专利号:US-3703530-A 优先权日:1970-08-24 标 题 :Alkyl - 2 - alkyl - 2,3 - dicarboxy-5-norbornene - 7-acetate intermediates for the total synthesis of elenolic acids and analogs thereof 发明人:KELLY ROBERT C 权利人:UPJOHN CO 摘要:A TOTAL SYNTHESIS OF ELENOLIC ACID, FORMULA XIV (R AND R2 ARE HYDROGEN, R1 AND R3 ARE METHYL) AND THE ANALOGS THEREOF, OF FORMULA XIV: 3-(R3-O-),4-(R-OOC-CH(-R2)-),5-(HCO-),6-R1-5,6-DIHYDRO- 4H-PYRAN WHEREIN R AND R3 ARE ALKYL OF 1 TO 8 CARBON ATOMS, INCLUSIVE, WHEREIN R1 IS ALKYL OF 1 TO 4 CARBON ATOMS, INCLUSIVE, AND WHEREIN R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL OF 1 TO 4 CARBON ATOMS, INCLUSIVE, IS CARRIED OUT BY A MULTI-STEP PROCESS STARTING FROM CYCLOPENTADIENE. COMPOUNDS OF FORMULA XIV HAVE VIRUCIDAL AND HYPOTENSIVE ACTIVITY AND CAN BE USED AS HYPOTENSIVE AGENTS IN MAMMALS (U.S. PAT. 3,033,877) OR AS VIRUCIDAL AGENTS TO DECONTAMINATE SURGICAL INSTRUMENTS, HOSPITAL WALLS, SWIMMING POOLS, OR CAN BE USED FOR NASAL WASHES IN MAMMALS.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:WO-2022269335-A1 优先权日:2021-06-23 标题 :A process for preparation of alicyclic acid dianhydride 发明人:RAO CHIKKAM SRINIVASA; VARMA SATISH RAMSHANKAR 权利人:VIVAN LIFE SCIENCES PVT LTD 摘要:The present invention depicts a method for synthesis of alicyclic acid dianhydride in simpler and economic manner. The process has advantages of an economical production method without using a catalyst, safe operation, high yield and most importantly purification under mild reaction conditions and high purity of product and the method is suitable in large scale industry.
专利号:US-3962217-A 优先权日:1969-10-24 标 题 :Process for the manufacture of Δ16 -steroid-14β,18,20-triols and -14β,20-diol-18-ols of the pregnane series 发明人:WEHRLI HANSULI; JEGER OSKAR 权利人:CIBA GEIGY CORP 摘要:The invention is for a selective reduction of the 20- oxo group in Δ 16 -steroid-14β,18-diol-20-ones of the pregnane series to form the two epimeric 20-alcohols having the 20 S and 20 R configuration. The process is especially intended for the manufacture of alkaloids of the batrachotoxin type, particularly for batrachotoxinine A, which is a pregnane derivative having a 20 S alcohol grouping, and epimers and derivatives, such as epi-batrachotixinine A or 7,8-dihydrobatrachotoxinine A. The process is characterized by reducing the said Δ 16 -steroid-14β,18-diol-20-ones in form of their 14,18-ketals, for instance the 14,18 acetonides and using appropriate complex light metal hydrides and operating at appropriate temperatures. The separation of the two isomers is easy and can be effected by the usual physical operations, such as crystallization or chromatography. In the 14β,18,20-triols obtained the 18-hydroxy group can be dehydrogenated to the corresponding 18-aldehydes, which are intermediates necessary in the synthesis of the said pharmacological interesting substances, such as batrachotoxin, by treatment with a sulphoxide in the presence of a carboxylic acid anhydride.
专利号:US-3793346-A 优先权日:1970-08-24 标 题:Intermediate in the total synthesis of elenolic acid 发明人:KELLY R 权利人:UPJOHN CO 摘要:A COMPOUND OF THE FORMULA 2-R4,2-R5,4-(R1-CH(-OH),5-(R-OOC-CH(-R2),6-(R3-OOC-)- 4,5,6,6A-TETRAHYDRO-3AH-CYCLOPENTA-1,3-DIOXOLE WHEREIN R AND R3 ARE ALKYL OF 1 TO 3 CABON ATOMS, INCLUSIVE, R1 IS ALKYL OF 1 TO 4 CARBON ATOMS R2 IS HYDROGEN OR ALKYL OF 1 TO 4 CARBON ATOMS, AND R4 AND R5 ARE HYDROGEN, ALKYL OF 1 TO 4 CARBON AOMS, INCLUSIVE, OR PHENYL, WITH THE PROVISO THAT ONLY ONE OF R4 AND R5 IS PHENYL, IS PRODUCED IN A MULTISTEP REACTION. THE COMPOUND IS AN INTERMEDIATE FOR ELENOLIC ACID.
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
[参考文献]: Christian Hallmann, Et Al. Relative Efficiency Of Free Fatty Acid Butyl Esterification Choice Of Catalyst And Derivatisation Procedure. J Chromatogr A. 2008 Jul 11:1198-1199:14-20.
合成参考文献
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