专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-7329515-B2 优先权日:2003-04-21 标题 :Solid support for the synthesis of 3′-amino oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules. The methods provided are particularly mild, do not require any modifications in standard protocols for the synthesis and deprotection of oligonucleotides, provide the 3′-amino oligonucleotides free of side products and do not introduce chiral centers to the oligonucleotides.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-2025019732-A1 优先权日:2023-07-07 标 题:Method for chemical-biological cascade synthesis of l-phosphinothricin and mutants therefor 发明人:XUE YAPING; CHENG FENG; ZOU SHUPING; XU JIANMIAO; ZHENG YUGUO 权利人:UNIV ZHEJIANG TECHNOLOGY 摘要:A method for chemical-biological cascade synthesis of L-phosphinothricin is carried out as follows: 3-(methylethoxyphosphinyl) ethyl propionate is synthesized by addition reaction from diethoxymethylphosphine and acrylic acid, then a condensation reaction is carried out with 3-(methylethoxyphosphinyl) ethyl propionate and sodium ethoxide as reactants, then the product is subjected to a hydrolysis reaction with diethyl oxalate to synthesize 4-(hydroxymethylphosphinyl)-2-oxobutyric acid, and finally, L-phosphinothricin is catalytically synthesized by taking 4-(hydroxymethylphosphinyl)-2-oxobutyric acid as a raw material, and using highly active and stable wet cells co-expressing phsophinothricin dehydrogenase and alcohol dehydrogenase or co-expressing a phsophinothricin dehydrogenase mutant and alcohol dehydrogenase as a biocatalyst, thereby solving the problems of existing L-phosphinothricin synthesis being tedious, low asymmetric amination reduction activity and poor stability.
专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-10913749-B2 优先权日:2015-05-07 标 题 :Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
参考标题:Zno/Fe3O4Nanoparticles Promoted Green Synthesis Of Pyrazolo Pyrimidinones: Study Of Antioxidant Activity 作者:Mona Ghoorchibeigi,Kambiz Larijani,Parviz A. Azar,Karim Zare,Iraj Mehregan |发布日期:2020.10 摘要:The Preparation Of Pyrazolo Pyrimidinone Derivatives Was Performed By Using Five Component Reactions Of Phthalaldehyde, Cyanomethylamine, Electron Deficient Acetylenic Compounds, Isocyanate, Hydrazine, And Catalytic Amounts Of Zno/fe3O4‐magnetic Nanoparticles As A High Performance Catalyst Under Ultrasonic Conditions At Ambient Temperature In Aquause Media At Room Temperature. It Should Be Mentioned
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