- Ethyl 2-nitroacetate as a new synthetic equivalent of ethoxycarbonylnitrile oxide
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It was shown that ethyl 2-nitroacetoacetate is a synthetic precursor of ethoxycarbonylnitrile oxide as well as of isoxazole- and isoxazoline-3-carboxylic acids and their esters.The elimination of acetic acid from ethyl 2-nitroacetoacetate occurs in a mixture of acetic acid and acetic anhydride in the presence of strong mineral acids, e.g., H2SO4, at room temperature and gives isoxazolines in yields of up to 85 - 91percent. - Key words: ethoxycarbonylnitrile oxide, isoxazoles, isoxazolines.
- Kislyi, V. P.,Laikhter, A. L.,Ugrak, B. I.,Semenov, V. V.
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- Efficient and regioselective one-pot synthesis of 3-substituted and 3,5-disubstituted isoxazoles
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(Figure Presented) A series of 3-substituted and 3,5-disubstituted isoxazoles have been efficiently synthesized in moderate to excellent yields by the reaction of N-hydroxyl-4-toluenesulfonamide with α,β-unsaturated aldehydes/ketones. This novel strategy is associated with readily available starting materials, mild conditions, high regioselectivity, and wide scope.
- Tang, Shibing,He, Jinmei,Sun, Yongquan,He, Liuer,She, Xuegong
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supporting information; experimental part
p. 3982 - 3985
(2009/12/03)
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- Ring-opening reactions of cyclopropanes. Part 8.1 Nitrosation of donor-acceptor cyclopropanes
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The reaction of 2,2-dialkoxycyclopropane-1-carboxylates 1a-d and monoalkoxycyclopropane 1e with NOCl gives isoxazoline- and/or isoxazole-3-carboxylates by regioselective ring-opening at C1-C2 bond. A mechanistic interpretation suggests the intermediacy of well-stabilised dipolar species.
- Cermola, Flavio,Di Gioia, Lucrezia,Graziano, Maria Liliana,Iesce, Maria Rosaria
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p. 677 - 681
(2007/10/03)
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- 4-[(4-(CARBOXYETHYL) PIPERIDINYL) METHYL] PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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3-Substituted pyrrolidines having a 4-carboxypiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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- 4(SPIROPIPERIDINYL)METHYL SUBSTITUTED PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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3-Substituted pyrrolidines having a spiropiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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- Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives
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The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.
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- Substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives as GABA alpha 5 ligands
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Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula
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- 1,3-Dipolar cycloaddition reaction of substituted trimethylstannylacetylenes with nitrile oxides
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1,3-Dipolar cycloaddition reaction of trimethylstannylacetylene with nitrile oxides yielded 3-substituted 5-(trimethylstannyl)isoxazoles. On the other hand, the same reaction of (trimethylstannyl)phenylacetylene, -1-hexyne, and -(trimethylsilyl)acetylene
- Sakamoto,Uchiyama,Kondo,Yamanaka
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p. 478 - 480
(2007/10/02)
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