Structural analysis and reactivity of unusual tetrahedral intermediates enabled by SmI2-mediated reduction of barbituric acids: vinylogous N-acyliminium additions to α-hydroxy-N-acyl-carbamides.

نویسندگان

  • Michal Szostak
  • Brice Sautier
  • David J Procter
چکیده

Structural characterisation and reactivity of new tetrahedral intermediates based on a highly modular barbituric acid scaffold, formed via chemoselective electron transfer using the SmI2-H2O reagent, are reported. Lewis acid promoted cleavage of bicyclic α-amino alcohols affords vinylogous N-acyliminium ions, which undergo selective (>95 : 5, 1,4 over 1,2) capture with a suite of diverse nucleophiles in a practical sequence to biologically active uracil derivatives.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Structural analysis and reactivity of unusual tetrahedral intermediates enabled by SmI2-mediated reduction of barbituric acids: vinylogous N-acyliminium additions to a-hydroxy-N-acyl-carbamides†

Structural characterisation and reactivity of new tetrahedral intermediates based on a highly modular barbituric acid scaffold, formed via chemoselective electron transfer using the SmI2–H2O reagent, are reported. Lewis acid promoted cleavage of bicyclic a-amino alcohols affords vinylogous N-acyliminium ions, which undergo selective (>95 :5, 1,4 over 1,2) capture with a suite of diverse nucleop...

متن کامل

Selective Reduction of Barbituric Acids Using SmI2/H2O: Synthesis, Reactivity, and Structural Analysis of Tetrahedral Adducts**

Since the 1864 landmark discovery by Adolf von Baeyer, barbituric acids have played a prominent role in medicine and organic synthesis. The barbituric acid scaffold occurs in more than 5000 pharmacologically active compounds, including commonly used anticonvulsant, hypnotic, and anticancer agents (Figure 1a). Moreover, as an easily accessible feedstock material, it is an extremely useful buildi...

متن کامل

Highly Chemoselective Reduction of Amides (Primary, Secondary, Tertiary) to Alcohols using SmI2/Amine/H2O under Mild Conditions

Highly chemoselective direct reduction of primary, secondary, and tertiary amides to alcohols using SmI2/amine/H2O is reported. The reaction proceeds with C-N bond cleavage in the carbinolamine intermediate, shows excellent functional group tolerance, and delivers the alcohol products in very high yields. The expected C-O cleavage products are not formed under the reaction conditions. The obser...

متن کامل

On the Role of Pre- and Post-Electron-Transfer Steps in the SmI2/Amine/H2O-Mediated Reduction of Esters: New Mechanistic Insights and Kinetic Studies

The mechanism of the SmI2 -mediated reduction of unactivated esters has been studied using a combination of kinetic, radical clocks and reactivity experiments. The kinetic data indicate that all reaction components (SmI2 , amine, H2 O) are involved in the rate equation and that electron transfer is facilitated by Brønsted base assisted deprotonation of water in the transition state. The use of ...

متن کامل

Tetra-N-Butyl ammonium hydroxide mediated one-pot synthesis of pyrano [2, 3-d] pyrimidinone Derivatives

Tetra-N-Butyl Ammonium Hydroxide was used as a catalyst for one-pot, three component condensation reactions consisting of aromatic aldehydes, malononitrile and barbituric acid in ethanol:water solvent system at 60oC. Current method has major advantages like mild reaction conditions with simple operation, high yields, by using a less toxic and lower costlier catalyst.In conclusion, we have explo...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Chemical communications

دوره 50 19  شماره 

صفحات  -

تاریخ انتشار 2014