95176-68-4Relevant academic research and scientific papers
Synthesis method of allyl aryl compound
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Paragraph 0024-0025, (2021/06/02)
The invention belongs to the technical field of synthesis of organic compounds, and relates to a synthesis method of an allyl aryl compound. Under the action of a nickel catalyst and a ligand, a cross-coupling reaction of an allyl alkyl ether compound and an arylboronic acid reagent is carried out, activation of carbon-oxygen bonds is realized, and the allyl aryl compound is obtained. The method has the advantages of low cost, simple process, high product purity and yield, wide substrate application range and the like. The synthesis method can be used for modifying drug molecules, and the synthesized product can be used as a novel medical intermediate.
Nickel-Catalyzed Arylation of C(sp3)-O Bonds in Allylic Alkyl Ethers with Organoboron Compounds
Li, Xiaowei,Li, Yuxiu,Zhang, Zhong,Shi, Xiaolin,Liu, Ruihua,Wang, Zemin,Li, Xiangqian,Shi, Dayong
supporting information, p. 6612 - 6616 (2021/09/02)
A nickel-catalyzed cross-coupling of allylic alkyl ethers with organoboron compounds through the cleavage of the inert C(sp3)-O(alkyl) bonds is described. Several types of allylic alkyl ethers can be coupled with various boronic acids or their derivatives to give the corresponding products in good to excellent yields with wide functional group tolerance and excellent regioselectivity. The gram-scale reaction and late-stage modification of biologically active compounds further prove the practicality of this synthetic method.
High-yielding sequential one-pot synthesis of chiral and achiral α-substituted acrylates via a metal-free reductive coupling reaction
Ramachary, Dhevalapally B.,Venkaiah, Chintalapudi,Reddy, Y. Vijayendar
supporting information, p. 5400 - 5406 (2014/07/21)
A general process for the high-yielding synthesis of substituted chiral and achiral α-substituted acrylates was achieved through the sequential one-pot combination of a metal-free reductive coupling reaction followed by an Eschenmoser methylenation. The proline catalyzed reaction of Meldrum's acid, aldehydes and Hantzsch ester followed by methylenation was successful with Eschenmoser's salt in the presence of an alcohol solvent. Herein, we have shown the high-yielding synthesis of privileged building blocks from chiral/achiral α-substituted acrylates and shown them to be very good intermediates in the pharmaceuticals and natural products synthesis. This journal is the Partner Organisations 2014.
Pd-catalyzed threefold arylation of Baylis-Hillman bromides and acetates with triarylbismuth reagents
Rao, Maddali L. N.,Giri, Somnath
, p. 4580 - 4589 (2012/11/07)
Functionalized alkyl 2-benzylacrylates and 2-benzylacrylonitriles were synthesized by means of atom-economic cross-couplings of Baylis-Hillman bromides or acetates with BiAr3 under palladium-catalyzed conditions. These reactions, involving thre
Design and pharmacological activity of phosphinic acid based NAALADase inhibitors
Jackson,Tays,Maclin,Ko,Li,Vitharana,Tsukamoto,Stoermer,Lu,Wozniak,Slusher
, p. 4170 - 4175 (2007/10/03)
A novel series of phosphinic acid based inhibitors of the neuropeptidase NAALADase are described in this work. This series of compounds is the most potent series of inhibitors of the enzyme described to date. In addition, we have shown that these compounds are protective in animal models of neurodegeneration. Compound 34 significantly prevented neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In addition, in the chronic constrictive model of neuropathic pain, compound 34 significantly attenuated the hypersensitivity observed with saline-treated animals. These data suggest that NAALADase inhibition may provide a new approach for the treatment of both neurodegenerative disorders and peripheral neuropathies.
ALKYLAMINOALKYL-TERMINATED SULFIDE/SULFONYL-CONTAINING PROPARGYL AMINO-DIOL COMPOUNDS FOR TREATMENT OF HYPERTENSION
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, (2008/06/13)
Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: STR1 wherein q is two or three; wherein r is zero or two; wherein R 2 is selected from hydrido, methyl, ethyl and phenyl; wherein R 3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R. sup.5 is propargyl or a propargyl containing moiety; wherein R. sup.7 is cyclohexylmethyl; wherein R 8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R. sup.12 and R 13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
