2739-74-4Relevant academic research and scientific papers
Palladium-Catalyzed Coupling Reaction of N-Heteroaryl Halides with Functionalized Alkylzinc Iodides
Sakamoto, Takao,Nishimura, Sumiko,Kondo, Yoshinori,Yamanaka, Hiroshi
, p. 485 - 486 (1988)
The reaction of N-heteroaryl halides with ω-ethoxycarbonyl-, and ω-chloroalkylzinc iodides, prepared from the corresponding alkyl iodides with zinc-copper couple, in the presence of dichlorobis(triphenylphosphine)palladium in N,N-dimethylacetamide/benzene yielded C-(ω-ethoxycarbonyl)- and C-(ω-chloroalkyl)-N-heteroarenes.
Base-Controlled Completely Selective Linear or Branched Rhodium(I)-Catalyzed C?H ortho-Alkylation of Azines without Preactivation
Tran, Ga?l,Hesp, Kevin D.,Mascitti, Vincent,Ellman, Jonathan A.
supporting information, p. 5899 - 5903 (2017/05/12)
A [RhI]/bisphosphine/base catalytic system for the ortho-selective C?H alkylation of azines by acrylates and acrylamides is reported. This catalytic system features an unprecedented complete linear or branched selectivity that is solely dependent on the catalytic base that is used. Complete branched selectivity is even achieved for ethyl methacrylate, which enables the introduction of a quaternary carbon center. Excellent functional group compatibility is demonstrated for both linear and branched alkylations. The operational simplicity and broad scope of this transformation allow for rapid access to functionalized azines of direct pharmaceutical and agrochemical relevance.
SPIROCYCLIC COMPOUNDS AS AGONISTS OF THE MUSCARINIC M1 RECEPTOR AND/OR M4 RECEPTOR
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Page/Page column 53, (2016/10/24)
This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula. (I) where p, q, r, s, X, Z, Y, R1, R2, R3and R4 are as defined herein.
SMYD2 INHIBITORS
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Paragraph 0136, (2016/02/20)
The present disclosure generally relates to compounds having cellular anti-proliferative activities, and more particularly relates to compounds which inhibit the activity of human SMYD2, a SET and MYND domain-containing protein lysine methyltransferase.
MUSCARINIC RECEPTOR AGONISTS
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Page/Page column 52, (2015/12/09)
This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.
Copper(II)-Catalyzed β-Borylation of Acetylenic Esters in Water
Peck, Cheryl L.,Calderone, Joseph A.,Santos, Webster L.
, p. 2242 - 2248 (2015/08/03)
A method for the β-borylation of alkynoates has been developed. In the presence of bis(pinacolato)diboron and catalytic amounts of both copper(II) and 4-picoline, substituted alkynoates undergo borylation in a regio-, stereo-, and chemoselective fashion. The reaction is performed under mild conditions using water as solvent and open to the atmosphere to exclusively afford (Z)-β-boryl-α,β-unsaturated esters.
Direct synthesis of ester-containing indium homoenolate and its application in palladium-catalyzed cross-coupling with aryl halide
Shen, Zhi-Liang,Goh, Kelvin Kau Kiat,Wong, Colin Hong An,Yang, Yong-Sheng,Lai, Yin-Chang,Cheong, Hao-Lun,Loh, Teck-Peng
supporting information; experimental part, p. 4778 - 4780 (2011/05/15)
An efficient method for the synthesis of ester-containing indium homoenolate via a direct insertion of indium into β-halo ester in the presence of CuI/LiCl was described. The synthetic utility of the indium homoenolate was demonstrated by palladium-cataly
Intramolecular pyridine activation - dearomatization reaction highly stereoselective synthesis of polysubstituted indolizidines and quinolizidines
Barbe, Guillaume,Pelletier, Guillaume,Charette, Andre B.
supporting information; experimental part, p. 3398 - 3401 (2009/12/01)
An unprecedented intramolecular pyridine activation-asymmetric dearomatization reaction is described. This process produces 5-substituted indolizidines and 6-substituted quinolizidines in excellent yields and in a highly regio- and diastereoselective fash
Novel 1,8-naphthyridin-2(1h)-one derivatives
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, (2008/06/13)
The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein: A is an unsubstituted or optionally substituted 5 or 6 membered heteroaryl group or a fused benzene ring in which any of the above-defined heteroaryl groups is fused to a benzene ring, B is carbon or nitrogen, R1 is hydrogen, lower alkyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, R2 is hydrogen, halogen, cyano, nitro, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, and m is an integer of from 1 to 8, both inclusive; or a pharmaceutically acceptable salt thereof possesses selective PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.
SUBSTITUTED DIBENZOXAZEPINE COMPOUNDS
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, (2008/06/13)
The present invention provides dibenzoxazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
