70090-69-6Relevant academic research and scientific papers
Ruthenium-Catalyzed Propargylic Reduction of Propargylic Alcohols with Hantzsch Ester
Ding, Haowei,Sakata, Ken,Kuriyama, Shogo,Nishibayashi, Yoshiaki
supporting information, p. 2130 - 2134 (2020/06/08)
Ruthenium-catalyzed propargylic reduction of propargylic alcohols bearing a terminal alkyne moiety is accomplished by using Hantzsch ester as a nucleophilic hydride source. A variety of secondary and tertiary propargylic alcohols are reduced to the corresponding propargylic reduced products such as 1-alkynes in excellent yields. Some mechanistic studies indicate that ruthenium-allenylidene complexes may work as key reactive intermediates.
Synthesis of γ-Boryl-Substituted Homoallylic Alcohols with anti Stereochemistry Based on a Double-Bond Transposition
Miura, Tomoya,Nakahashi, Junki,Sasatsu, Takanori,Murakami, Masahiro
, p. 1138 - 1142 (2019/01/04)
The stereoselective synthesis of anti isomers of γ-boryl-substituted homoallylic alcohols is disclosed. (E)-1,2-Di(boryl)alk-1-enes undergo Ru-catalyzed double-bond transposition with control of the geometry. The in situ generated (E)-1,2-di(boryl)alk-2-enes add to aldehydes in a stereospecific manner. The alkenylboron group within the product is amenable to a variety of synthetic derivatizations.
Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: A case of clofilium analogues
Louvel, Julien,Carvalho, Jo?o F.S.,Yu, Zhiyi,Soethoudt, Marjolein,Lenselink, Eelke B.,Klaasse, Elisabeth,Brussee, Johannes,Ijzerman, Adriaan P.
, p. 9427 - 9440 (2014/01/06)
Cardiotoxicity is a side effect that plagues modern drug design and is very often due to the off-target blockade of the human ether-à-go-go related gene (hERG) potassium channel. To better understand the structural determinants of this blockade, we design
Biarylphosphonite gold(I) complexes as superior catalysts for oxidative cyclization of propynyl arenes into indan-2-ones
Henrion, Guilhem,Chavas, Thomas E. J.,Le Goff, Xavier,Gagosz, Fabien
, p. 6277 - 6282 (2013/07/11)
Striking gold: A series of variously functionalized propynyl arenes was smoothly converted into indan-2-ones by a new gold(I)-catalyzed oxidative cyclization process. [LAu]NTf2 (Tf=trifluoromethanesulfonyl) is a superior catalyst both in terms of yield and kinetics for the present transformation. Copyright
Synthesis of allenes via Nickel-catalyzed cross-coupling reaction of propargylic bromides with grignard reagents
Li, Qinghan,Gau, Hanmou
experimental part, p. 747 - 750 (2012/06/29)
We describe a convenient method for the synthesis of terminal allenes from cross-coupling of propargylic bromide with Grignard reagent. The reaction of propargylic bromide with 1.2 equivalents of Grignard reagent mediated by Ni(acac)2 (2 mol%) and Ph3P (4 mol%) in THF may produce terminal allenes in good yields and high regioselectivities at room temperature. Georg Thieme Verlag Stuttgart · New York.
An efficient synthesis of isotope-labeled PD0331179 and its labeled metabolite
Zhang, Yinsheng
, p. 419 - 422 (2013/01/15)
4-[1-Methyl-2,4-dioxo-6-(3-phenyl-prop-1-ynyl)-1,4-dihydro-2H-quinazolin-3- ylmethyl]-benzoic acid, PD0331179, was under investigation as a matrix metalloproteinase-13 inhibitor. 14C-labeled and 2H-labeled PD0331179 and its 2/s
Preparation of thiolate-bridged dinuclear ruthenium complexes bearing a phosphine ligand and application to propargylic reduction of propargylic alcohols with 2-propanol
Yuki, Masahiro,Miyake, Yoshihiro,Nishibayashi, Yoshiaki
experimental part, p. 5994 - 6001 (2011/02/27)
Novel thiolate-bridged dinuclear ruthenium complexes bearing a phosphine ligand, [CpRu{PhP(C6H4-o-S)2}RuCp](OTf) 2, [CpRu{PhP(C6H4-o-S)2}RuCp(OH 2)](OTf)2, and [CpFe{PhP(C6H 4-o-S)2}RuCp](OTf)2, are prepared and characterized by X-ray analysis. These dinuclear complexes work as effective catalysts toward propargylic reduction of propargylic alcohols with 2-propanol via allenylidene complexes as key intermediates to give the corresponding alkynes in good to high yields.
ALLOSTERIC ENHANCERS OF THE A1 ADENOSINE RECEPTOR
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Page/Page column 28, (2009/12/04)
The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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Page/Page column 34-35, (2010/02/08)
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
