14064-13-2Relevant 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.
Hemilabile Benzyl Ether Enables Γ-C(sp3)-H Carbonylation and Olefination of Alcohols
Tanaka, Keita,Ewing, William R.,Yu, Jin-Quan
supporting information, p. 15494 - 15497 (2019/10/16)
Pd-catalyzed C(sp3)-H activation of alcohol typically shows β-selectivity due to the required distance between the chelating atom in the attached directing group and the targeted C-H bonds. Herein we report the design of a hemilabile directing group which exploits the chelation of a readily removable benzyl ether moiety to direct Γ- or δ-C-H carbonylation and olefination of alcohols. The utility of this approach is also demonstrated in the late-stage C-H functionalization of β-estradiol to rapidly prepare desired analogues that required multi-step syntheses with classical methods.
Hemilabile Benzyl Ether Enables γ-C(sp3)-H Carbonylation and Olefination of Alcohols
Tanaka, Keita,Ewing, William R.,Yu, Jin-Quan
supporting information, (2019/10/22)
Pd-catalyzed C(sp3)-H activation of alcohol typically shows β-selectivity due to the required distance between the chelating atom in the attached directing group and the targeted C-H bonds. Herein we report the design of a hemilabile directing group which exploits the chelation of a readily removable benzyl ether moiety to direct γ- or δ-C-H carbonylation and olefination of alcohols. The utility of this approach is also demonstrated in the late-stage C-H functionalization of β-estradiol to rapidly prepare desired analogues that required multi-step syntheses with classical methods.
Catalytic Reduction of Alkyl and Aryl Bromides Using Propan-2-ol
Haibach, Michael C.,Stoltz, Brian M.,Grubbs, Robert H.
, p. 15123 - 15126 (2017/11/20)
Milstein's complex, (PNN)RuHCl(CO), catalyzes the efficient reduction of aryl and alkyl halides under relatively mild conditions by using propan-2-ol and a base. Sterically hindered tertiary and neopentyl substrates are reduced efficiently, as well as more functionalized aryl and alkyl bromides. The reduction process is proposed to occur by radical abstraction/hydrodehalogenation steps at ruthenium. Our research represents a safer and more sustainable alternative to typical silane, lithium aluminium hydride, and tin-based conditions for these reductions.
CYCLOALKYL METHOXYBENZYL PHENYL PYRAN DERIVATIVES AS SODIUM DEPENDENT GLUCOSE CO TRANSPORTER (SGLT2) INHIBITORS
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, (2012/03/26)
The invention relates to the cycloalkyl methoxybenzyl phenyl pyran derivatives as Sodium dependent glucose co transporter (SGLT) inhibitors, particularly SGLT2 and method of treating diseases, conditions and/or disorders inhibited by SGLT2 with them, and processes for preparing them.
ANDROGEN RECEPTOT-ABLATIVE AGENTS
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Page/Page column 29; 39, (2009/10/18)
Compounds of the thiazolidinedione family are provided and shown to be effective androgen receptor ablative agents that can be used in methods of treating or preventing cancer or precancer, including prostate cancer. Also provided are methods of treating
Pharmacological exploitation of the peroxisome proliferator-activated receptor γ agonist ciglitazone to develop a novel class of androgen receptor-ablative agents
Yang, Jian,Wei, Shuo,Wang, Da-Sheng,Wang, Yu-Chieh,Kulp, Samuel K.,Chen, Ching-Shih
, p. 2100 - 2107 (2008/12/22)
On the basis of our finding that the peroxisome proliferator-activated receptor γ (PPARγ) agonist ciglitazone at high doses was able to mediate PPARγ-independent transcriptional repression of androgen receptor (AR) in a tumor cell-specific manner, we used
Practical and efficient method for amino acid derivatives containing β-quaternary center: application toward synthesis of hepatitis C virus NS3 serine protease inhibitors
Arasappan, Ashok,Venkatraman, Srikanth,Padilla, Angela I.,Wu, Wanli,Meng, Tao,Jin, Yan,Wong, Jesse,Prongay, Andrew,Girijavallabhan, Viyyoor,George Njoroge
, p. 6343 - 6347 (2008/02/10)
A practical and efficient route toward synthesis of amino acid derivatives containing β-quaternary center has been developed using diastereoselective Strecker reaction. The method was employed for preparation of >100 g of β-methylcyclohexyl glycine deriva
NOVEL KETOAMIDES WITH CYCLIC P4'S AS INHIBITORS OF NS3 SERINE PROTEASE OF HEPATITIS C VIRUS
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Page/Page column 76-77, (2008/06/13)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
CYCLOBUTENEDIONE GROUPS-CONTAINING COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE
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Page/Page column 78, (2010/02/14)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
