59115-90-1Relevant academic research and scientific papers
Preparation of isoquinazolines: Via metal-free [4 + 2] cycloaddition of ynamides with nitriles
Wu, Hao,Liu, Yu,He, Ming-Xing,Wen, Hao,Cao, Wei,Chen, Ping,Tang, Yu
, p. 8408 - 8416 (2019/09/30)
TfOH-mediated [4 + 2] cycloaddition of ynamides with nitriles to construct 1,2-dihydroquinazolines is realized by a direct reaction in moderate to excellent yields (up to 93%) in a stereospecific manner. A rapid and efficient strategy has been employed for the syntheses of alkyl-substituted 1,2-dihydroquinazoline derivatives, and it exhibits good functional group tolerance, has a short reaction time, shows excellent diastereoselectivity, and is a simple and high-yielding reaction.
Br?nsted Acid-Catalyzed Intramolecular Hydroarylation of β-Benzylstyrenes
Cai, Xiao,Keshavarz, Amir,Omaque, Justin D.,Stokes, Benjamin J.
supporting information, p. 2626 - 2629 (2017/05/24)
Using triphenylmethylium tetrakis(pentafluorophenyl)borate as a convenient Br?nsted acid precatalyst, β-(α,α-dimethylbenzyl)styrenes are shown to cyclize efficiently to afford a variety of new indanes that possess a benzylic quaternary center. The geminal dimethyl-containing quaternary center is proposed to be necessary to arm the substrate for cyclization through steric biasing.
Protected amino hydroxy adamantane carboxylic acid and process for its preparation
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Paragraph 0333; 0334, (2015/11/24)
Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided. The provided compounds can be used for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
Evaluating a sodium dispersion reagent for the Bouveault-Blanc reduction of esters
An, Jie,Work, D. Neil,Kenyon, Craig,Procter, David J.
, p. 6743 - 6747 (2014/08/05)
A new sodium dispersion reagent has been evaluated for the reduction of esters. Na-D15, a sodium dispersion with sodium particle size of 5-15 μm, is a nonpyrophoric reagent that can be handled in air. In this study, a broad range of aliphatic ester substrates were reduced to primary alcohols by Na-D15/i-PrOH with good yields. The method compares favorably with modern metal hydride reductions and is much safer and efficient than the traditional Bouveault-Blanc reduction.
PYRIMIDONE DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Paragraph 1026-1027, (2014/07/22)
The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
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Paragraph 0215, (2014/02/16)
The present invention relates to a compound having the general formula (Di), (Dii), or (Diii), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
Preparation of samarium(II) iodide: Quantitative evaluation of the effect of water, oxygen, and peroxide content, preparative methods, and the activation of samarium metal
Szostak, Michal,Spain, Malcolm,Procter, David J.
supporting information; experimental part, p. 3049 - 3059 (2012/06/01)
Samarium(II) iodide (SmI2) is one of the most important reducing agents in organic synthesis. Synthetic chemistry promoted by SmI2 depends on the efficient and reliable preparation of the reagent. Unfortunately, users can experience difficulties preparing the reagent, and this has prevented realization of the full synthetic potential of SmI2. To provide synthetic chemists with general and reliable methods for the preparation of SmI2, a systematic evaluation of the factors involved in its synthesis has been carried out. Our studies confirm that SmI2 is a user-friendly reagent. Factors such as water, oxygen, and peroxide content in THF have little influence on the synthesis of SmI2. In addition, the use of specialized glovebox equipment or Schlenk techniques is not required for the preparation of SmI2. However, our studies suggest that the quality of samarium metal is an important factor and that the use of low quality metal is the main cause of failed preparations of the reagent. Accordingly, we report a straightforward method for activation of "inactive" samarium metal and demonstrate the broad utility of this protocol through the electron transfer reductions of a range of substrates using SmI2 prepared from otherwise "inactive" metal. An investigation into the stability of SmI2 solutions and an evaluation of commercially available solutions of the reagent is also reported.
An improved bouveault-blanc ester reduction with stabilized alkali metals
Bodnar, Brian S.,Vogt, Paul F.
supporting information; experimental part, p. 2598 - 2600 (2009/08/07)
Significantly improved Bouveault-Blanc conditions for ester reduction have been developed using sodium in silica gel (Na-SG), a free-flowing powder that can be easily handled in the open atmosphere. Primary alcohols were prepared in excellent yield from a variety of aliphatic esters under mild reaction conditions. The chemistry presented here is far safer than the classic Bouveault-Blanc reduction and is competitive with more modern hydride reduction methods.
Gold-catalyzed double migration-benzannulation cascade toward naphthalenes
Dudnik, Alexander S.,Schwier, Todd,Gevorgyan, Vladimir
supporting information; body text, p. 1465 - 1468 (2009/04/10)
(Chemical Equation Presented) A novel gold(I)-catalyzed cycloisomerization of propargylic esters leading to unsymmetrically substituted naphthalenes has been developed. This cascade reaction involves an unprecedented tandem sequence of 1,3- and 1,2-migration of two different migrating groups. It is believed that this transformation likely proceeds via the formation of 1,3-diene intermediate or its precursor, which upon cyclization and aromatization steps transforms into the naphthalene core. 2008 American Chemical Society.
New Synthetic Methods for Seven- and Eight-Membered Cyclic Ethers Based on the Ring-Expansion Reactions of Hydroxy or Lithioxy Methoxyallenylisochroman Derivatives
Nagao, Yoshimitsu,Tanaka, Satoru,Hayashi, Kazuhiko,Sano, Shigeki,Shiro, Motoo
, p. 481 - 484 (2007/10/03)
The Pd(0)-catalyzed ring-expansion reactions of hydroxy methoxyallenyl-4,4-dialkylisochroman derivatives in the presence of P(o-tolyl)3 proceeded smoothly via hydropalladation to give 3-benzoxepan-1-one derivatives in high yields. Treatment of
