55373-74-5Relevant academic research and scientific papers
Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors
Kitano, Yasunori,Suzuki, Tsuyoshi,Kawahara, Eiji,Yamazaki, Takahisa
, p. 5863 - 5867 (2008/04/03)
The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC50 values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yn/en-yl)q
Synthesis of annulated oxazolidinones as potential precursors of cyclic cis-β-amino alcohols
Chudinov,Gashev,Chernysheva,Semenov
, p. 123 - 136 (2007/10/03)
A simple method for the synthesis of annulated 1,3-oxazolidin-2-ones from accessible ketones, acetylene, and carbon dioxide was developed. If their molecules contain arylalkyl substituents, intramolecular cyclization in acidic media gave rise to fused heterocyclic systems in high yields. The effects of the substituents in positions 3 and 5 of the oxazolidine ring on the regioselectivity of this cyclization were studied. The possibilities of converting oxazolidinones into cyclic cis-β-amino alcohols were studied.
Lewis base-catalyzed alkynylation of carbonyl compounds with trimethylsilylacetylenes
Kitazawa, Takayuki,Minowa, Tomofumi,Mukaiyama, Teruaki
, p. 1002 - 1003 (2007/10/03)
Alkynylation of carbonyl compounds with trimethylsilylacetylenes in the presence of a catalytic amount of Lewis bases such as acetate or phenoxide anion is described. The alkynylation proceeded under mild conditions and afforded the corresponding propargyl alcohols in good to excellent yields. Copyright
Ortho-[2,3]-wittig rearrangement of benzyl propargyl ethers: Striking preference over the competing [1,2]-wittig shift
Tomooka, Katsuhiko,Harada, Manabu,Hanji, Takayuki,Nakai, Takeshi
, p. 1394 - 1395 (2007/10/03)
Treatment of benzyl γ-(trimethylsilyl)propargyl ether with n-BuLi is shown to afford the rarely precedent ortho-[2,3]-Wittig product in remarkable preference to the [1,2]-Wittig product. The factors governing the periselectivity in this type of carbanion
The Resolution of Tertiary α-Acetylene- Acetate Esters by the Lipase from Candida Cylindracea
O'Hagan, David,Zaidi, Naveed A.
, p. 1111 - 1118 (2007/10/02)
The resolution of tertiary alcohols using the Candida cylindracea lipase is explored.In particular strategies are deployed to limit nonenzymatic hydrolysis of the tertiary acetate substrates in buffer, such that a full range of the steric requirements and
Novel substituted (4.2.0)bicyclooctane derivatives with valuable therapeutic properties
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, (2008/06/13)
Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): STR1 wherein: A is --C C--, trans --HC=CH--, --CH2 CH2 -- or --CH=CHCH2 --; X is lower alkoxy, hydroxy, or (2,2,2)-trifluoroethoxy; Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl); is an integer of 2-4; R1 is --CH2 OH, --CHO, --CO2 R or --CO2 H, and the olefin formed by the R1 (CH2)n CH= moiety is either (E) or (Z); R2 is hydrogen or methyl, or optionally --CH=CH2 when A is --CH=CHCH2 --; and R3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, STR2 --(CH2)m -phenyl or CH2 O-phenyl; in which each phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen; in which: a is an integer of 0, 1 or 2; b is an integer of 3-7; m is an integer of 0, 1 or 2; and R is STR3 wherein x is STR4 in which each R4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, and the pharmaceutically acceptable, non-toxic salts and esters thereof.
Novel 8-(lower alkyl)bicyclo[4.2.0]octane derivatives with valuable therapeutic properties
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, (2008/06/13)
Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): STR1 wherein: Y is exo-(lower alkyl) or endo-(lower alkyl); n is 2 or 3; R1 is CH2 OH, CHO, CO2 R or CO2 H; R2 is hydrogen or methyl; and R3 is linear or branched alkyl having 5-10 carbon atoms, STR2 or --(CH2)m -phenyl optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, in which a is 0, 1 or 2; b is 3-7; m is 1 or 2; and R is STR3 wherein X is STR4 in which each R4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, and the pharmaceutically acceptable, non-toxic salts and esters thereof.
Novel [4,2,0]bicyclooctane derivatives with valuable therapeutic properties
-
, (2008/06/13)
Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): STR1 wherein: n is 2 or 3; R1 is CH2 OH, CHO, CO2 R or CO2 H; R2 is hydrogen or methyl; and R3 is linear or branched alkyl having 5-10 carbon atoms, STR2 optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, in which a is 0, 1 or 2; b is 3-7; m is 1 or 2; and R is STR3 in which each R4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, and the pharmaceutically acceptable, non-toxic salts and esters thereof.
