CAS: 623-47-2; Ethyl Propiolate

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4341-76-8 627-09-8 41658-03-1

上下游产品

CAS号64-17-5 乙醇 | CAS号471-25-0 丙炔酸 | CAS号764-01-2 2-丁炔-1-醇 | CAS号1972-28-7 偶氮二甲酸二乙酯 | CAS号108-95-2 苯酚 | CAS号107-19-7 丙炔醇 | CAS号287108-60-5 5-bromo-2-[(4-h... | CAS号541-41-3 氯甲酸乙酯 | CAS号74-86-2 乙炔 | CAS号527-60-6 2,4,6-三甲酚 | CAS号1112-29-4 Tetraethyl(etho... | CAS号995-37-9 ethyl (E)-3-die... | CAS号106202-26-0 ethyl 3-(3-nitr... | CAS号104923-75-3 ethyl 4-hydroxy... | CAS号1101120-33-5 5-[(叔丁氧羰基)氨基]吡唑... | CAS号106551-83-1 7-phenyl-1,6,7,... | CAS号105174-97-8 3-溴异恶唑-5-甲酸乙酯 | CAS号111303-36-7 3-溴-4-异噁唑羧酸乙酯 | CAS号35441-10-2 1,2-二氢-6-羟基-2-氧... | CAS号50820-64-9 吲哚-6-甲酸乙酯

乙醛酸乙酯置于c7H13N2O4P,Potassium Carbonate体系中,用 甲醇 作为反应溶剂,化学反应生成 丙炔酸乙酯
参考文献:烯丙基化和异戊二烯化铬酮的串联克莱森重排/6-内环化方法
标题:烯丙基化和异戊二烯化铬酮的串联克莱森重排/6-内环化方法
摘要:源自邻酰基苯酚的烯丙基,二甲基烯丙基和异戊二烯醚在微波辐射下反应形成 C-烯丙基化或异戊二烯化色酮衍生物,具体取决于芳烃和烯丙基取代基的取代模式.该反应通过串联克莱森重排和 6-Endo-Trig 或 6-Endo-Dig 环化序列进行.对于异戊二烯醚,串联序列可以通过 Cope 重排扩展以提供 6-异戊二烯色酮.该方法可用于合成天然产物和药物.
DOI:10.1002/ejoc.201501151

专利信息

专利号:US-8153839-B2
优先权日:2005-09-14
标题:Method for synthesis of keto acids or amino acids by hydration of acetylene compound
发明人：OGO SEIJI; FUKUZUMI SHUN-ICHI
权利人:OGO SEIJI; FUKUZUMI SHUN-ICHI; JAPAN SCIENCE & TECH AGENCY
摘要:An object of the present invention is to provide a method for synthesis of keto acids by hydration of an acetylene compound (acetylene-carboxylic acids) under mild conditions free from harmful mercury catalysts and a method for synthesis of amino acids from acetylene-carboxylic acids in a single container (one-pot or tandem synthesis). In one embodiment of the method according to the present invention for synthesis of keto acids, acetylene-carboxylic acids is hydrated in the presence of a metal salt represented by General Formula (1), n nwhere M 1 represents an element in Group VIII, IX, or X of the periodic table, and X 1 , X 2 , or X 3 ligand represents halogen, H 2 O, or a solvent molecule, and k represents a valence of a cation species, and Y represents an anion species, and L represents a valence of the anion species, and each of K and L independently represents 1 or 2, and k×m=L×n.

专利号:WO-2015198349-A1
优先权日:2014-06-25
标 题 :A one pot synthesis of 3-substituted quinoline carboxylates and its derivatives
发明人：GADAKH SUNITA KHANDERAO; SUDALAI ARUMUGAM
权利人:COUNCIL SCIENT IND RES
摘要:The present invention provides a one pot, simple, cost effective and industrially feasible catalytic synthesis of quinolines or substituted quinolines from anilines with yield >80% yield. The present invention also discloses a process for the synthesis of oxolinic acid using quinolines with yield > 45%.

专利号:US-2015045564-A1
优先权日:2012-01-03
标 题 :Cu-MEDIATED ANNULATION FOR THE EFFECTIVE SYNTHESIS OF 3-SUBSTITUTED PHTHALIDES
发明人：REDDY SANTHOSH REKULA; PRAGATI KISHORE PRASAD; NAGA KIRAN; SUDALAI ARUMUGAM
权利人:COUNCIL SCIENT IND RES
摘要:The present invention disclosed herein is a novel commercially feasible, one pot synthesis of library of 3-substituted phthalides of formula I via CuCN mediated oxidative cyclization in high yield. Formula I

专利号:US-9969686-B2
优先权日:2014-08-05
标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.

专利号:US-7288671-B2
优先权日:1999-05-14
标题:Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
发明人：PALLADINO MICHAEL; THEODORAKIS EMMANUEL A
权利人:UNIV CALIFORNIA
摘要:Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus are useful in the treatment of various diseases. n nwherein the R groups are defined as follows: if any R 3 -R 5 , R 7 , R 8 , R 11 -R 13 is not hydrogen, R 2 or R 6 or R 9 is not methyl, or R 10 is not CH 2 , then R 1 is selected from the group consisting of hydrogen, a halogen, COOH, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 1 -C 12 esters, C 1 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, (C 1 -C 12 )(C 1 -C 12 ) cyclic amides, (C 1 -C 12 ) amines, C 1 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers, C 1 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 5 -C 12 aryls. If all R 3 -R 5 , R 7 , R 8 , R 11 -R 13 are hydrogen, R 2 , R 6 , and R 9 are each methyl, and R 10 is CH 2 , then R 1 is selected from hydrogen, a halogen, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 2 -C 12 esters, C 2 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, C 2 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers other than methyl-acetyl ether, C 2 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 2 -C 12 aryls. R 2 and R 9 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, C 1 -C 12 acyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. R 3 -R 5 , R 7 , R 8 , and R 11 -R 13 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, and C 5 -C 12 aryl. R 6 is selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, and C 2 -C 12 alkynyl. R 10 is selected from hydrogen, a halogen, CH 2 , C 1 -C 6 alkyl, C 1 -C 6 substituted alkyl, C 2 -C 6 alkenyl, C 2 -C 6 substituted alkenyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.

专利号:US-7829669-B2
优先权日:1999-06-28
标 题:Catalytically active recombinant memapsin and methods of use thereof
发明人：KOELSCH GERALD; TANG JORDAN J N; HONG LIN; GHOSH ARUN K; LIN XINLI
权利人:OKLAHOMA MED RES FOUND; UNIV ILLINOIS
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bond to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.