41298-85-5Relevant articles and documents
One pot synthesis of α-N-heteroaryl ketone derivatives from aryl ketones using aqueous NaICl2
Ghodse, Shrikant M.,Hatvate, Navnath T.,Telvekar, Vikas N.
supporting information, (2021/12/08)
A simple and efficient method for the synthesis of α-heteroaryl ketones from aryl ketones and amine using aqueous sodium dichloroiodate is established. This method is mild, operationally simple, has a short reaction time, and easy workup procedure to afford the corresponding α-N-heteroaryl ketone derivatives in moderate to good yield.
Expeditious one-pot synthesis of C3-piperazinyl-substituted quinolines: Key precursors to potent c-Met inhibitors
Wang, Yuanxiang,Ai, Jing,Liu, Gang,Geng, Meiyu,Zhang, Ao
supporting information; scheme or table, p. 5930 - 5933 (2011/10/08)
An effective one-pot synthesis of quinolines bearing diverse C3-piperazinyl functions was developed by using a modified Friedlaender's protocol. The method not only enables the synthesis of our early reported c-Met inhibitor on a large scale, but also provides a way to generate novel multi-substituted quinolines for further structure-activity relationship (SAR) study.
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides
Brienne,Varech,Leclercq,Jacques,Radembino,Dessalles,Mahuzier,Gueyouche,Bories,Loiseau,Gayral
, p. 2232 - 2239 (2007/10/02)
Two series of 2-substituted 1,2-epoxyethanesulfonamides 2 and ethynesulfonamides 5 were synthesized and evaluated for their antifilarial activity. The trans epoxides 2T were stereospecifically prepared by a Darzens reaction between aldehydes and halomethanesulfonamides. The cis isomers 2c were obtained from ethynesulfonamides 5 by semihydrogenation followed by KOCl epoxidation. 2-Substituted ethynesulfonamides 5 were synthesized from appropriate trans-ethenesulfonamides by a bromination/dehydrobromination sequence. These products, as well as several synthetic intermediates, were evaluated for antifilarial activity against Molinemia dessetae either in vivo in its natural host, the rodent Proechimys oris, or in vitro by a new test using cultures of the infective larvae. Most of the epoxides 2T and acetylenic derivatives 5 bearing a 2-aryl substituent were active in vitro. Among these compounds, four epoxides 2T and one acetylenic derivative 5 showed marked macrofilaricidal activity in vivo without any microfilaricidal activity. The differences between the in vivo and in vitro results may be due, in part, to the low chemical stability of the epoxy sulfonamides 2T. Despite this limitation, the activities observed in this reliable animal model suggest further development and testing of both series 2T and 5 as macrofilaricides.