专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:WO-2024105686-A1 优先权日:2022-11-14 标 题 :A process for the synthesis of stilbene and intermediates thereof 发明人:KANUMURU RAHUL RAJU; KOCHUMALAYIL SHAJI GEORGE; SURANENI RAVIKUMAR; VANA MURALI MOHANARAO 权利人:FERTIS INDIA PVT LTD 摘要:The present invention discloses a process for the preparation of Stilbene such as Pterostilbene and Resveratrol. More particularly, the present invention discloses synthesis of Stilbene employing a novel intermediate, 5-(4-(1-ethoxyethoxy) styryl)-benzene 1,3 diol and 1-(4-(1-ethoxyethoxy) styryl)-3,5-dimethoxy- benzene.
专利号:US-2022356139-A1 优先权日:2019-09-03 标 题:Synthesis of deuterated aldehydes 发明人:WANG WEI 权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA 摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.
参考标题:Diastereoselective Pictet−spengler Approach For The Synthesis Of Pyrrolo[3,2-E][1,4]Diazepin-2-One Peptide Turn Mimics 作者:Philippe Deaudelin,William D. Lubell |发布日期:2008.7.3 摘要:Diffraction Demonstrated That The Alpha-Amino Acid Residue Adopted Dihedral Angle Geometry Similar To An Ideal Gamma-Turn, Illustrating The Potential For Employing These Novel Heterocycles As Peptide Turn Mimics.
合成参考文献
参考文献:10.1107/s160053681101614x 摘要:Fun HK, Loh WS, Sarojini BK, Khaleel VM, Narayana B. (2E)-3-[3-(Benz-yloxy)phen-yl]-1-(2-hy-droxy-phen-yl)prop-2-en-1-one. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1313–4. 参考文献:10.1107/s1600536811016977 摘要:Fun HK, Arshad S, Sarojini BK, Khaleel VM, Narayana B. (2E)-3-(3-Benzyl-oxyphen-yl)-1-(2-hydroxy-5-methyl-phen-yl)prop-2-en-1-one. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1372–3.