131330-80-8Relevant academic research and scientific papers
Method for synthesizing alpha-acrylic acid compound by catalyzing carbon dioxide and alkyne with palladium
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Paragraph 0090-0098, (2020/05/02)
The invention belongs to the technical field of organic synthesis, and discloses a method for synthesizing an alpha-acrylic acid compound by catalyzing carbon dioxide and alkyne with palladium. The preparation method comprises the following steps: adding an alkyne compound, a palladium salt catalyst, alkali, a diphosphine ligand, a silane reducing agent and a solvent into a high-pressure reactionkettle, introducing carbon dioxide, stirring and reacting at 60-120 DEG C, washing a reaction liquid with water for extraction, and separating for purification to obtain the alpha-acrylic acid compound. By using the palladium salt as the catalyst and the diphosphine ligand as the ligand, the method has the characteristics of high yield, single selectivity, wide substrate applicability and the like. In addition, by taking the alkyne compound and carbon dioxide as raw materials in the reaction, the method has the advantages as follows: the raw materials are simple and easily available, the operation is simple and convenient and the atom economy is high.
Palladium-Catalyzed Highly Regioselective Hydrocarboxylation of Alkynes with Carbon Dioxide
Chen, Pengquan,Cheng, Ruixiang,Jiang, Huanfeng,Lei, Ming,Lou, Hongming,Qi, Chaorong,Shi, Fuxing,Wang, Lu,Wu, Wanqing,Xiong, Wenfang,Zhu, Baiyao
, p. 7968 - 7978 (2020/08/21)
A Pd-catalyzed highly regioselective hydrocarboxylation of alkynes with carbon dioxide has been established. By the combination of Pd(PPh3)4 and 2,2′-bis(diphenylphosphino)-1,1′-binaphthalene (binap), a variety of functionalized alkynes, including aryl alkynes, aliphatic alkynes, propargylamines, and propargyl ethers, could be leveraged to provide a wide array of α-acrylic acids in high yields with high regioselectivity under mild reaction conditions. Experimental and DFT mechanistic studies revealed that this reaction proceeded via the cyclopalladation process of alkynes and carbon dioxide in the presence of binap to generate a five-membered palladalactone intermediate and enabled the formation of Markovnikov adducts. Moreover, this strategy provided an effective method for the late-stage functionalization of alkyne-containing complicated molecules, including natural products and pharmaceuticals.
Matrix metalloprotease inhibitors
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, (2008/06/13)
Compounds of formula (I): STR1 as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption disease, such as osteoporosis.
New orally active enkephalinase inhibitors: Their synthesis, biological activity, and analgesic properties
Senokuchi, Kazuhiko,Nakai, Hisao,Nagao, Yuuki,Sakai, Yasuhiro,Katsube, Nobuo,Kawamura, Masanori
, p. 441 - 463 (2007/10/03)
A series of (4s)-4-[(2S)-benzyl-3-mercaptopropionylamino]-4-(N- phenylcarbamoyl)-butyric acids has been identified as potent systemically active enkephalinase inhibitors. Structure-activity relationships (SAR) are discussed. Further chemical modification of the inhibitors was carried out in order to identify the inhibitors which are orally active in an animal model. Compounds of particular interest are the prodrug-like analogues, including 5b (ONO-9902). Their analgesic effects after oral administration were evaluated.
MATRIX METALLOPROTEASE INHIBITORS
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, (2008/06/13)
Compounds of formula (I): STR1 as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.
A New Indirect Application of Aggregative Activation: Synthesis of Esters by Cobalt-Catalyzed Carbonylation of Aryl, Heterocyclic, and Vinyl Halides under Atmospheric Pressure
Marchal, Joel,Bodiguel, Jacques,Fort, Yves,Caubere, Paul
, p. 8336 - 8340 (2007/10/02)
Sun lamp illuminated alkoxycarbonylation of aryl, heteroaryl, and vinyl halides was performed under atmospheric pressure of CO in the presence of a cobalt catalyst in situ generated from Co(OAc)2.Illunination through a Pyrex flask was sufficient to catalyze the reaction.This process avoids the use of Co2(CO)8 and excess CH3I, which were required in the earlier procedure.A SRN1 mechanism is proposed.
