1,1-Dioxonaphtho[1,2-B]Thiophene-2-Methyloxycarbonyl (α-Nsmoc) And 3,3-Dioxonaphtho[2,1-B]Thiophene-2-Methyloxycarbonyl (β-Nsmoc) Amino-Protecting Groups 作者:Louis A. Carpino,Adel Ali Abdel-Maksoud,Dumitru Ionescu,E. M. E. Mansour,Mohamed A. Zewail |发布日期:2007.3.1 摘要:Mechanistically Similar To That Previously Established For The Bsmoc Derivative In That The Reaction Is Initiated By Michael Addition To The β-Carbon Atom Of The α,β-Unsaturated Sulfone System. Application Of α- And β-Nsmoc Amino Acids To The Solid-Phase Synthesis Of Two Model Peptides Was Examined. An Advantage Of The α-Nsmoc System Over The Long-Known Bsmoc System Proved To Be The Milder Conditions Needed For
合成参考文献
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